Latham, Antony M. et al. published their research in PLoS One in 2014 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazine and phthalazinone derivatives are important owing to their significant biological activities and pharmacological properties. Both pyridazine and phthalazine give rise to very good TREPR signals in rigid media at low temperatures.Computed Properties of C20H15ClN4

In silico design and biological evaluation of a dual specificity kinase inhibitor targeting cell cycle progression and angiogenesis was written by Latham, Antony M.;Kankanala, Jayakanth;Fearnley, Gareth W.;Gage, Matthew C.;Kearney, Mark T.;Homer-Vanniasinkam, Shervanthi;Wheatcroft, Stephen B.;Fishwick, Colin W. G.;Ponnambalam, Sreenivasan. And the article was included in PLoS One in 2014.Computed Properties of C20H15ClN4 This article mentions the following:

Background: Protein kinases play a central role in tumor progression, regulating fundamental processes such as angiogenesis, proliferation and metastasis. Such enzymes are an increasingly important class of drug target with small mol. kinase inhibitors being a major focus in drug development. However, balancing drug specificity and efficacy is problematic with off-target effects and toxicity issues. Methodol.: We have utilized a rational in silico -based approach to demonstrate the design and study of a novel compound that acts as a dual inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2) and cyclin-dependent kinase 1 (CDK1). This compound acts by simultaneously inhibiting pro-angiogenic signal transduction and cell cycle progression in primary endothelial cells. JK-31 displays potent in vitro activity against recombinant VEGFR2 and CDK1/cyclin B proteins comparable to previously characterized inhibitors. Dual inhibition of the vascular endothelial growth factor A (VEGF-A)-mediated signaling response and CDK1-mediated mitotic entry elicits anti-angiogenic activity both in an endothelial-fibroblast co-culture model and a murine ex vivo model of angiogenesis. Conclusions: We deduce that JK-31 reduces the growth of both human endothelial cells and human breast cancer cells in vitro . This novel synthetic mol. has broad implications for development of similar multi-kinase inhibitors with anti-angiogenic and anti-cancer properties. In silico design is an attractive and innovative method to aid such drug discovery. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Computed Properties of C20H15ClN4).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazine and phthalazinone derivatives are important owing to their significant biological activities and pharmacological properties. Both pyridazine and phthalazine give rise to very good TREPR signals in rigid media at low temperatures.Computed Properties of C20H15ClN4

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

Kang, Kyu-Tae et al. published their research in Yakhak Hoechi in 2018 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Pyridazine and phthalazine have quite different spectroscopic properties compared with their isomers, pyrazine and quinoxaline. In addition, phthalazines are known as serotonin reuptake inhibitors and are considered as anti-depression agents.Electric Literature of C20H15ClN4

Two-cell tube formation assay system for angiogenesis research was written by Kang, Kyu-Tae. And the article was included in Yakhak Hoechi in 2018.Electric Literature of C20H15ClN4 This article mentions the following:

Blood vessels are formed by two cell types: endothelial cells and vascular mural cells. However, most in vitro angiogenesis assays are performed by only endothelial cells. Here, we developed an in vitro angiogenesis assay system using two human vascular cell precursors: endothelial colony forming cells (ECFC) and mesenchymal stem cells (MSC). The progression of tube formation was monitored by a real-time cell recorder for 24 h. Utilized an image-stitching software to increase the analyzed image area up to 9-times larger than one image from 10X object lens. Tube number was higher in ECFC+MSC than ECFC at 6 h time point, but became lower at 12 and 24 h when compared with ECFC. The length per tube was higher in ECFC+MSC than ECFC at all-time points. VEGF treatment increased tube formation in both ECFC+MSC and ECFC. Vatalanib, VEGF inhibitor, inhibited tube formation of ECFC dose-dependently. Interestingly, ECFC+MSC-induced tube formation was not changed by vatalanib, suggesting that MSC may potentiate the stability and durability of tubular structures. These results indicate that two-cell tube formation assay system can mimic in vivo angiogenic process by two vascular cells, and will be an effective pre-clin. in vitro assay model to evaluate pro- or anti-angiogenic property. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Electric Literature of C20H15ClN4).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Pyridazine and phthalazine have quite different spectroscopic properties compared with their isomers, pyrazine and quinoxaline. In addition, phthalazines are known as serotonin reuptake inhibitors and are considered as anti-depression agents.Electric Literature of C20H15ClN4

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

Maile, Madon M. et al. published their research in Anti-Angiogenesis Drug Discovery and Development in 2014 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazines, as an important class of bicyclic N-heterocycles, have attracted sizable attention due to their valuable biological and pharmacological activities. Both pyridazine and phthalazine give rise to very good TREPR signals in rigid media at low temperatures.Recommanded Product: 212141-54-3

Discovery and development of antiangiogenetic drugs in ovarian cancer was written by Maile, Madon M.;Wong, Evelyn Y. T.;Suzin, Daphne;Birrer, Nicole E.;Penson, Richard T.. And the article was included in Anti-Angiogenesis Drug Discovery and Development in 2014.Recommanded Product: 212141-54-3 This article mentions the following:

It is more than 30 years since the seminal observations by Folkman of the development of new blood vessels (angiogenesis) in tumors. Ovarian cancer remains the most lethal gynecol. malignancy in the US, and angiogenesis is a particularly important target as VEGF levels are high, manifest as ascites and pleural effusions, and the response rates to single agent bevacizumab, a recombinant humanized monoclonal antibody directed against VEGF, are the highest (16-25%) of any reported in oncol. Antiangiogenics have generally been well tolerated, but are associated with gastrointestinal perforation in 1-2%. New angiogenesis targets are being identified (ANG-2, PDGFR, FGFR, inflammation and the microenvironment), and a plethora of new agents is in clin. development: tyrosine-kinase inhibitors (sunitinib, cediranib, pazopanib), multitargeted agents (XL-184), anti-angiopoietins (trebananib), novel antivascular approaches (VB-111 and ombrabulin). Antiangiogenic therapy appears to impact PFS, but does not impact cure. In subsets of patients, it may improve overall survival (OS), and its use remains costly and controversial. Although approved in Europe, the pathway to approval of bevacizumab for ovarian cancer in the US is currently still unclear. There is a clin. need to define the role of these drugs in ovarian cancer management and to identify robust predictive biomarkers. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Recommanded Product: 212141-54-3).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazines, as an important class of bicyclic N-heterocycles, have attracted sizable attention due to their valuable biological and pharmacological activities. Both pyridazine and phthalazine give rise to very good TREPR signals in rigid media at low temperatures.Recommanded Product: 212141-54-3

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

Lee, Jonathan A. et al. published their research in PLoS One in 2015 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazines, as an important class of bicyclic N-heterocycles, have attracted sizable attention due to their valuable biological and pharmacological activities. In addition, phthalazines are known as serotonin reuptake inhibitors and are considered as anti-depression agents.Formula: C20H15ClN4

Novel phenotypic outcomes identified for a public collection of approved drugs from a publicly accessible panel of assays was written by Lee, Jonathan A.;Shinn, Paul;Jaken, Susan;Oliver, Sarah;Willard, Francis S.;Heidler, Steven;Peery, Robert B.;Oler, Jennifer;Chu, Shaoyou;Southall, Noel;Dexheimer, Thomas S.;Smallwood, Jeffrey;Huang, Ruili;Guha, Rajarshi;Jadhav, Ajit;Cox, Karen;Austin, Christopher P.;Simeonov, Anton;Sittampalam, G. Sitta;Husain, Saba;Franklin, Natalie;Wild, David J.;Yang, Jeremy J.;Sutherland, Jeffrey J.;Thomas, Craig J.. And the article was included in PLoS One in 2015.Formula: C20H15ClN4 This article mentions the following:

