Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase was written by Staben, Steven T.;Heffron, Timothy P.;Sutherlin, Daniel P.;Bhat, Seema R.;Castanedo, Georgette M.;Chuckowree, Irina S.;Dotson, Jenna;Folkes, Adrian J.;Friedman, Lori S.;Lee, Leslie;Lesnick, John;Lewis, Cristina;Murray, Jeremy M.;Nonomiya, Jim;Olivero, Alan G.;Plise, Emile;Pang, Jodie;Prior, Wei Wei;Salphati, Laurent;Rouge, Lionel;Sampath, Deepak;Tsui, Vickie;Wan, Nan Chi;Wang, Shumei;Weismann, Christian;Wu, Ping;Zhu, Bing-Yan. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Recommanded Product: 18213-75-7 This article mentions the following:
Starting from HTS hit 1a, X-ray co-crystallization and mol. modeling were used to design potent and selective inhibitors of PI3-kinase. Bioavailablity in this series was improved through careful modulation of physicochem. properties. Compound 12 (I) displayed in vivo knockdown of PI3K pharmacodynamic markers such as pAKT, pPRAS40, and pS6RP in a PC3 prostate cancer xenograft model. In the experiment, the researchers used many compounds, for example, 5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7Recommanded Product: 18213-75-7).
5-Amino-1-methyl-1H-pyrazole-4-carboxamide (cas: 18213-75-7) belongs to pyrazole derivatives. As is the case with imidazoles, the pyrazole ring offers many opportunities to create new multiring systems that incorporate this heterocycle. The pyrazole ring is resistant to oxidation and reduction but the groups, such as alkyl and formyl attached to the ring, are oxidized to respective acids. Only electrolytic oxidation, ozonolysis, and a strong base cause ring opening.Recommanded Product: 18213-75-7
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics