54660-14-9Relevant articles and documents
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors
Sun, Yan,Fu, Rong,Lin, Songwen,Zhang, Jingbo,Ji, Ming,Zhang, Yan,Wu, Deyu,Zhang, Kehui,Tian, Hua,Zhang, Mingyi,Sheng, Li,Li, Yan,Jin, Jing,Chen, Xiaoguang,Xu, Heng
, (2020/12/09)
As abnormal PI3K signaling is a feature of many types of cancer, the development of orally active PI3K inhibitors is of great significance for targeted cancer therapy. Through integrating strategies of reducing aromatic character/increasing the fraction of sp3 carbons together with scaffold hopping, we designed and synthesized two new series of thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives for use as PI3K inhibitors. Our structure–activity relationship studies led to the identification of thieno[2,3-d]pyrimidine 6a and thiazolo[5,4-d]pyrimidine 7a, which exhibited remarkable nanomolar PI3K potency, good antiproliferative activity, favorable pharmacokinetic properties and significant in vivo anti-cancer efficacy. Notably, thiazolo[5,4-d]pyrimidine 7a had better anti-cancer activity than thieno[2,3-d]pyrimidine 6a and is worthy of further pre-clinical evaluation for its use in cancer treatment.
Palladium-catalyzed amination of chloro-substituted 5-nitropyrimidines with amines
Liu, Meng-Meng,Mei, Qiong,Zhang, Yi-Xiao,Bai, Peng,Guo, Xiang-Hai
, p. 583 - 587 (2017/06/19)
A concise and efficient approach was developed for the synthesis of mono-substituted and di-substituted pyrimidines products via palladium-catalyzed amination of chloro-substituted 5-nitropyrimidines and amines. This synthetic methodology can produce vari