Phenotypic assays have a proven track record for generating leads that become first-in-class therapies. Whole cell assays that inform on a phenotype or mechanism also possess great potential in drug repositioning studies by illuminating new activities for the existing pharmacopeia. The National Center for Advancing Translational Sciences (NCATS) pharmaceutical collection (NPC) is the largest reported collection of approved small mol. therapeutics that is available for screening in a high-throughput setting. Via a wide-ranging collaborative effort, this library was analyzed in the Open Innovation Drug Discovery (OIDD) phenotypic assay modules publicly offered by Lilly. The results of these tests are publically available online at www.ncats.nih.gov/expertise/preclin./pd2 and via the PubChem Database (AID 1117321). Phenotypic outcomes for numerous drugs were confirmed, including sulfonylureas as insulin secretagogues and the anti-angiogenesis actions of multikinase inhibitors sorafenib, axitinib and pazopanib. Several novel outcomes were also noted including the Wnt potentiating activities of rotenone and the antifolate class of drugs, and the anti-angiogenic activity of cetaben. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Formula: C20H15ClN4).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazines, as an important class of bicyclic N-heterocycles, have attracted sizable attention due to their valuable biological and pharmacological activities. In addition, phthalazines are known as serotonin reuptake inhibitors and are considered as anti-depression agents.Formula: C20H15ClN4

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

El-Helby, Abdel-Ghany A. et al. published their research in Archiv der Pharmazie (Weinheim, Germany) in 2017 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Like many other isomeric benzodiazines, phthalazine derivatives reveal numerous pharmacological and biological activities such as antimicrobial, antidiabetic, analgesic, anticonvulsant, antitumor, antiproliferative, antiepileptic, anti-inflammatory, and vasorelaxant. In addition, phthalazines are known as serotonin reuptake inhibitors and are considered as anti-depression agents.Safety of N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine

Design, Synthesis, Molecular Docking, and Anticancer Activity of Phthalazine Derivatives as VEGFR-2 Inhibitors was written by El-Helby, Abdel-Ghany A.;Ayyad, Rezk R. A.;Sakr, Helmy;El-Adl, Khaled;Ali, Mamdouh M.;Khedr, Fathalla. And the article was included in Archiv der Pharmazie (Weinheim, Germany) in 2017.Safety of N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine This article mentions the following:

Novel series of phthalazine derivatives 6-11 were designed, synthesized, and evaluated for their anticancer activity against two human tumor cell lines, HCT-116 human colon adenocarcinoma and MCF-7 breast cancer cells, targeting the VEGFR-2 enzyme. Compounds 7a,b and 8b,c showed the highest anticancer activities against both HCT116 human colon adenocarcinoma cells with IC50 of 6.04 ± 0.30, 13.22 ± 0.22, 18 ± 0.20, and 35 ± 0.45 μM, resp., and MCF-7 breast cancer cells with IC50 of 8.8 ± 0.45, 17.9 ± 0.50, 25.2 ± 0.55, and 44.3 ± 0.49 μM, resp., in comparison to sorafenib as reference drug with IC50 of 5.47 ± 0.3 and 7.26 ± 0.3 μM, resp. Eleven compounds in this series were further evaluated for their inhibitory activity against VEGFR-2, where compounds 7a, 7b, 8c, and 8b also showed the highest VEGFR-2 inhibition with IC50 of 0.11 ± 0.01, 0.31 ± 0.03, 0.72 ± 0.08, and 0.91 ± 0.08 μM, resp., in comparison to sorafenib as reference ligand with IC50 of 0.1 ± 0.02. Furthermore, mol. docking studies were performed for all synthesized compounds to predict their binding pattern and affinity towards the VEGFR-2 active site, in order to rationalize their anticancer activity in a qual. way. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Safety of N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Like many other isomeric benzodiazines, phthalazine derivatives reveal numerous pharmacological and biological activities such as antimicrobial, antidiabetic, analgesic, anticonvulsant, antitumor, antiproliferative, antiepileptic, anti-inflammatory, and vasorelaxant. In addition, phthalazines are known as serotonin reuptake inhibitors and are considered as anti-depression agents.Safety of N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

Gohlke, Bjoern-Oliver et al. published their research in BMC Bioinformatics in 2015 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Like many other isomeric benzodiazines, phthalazine derivatives reveal numerous pharmacological and biological activities such as anticonvulsant, antitumor, antiproliferative, antiepileptic, anti-inflammatory, and vasorelaxant. Phthalazine derivatives are also considered as p38MAP kinase inhibitors, selective binders of gamma-aminobutyric acid (GABA) receptors, cyclooxygenase-2 (COX-2) inhibitors, and high-affinity ligands of voltages gated calcium channels.Formula: C20H15ClN4

