Chemical engineers ensure the efficiency and safety of chemical processes, adapt the chemical make-up of products to meet environmental or economic needs, and apply new technologies to improve existing processes. 1603-79-8, Name is Ethyl benzoylformate, SMILES is CCOC(=O)C(=O)C1=CC=CC=C1, belongs to phthalazine compound. In a document, author is Lu, Xiuhong, introduce the new discover, SDS of cas: 1603-79-8.
We report herein the design and synthesis of a series of optimized phthalazine compounds as novel hedgehog signaling pathway inhibitors. The 4-methylamino-piperidine moiety of Taladegib was replaced by different four, five or six-membered azacycle or azaspirocycle building blocks. The in vitro Gliluciferase assay results demonstrate that the scaffold hopping in this region afforded significant influences on Hh pathway inhibition. Pyrrolidin-3-amine moiety was found to be the best linker between pharmacophores phthalazine and fluorine substituted benzoyl group. Meanwhile the optimization of 1-methyl-1H-pyrazol by different aromatic rings was also investigated and the SAR was described. Many new derivatives were found to show potent Hh signaling inhibitory activity with nanomolar IC50 values. Among these compounds, compound 23b showed the highest inhibitory potency with an IC50 value of 0.17 nM, which was 35-fold more potent than the lead compound Taladegib and 23-fold more potent than the marketed drug Vismodegib. The selected compounds 23a and 23b also possess potent antitumor activities against medulloblastoma cells proliferation in vitro. In vivo efficacy of 23b in a ptch(+/-)p53(-/-) mouse medulloblastoma allograft model also indicated encouraging results. (C) 2017 Elsevier Masson SAS. All rights reserved.
A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 1603-79-8. SDS of cas: 1603-79-8.
Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem