24091-92-7Relevant articles and documents
Ogura et al.
, p. 2219 (1975)
Extensive investigation of benzylic N-containing substituents on the pyrrolopyrimidine skeleton as Akt inhibitors with potent anticancer activity
Chen, Xin,Guo, Kaiwen,Liu, Yang,Ran, Fansheng,Zhang, Zhen,Zhao, Guisen
, (2020/03/03)
Continuous optimization of benzylic substituents on 1-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperazin-1-yl)-2-phenylethan-1-one structure as Akt inhibitors was described in this paper. Particularly, compounds 8 and 14g exhibited high enzymatic potency against all Akt isoforms and antiproliferative effects in mantle cell lymphoma cell lines, as well as favorable cytotoxicities in patient primary cancer cells. Low micromolar doses of both 8 and 14g dose-dependently induced cell apoptosis and G2/M cell cycle arrest, also suppressed the phosphorylation level of Akt downstream targets GSK3β and S6.
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization
Liu, Kun,Kurukulasuriya, Ravi,Dykstra, Kevin,DiMichelle, Lisa,Liu, Jinchu,Vachal, Petr,Ogawa, Anthony,DeVita, Robert J.,Shen, Dong-Ming,Tan, Qiang,Chen, Yili,Gauthier, Don,Verras, Andreas,Crespo, Alejandro,Zamlynny, Beata,Madwed, Jeffrey,Hoek, Maarten,Bateman, Thomas,Yang, Yun-Fang,Houk,Krska, Shane,Cernak, Tim
, p. 1854 - 1858 (2019/05/21)
The derivatization of pharmaceuticals is a core activity in the discovery and development of new medicines. Late-stage functionalization via modern C–H functionalization chemistry has emerged as a powerful technique with which to diversify advanced pharma