2D and 3D similarity landscape analysis identifies PARP as a novel off-target for the drug Vatalanib was written by Gohlke, Bjoern-Oliver;Overkamp, Tim;Richter, Anja;Richter, Antje;Daniel, Peter T.;Gillissen, Bernd;Preissner, Robert. And the article was included in BMC Bioinformatics in 2015.Formula: C20H15ClN4 This article mentions the following:

Background: Searching for two-dimensional (2D) structural similarities is a useful tool to identify new active compounds in drug-discovery programs. However, as 2D similarity measures neglect important structural and functional features, similarity by 2D might be underestimated. In the present study, we used combined 2D and three-dimensional (3D) similarity comparisons to reveal possible new functions and/or side-effects of known bioactive compounds Results: We utilized more than 10,000 compounds from the SuperTarget database with known inhibition values for twelve different anti-cancer targets. We performed all-against-all comparisons resulting in 2D similarity landscapes. Among the regions with low 2D similarity scores are inhibitors of vascular endothelial growth factor receptor (VEGFR) and inhibitors of poly ADP-ribose polymerase (PARP). To demonstrate that 3D landscape comparison can identify similarities, which are untraceable in 2D similarity comparisons, we analyzed this region in more detail. This 3D anal. showed the unexpected structural similarity between inhibitors of VEGFR and inhibitors of PARP. Among the VEGFR inhibitors that show similarities to PARP inhibitors was Vatalanib, an oral “multi-targeted” small mol. protein kinase inhibitor being studied in phase-III clin. trials in cancer therapy. An in silico docking simulation and an in vitro HT universal colorimetric PARP assay confirmed that the VEGFR inhibitor Vatalanib exhibits off-target activity as a PARP inhibitor, broadening its mode of action. Conclusion: In contrast to the 2D-similarity search, the 3D-similarity landscape comparison identifies new functions and side effects of the known VEGFR inhibitor Vatalanib. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Formula: C20H15ClN4).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Like many other isomeric benzodiazines, phthalazine derivatives reveal numerous pharmacological and biological activities such as anticonvulsant, antitumor, antiproliferative, antiepileptic, anti-inflammatory, and vasorelaxant. Phthalazine derivatives are also considered as p38MAP kinase inhibitors, selective binders of gamma-aminobutyric acid (GABA) receptors, cyclooxygenase-2 (COX-2) inhibitors, and high-affinity ligands of voltages gated calcium channels.Formula: C20H15ClN4

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

Ali, Sehar et al. published their research in PLoS One in 2021 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Like many other isomeric benzodiazines, phthalazine derivatives reveal numerous pharmacological and biological activities such as antimicrobial, antidiabetic, analgesic, anticonvulsant, antitumor, antiproliferative, antiepileptic, anti-inflammatory, and vasorelaxant. Phthalazine derivatives are also considered as p38MAP kinase inhibitors, selective binders of gamma-aminobutyric acid (GABA) receptors, cyclooxygenase-2 (COX-2) inhibitors, and high-affinity ligands of voltages gated calcium channels.Product Details of 212141-54-3

Changes in the tumor microenvironment and outcome for TME-targeting therapy in glioblastoma: A pilot study was written by Ali, Sehar;Borin, Thaiz F.;Piranlioglu, Raziye;Ara, Roxan;Lebedyeva, Iryna;Angara, Kartik;Achyut, Bhagelu R.;Arbab, Ali Syed;Rashid, Mohammad H.. And the article was included in PLoS One in 2021.Product Details of 212141-54-3 This article mentions the following:

Glioblastoma (GBM) is a hypervascular and aggressive primary malignant tumor of the central nervous system. Recent investigations showed that traditional therapies along with antiangiogenic therapies failed due to the development of post-therapy resistance and recurrence. Previous investigations showed that there were changes in the cellular and metabolic compositions in the tumor microenvironment (TME). It can be said that tumor cell-directed therapies are ineffective and rethinking is needed how to treat GBM. It is hypothesized that the composition of TME-associated cells will be different based on the therapy and therapeutic agents, and TME-targeting therapy will be better to decrease recurrence and improve survival. Therefore, the purpose of this study is to determine the changes in the TME in respect of T-cell population, M1 and M2 macrophage polarization status, and MDSC population following different treatments in a syngeneic model of GBM. In addition to these parameters, tumor growth and survival were also studied following different treatments. The results showed that changes in the TME-associated cells were dependent on the therapeutic agents, and the TME-targeting therapy improved the survival of the GBM bearing animals. The current GBM therapies should be revisited to add agents to prevent the accumulation of bone marrow-derived cells in the TME or to prevent the effect of immune-suppressive myeloid cells in causing alternative neovascularization, the revival of glioma stem cells, and recurrence. Instead of concurrent therapy, a sequential strategy would be better to target TME-associated cells. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Product Details of 212141-54-3).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Like many other isomeric benzodiazines, phthalazine derivatives reveal numerous pharmacological and biological activities such as antimicrobial, antidiabetic, analgesic, anticonvulsant, antitumor, antiproliferative, antiepileptic, anti-inflammatory, and vasorelaxant. Phthalazine derivatives are also considered as p38MAP kinase inhibitors, selective binders of gamma-aminobutyric acid (GABA) receptors, cyclooxygenase-2 (COX-2) inhibitors, and high-affinity ligands of voltages gated calcium channels.Product Details of 212141-54-3

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

Santiago, Daniel N. et al. published their research in Journal of Chemical Information and Modeling in 2012 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives.Like many other isomeric benzodiazines, phthalazine derivatives reveal numerous pharmacological and biological activities such as analgesic, anticonvulsant, antitumor, antiproliferative. As with cinnolines, phthalazines were also prepared most frequently through condensations of hydrazine derivatives and carbonyl-containing compounds.Recommanded Product: N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine

Virtual Target Screening: Validation Using Kinase Inhibitors was written by Santiago, Daniel N.;Pevzner, Yuri;Durand, Ashley A.;Tran, MinhPhuong;Scheerer, Rachel R.;Daniel, Kenyon;Sung, Shen-Shu;Woodcock, H. Lee III;Guida, Wayne C.;Brooks, Wesley H.. And the article was included in Journal of Chemical Information and Modeling in 2012.Recommanded Product: N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine This article mentions the following:

Computational methods involving virtual screening could potentially be employed to discover new biomol. targets for an individual mol. of interest (MOI). However, existing scoring functions may not accurately differentiate proteins to which the MOI binds from a larger set of macromols. in a protein structural database. An MOI will most likely have varying degrees of predicted binding affinities to many protein targets. However, correctly interpreting a docking score as a hit for the MOI docked to any individual protein can be problematic. In our method, which we term “Virtual Target Screening (VTS)”, a set of small drug-like mols. are docked against each structure in the protein library to produce benchmark statistics. This calibration provides a reference for each protein so that hits can be identified for an MOI. VTS can then be used as tool for: drug repositioning (repurposing), specificity and toxicity testing, identifying potential metabolites, probing protein structures for allosteric sites, and testing focused libraries (collection of MOIs with similar chemotypes) for selectivity. To validate our VTS method, twenty kinase inhibitors were docked to a collection of calibrated protein structures. Here, we report our results where VTS predicted protein kinases as hits in preference to other proteins in our database. Concurrently, a graphical interface for VTS was developed. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Recommanded Product: N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives.Like many other isomeric benzodiazines, phthalazine derivatives reveal numerous pharmacological and biological activities such as analgesic, anticonvulsant, antitumor, antiproliferative. As with cinnolines, phthalazines were also prepared most frequently through condensations of hydrazine derivatives and carbonyl-containing compounds.Recommanded Product: N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

Arena, Claudia et al. published their research in BioMed Research International in 2018 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazine and phthalazinone derivatives are important owing to their significant biological activities and pharmacological properties. As with pyridazines, phthalazines, the other benzopyridazines, were also prepared most frequently through the condensation of hydrazines with carbonyl-containing compounds, typically phthalate derivatives. COA of Formula: C20H15ClN4

Stomatitis and VEGFR-tyrosine kinase inhibitors (VR-TKIs): a review of current literature in 4369 patients was written by Arena, Claudia;Troiano, Giuseppe;De Lillo, Alfredo;Testa, Nunzio F.;Lo Muzio, Lorenzo. And the article was included in BioMed Research International in 2018.COA of Formula: C20H15ClN4 This article mentions the following:

