Month: November 2022

Im, Jeong Kyun published the artcileN-Chlorination-induced, oxidative ring contraction of 1,4-dimethoxyphthalazines, SDS of cas: 240400-95-7, the publication is Tetrahedron Letters (2020), 61(26), 152048, database is CAplus.

A rarely explored oxidative ring contraction of electron-rich 1,2-diazine was described. Upon treatment with an electrophilic chlorinating reagent (TCICA), 1,4-dimethoxyphthalazines undergo an N-chlorination-induced ring contraction that was accompanied by the loss of one nitrogen atom. The scope of this unusual reactivity was examined with a range of 1,4-dimethoxyphthalazine derivatives In addition, a mechanism proceeding via a bicyclic species was proposed on the basis of an isolated reaction intermediate and DFT calculations

Tetrahedron Letters published new progress about 240400-95-7. 240400-95-7 belongs to phthalazine, auxiliary class Chloride,Bromide,Phthalazine, name is 6-Bromo-1,4-dichlorophthalazine, and the molecular formula is C8H3BrCl2N2, SDS of cas: 240400-95-7.

Tille, J.-C. published the artcileVascular endothelial growth factor (VEGF) receptor-2 antagonists inhibit VEGF- and basic fibroblast growth factor-induced angiogenesis in vivo and in vitro, Recommanded Product: N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine, the publication is Journal of Pharmacology and Experimental Therapeutics (2001), 299(3), 1073-1085, database is CAplus and MEDLINE.

Exponential tumor growth is angiogenesis-dependent. Vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF) are potent angiogenic inducers that act synergistically in vivo and in vitro. We assessed the effect of specific inhibitors of VEGF receptor (VEGFR)-2 tyrosine kinase activity in in vivo and in vitro models of VEGF- and bFGF-induced angiogenesis. In an implant mouse model of angiogenesis, VEGFR-2 inhibitors completely blocked angiogenesis induced by VEGF, and, surprisingly, also inhibited the effect of bFGF to various extents. In vitro, VEGF- and bFGF-induced bovine microvascular and aortic endothelial (BME and BAE) cell collagen gel invasion could be blocked by the VEGFR-2 inhibitors by 100 and ∼90%, resp. Similar results were obtained with VEGFR-1-IgG and VEGFR-3-IgG fusion proteins and with VEGFR-2 blocking antibodies. Both BME and BAE cells produce VEGF and VEGF-C, which is not modulated by bFGF. Thus, the unexpected inhibition of bFGF-induced angiogenesis by VEGFR-2 antagonists reveals a requirement for endogenous VEGF and VEGF-C in this process. These findings broaden the spectrum of mediators of angiogenesis that can be inhibited by VEGFR-2 antagonists and highlight the importance of these compounds as agents for inhibiting tumor growth sustained by both VEGF and bFGF.

Journal of Pharmacology and Experimental Therapeutics published new progress about 300842-64-2. 300842-64-2 belongs to phthalazine, auxiliary class Protein Tyrosine Kinase/RTK,VEGFR, name is N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine, and the molecular formula is C8H8O3, Recommanded Product: N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine.

Kuroboshi, Manabu published the artcileAsymmetric dihydroxylation of olefins in a chiral ligand-immobilized silica-gel/water disperse system, COA of Formula: C8H3BrCl2N2, the publication is Proceedings – Electrochemical Society (2003), 141-144, database is CAplus.

A newly designed (DHQD)₂PHAL-type ligand was synthesized and immobilized on silica gel at the phtharadine unit. Asym. dihydroxylation of olefins was carried out in a disperse system with (DHQD)₂PHAL-immobilized silica gel as a disperse phase and an aqueous NaHCO₃-K₃Fe(CN)₆ as a disperse media to give the corresponding diols in moderate to good yields and enantiomeric excess. Recycle use of the (DHQD)₂PHAL-immobilized silica gel was successfully achieved.

Proceedings – Electrochemical Society published new progress about 240400-95-7. 240400-95-7 belongs to phthalazine, auxiliary class Chloride,Bromide,Phthalazine, name is 6-Bromo-1,4-dichlorophthalazine, and the molecular formula is C8H3BrCl2N2, COA of Formula: C8H3BrCl2N2.

Im, Jeong Kyun published the artcileN-Chlorinative Ring Contraction of 1,4-Dimethoxyphthalazines via a Bicyclization/Ring-Opening Mechanism, Application of 6-Bromo-1,4-dichlorophthalazine, the publication is Synthesis (2021), 53(10), 1760-1770, database is CAplus.

An unprecedented N-chlorinative ring contraction of 1,2-diazines was discovered and investigated with an electrophilic chlorinating reagent, trichloroisocyanuric acid (TCICA). Through optimization and mechanistic anal., the assisting role of n-Bu4NCl as an exogenous nucleophile was identified and the optimized reaction conditions were applied to a range of 1,4-dimethoxyphthalazine derivatives Also, an improvement of overall efficiency was demonstrated by the use of a labile O-silyl group. A bicyclization/ring-opening mechanism inspired by the Favorskii rearrangement was proposed and supported by the DFT calculations Furthermore, the efforts on scope expansion as well as the evaluation of other electrophilic promoters revealed that the newly developed ring contraction reactivity was a unique characteristic of 1,4-dimethoxyphthalazine scaffold and TCICA.

Synthesis published new progress about 240400-95-7. 240400-95-7 belongs to phthalazine, auxiliary class Chloride,Bromide,Phthalazine, name is 6-Bromo-1,4-dichlorophthalazine, and the molecular formula is C8H3BrCl2N2, Application of 6-Bromo-1,4-dichlorophthalazine.

Bold, Guido published the artcileCGP 79787D (PTK787/ZK222584), CGP 84738, NVP-AAC789, NVP-AAD777, and related 1-anilino-(4-pyridylmethyl)phthalazines as inhibitors of VEGF- and bFGF-induced angiogenesis, Application In Synthesis of 300842-64-2, the publication is Drugs of the Future (2002), 27(1), 43-55, database is CAplus.

A review. The pharmacol. profile of the class of 1-anilino-(4-pyridylmethyl)-phthalazines is presented. 1-Anilino-(4-pyridylmethyl)phthalazines are potent, selective and orally well absorbed inhibitors of vascular endothelial growth factor (VEGF) receptor tyrosine kinases. In vitro they block VEGF-stimulated autophosphorylation of KDR expressing cells, resulting in the inhibition of survival effects of VEGF on endothelial cells. They also block platelet derived factor-mediated effects at slightly higher concentration but do not affect other pathways such as the bFGF receptor.

Drugs of the Future published new progress about 300842-64-2. 300842-64-2 belongs to phthalazine, auxiliary class Protein Tyrosine Kinase/RTK,VEGFR, name is N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine, and the molecular formula is C21H17BrN4, Application In Synthesis of 300842-64-2.

Weiss, Matthew M. published the artcileSulfonamides as Selective Na_V1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities, Name: 6-Bromo-1,4-dichlorophthalazine, the publication is Journal of Medicinal Chemistry (2017), 60(14), 5969-5989, database is CAplus and MEDLINE.

Several reports have recently emerged regarding the identification of heteroarylsulfonamides as Na_V1.7 inhibitors that demonstrate high levels of selectivity over other Na_V isoforms. The optimization of a series of internal Na_V1.7 leads that address a number of metabolic liabilities including bioactivation, PXR activation, as well as CYP3A4 induction and inhibition led to the identification of potent and selective inhibitors that demonstrated favorable pharmacokinetic profiles and were devoid of the aforementioned liabilities. The key to achieving this within a series prone to transporter-mediated clearance was the identification of a small range of optimal cLogD values and the discovery of subtle PXR SAR that was not lipophilicity dependent. This enabled the identification of compound 20, which was advanced into a target engagement pharmacodynamic model where it exhibited robust reversal of histamine-induced scratching bouts in mice.

Journal of Medicinal Chemistry published new progress about 240400-95-7. 240400-95-7 belongs to phthalazine, auxiliary class Chloride,Bromide,Phthalazine, name is 6-Bromo-1,4-dichlorophthalazine, and the molecular formula is C8H11NO, Name: 6-Bromo-1,4-dichlorophthalazine.