Background. Multitargeted tyrosine kinase inhibitors (TKIs) represent a new class of target-specific antineoplastic agents. These agents show some specific adverse events such as fatigue/asthenia, anorexia/loss of appetite, dysgeusia, diarrhea/abdominal pain, hypothyroidism, hypertension, myelosuppression, and stomatitis. Materials and Methods. A systematic search was performed on PubMed online database using a combination of MESH terms and free text words, “sunitinib” OR “sorafenib” OR “axitinib” OR “cabozantinib” OR “pazopanib” OR “regorafenib” OR “nintedanib” OR “vatalanib” combined through the use of Boolean operator AND with the key words”stomatitis” OR “mucositis,” (i) on human subjects, (ii) written in the English language, and (iii) reporting about the incidence of stomatitis or oral mucositis. Results.. The incidence of stomatitis of any grade was 35.2% for sunitinib, 20.52% for sorafenib, 20.63% for axitinib, and 34.21% for cabozantinib. All the agents showed high rates of lowgrade stomatitis (G1-G2), while the onset of severe stomatitis (G3-G4) was very low. Conclusions. Anal. of the reports with patients treated with sunitinib, sorafenib, axitinib, and cabozantinib showed a clear prevalence of stomatitis grade 1 or grade 2. These data differ from those of patients treated with conventional chemotherapy in which mucositis is predominantly of grade 3 or grade 4. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3COA of Formula: C20H15ClN4).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazine and phthalazinone derivatives are important owing to their significant biological activities and pharmacological properties. As with pyridazines, phthalazines, the other benzopyridazines, were also prepared most frequently through the condensation of hydrazines with carbonyl-containing compounds, typically phthalate derivatives. COA of Formula: C20H15ClN4

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem

Li, Yan et al. published their research in Journal of Chemical Information and Modeling in 2016 | CAS: 212141-54-3

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Although, N-containing heterocyclic compounds are widely distributed in nature, the presence of two adjacent nitrogen atoms in the phthalazine ring makes it rare and not very familiar in isolated extracts from living organisms. Phthalazine derivatives are also considered as p38MAP kinase inhibitors, selective binders of gamma-aminobutyric acid (GABA) receptors, cyclooxygenase-2 (COX-2) inhibitors, and high-affinity ligands of voltages gated calcium channels.Synthetic Route of C20H15ClN4

AutoT&T v.2: An Efficient and Versatile Tool for Lead Structure Generation and Optimization was written by Li, Yan;Zhao, Zhixiong;Liu, Zhihai;Su, Minyi;Wang, Renxiao. And the article was included in Journal of Chemical Information and Modeling in 2016.Synthetic Route of C20H15ClN4 This article mentions the following:

In structure-based drug design, automated de novo design methods are helpful tools for lead discovery as well as lead optimization. In a previous study the authors reported a new de novo design method, namely, Automatic Tailoring and Transplanting (AutoT&T). It overcomes some intrinsic problems in conventional fragment-based buildup methods. In this study, the authors describe an upgraded version, namely, AutoT&T2. Structural operations conducted by AutoT&T2 have been largely optimized by introducing several new algorithms. As a result, its overall speed in multiround optimization jobs has been improved by a few thousand fold. With this improvement, it is now practical to conduct structural crossover among multiple lead mols. using AutoT&T2. Three different test cases are described in this study that demonstrate the new features and versatile applications of AutoT&T2. The AutoT&T2 software suite is available to the public. Besides, a Web portal for running AutoT&T2 online is provided at http://www.sioc-ccbg.ac.cn/software/att2 for testing. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Synthetic Route of C20H15ClN4).

N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Although, N-containing heterocyclic compounds are widely distributed in nature, the presence of two adjacent nitrogen atoms in the phthalazine ring makes it rare and not very familiar in isolated extracts from living organisms. Phthalazine derivatives are also considered as p38MAP kinase inhibitors, selective binders of gamma-aminobutyric acid (GABA) receptors, cyclooxygenase-2 (COX-2) inhibitors, and high-affinity ligands of voltages gated calcium channels.Synthetic Route of C20H15ClN4

Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem