1042904-03-9Relevant academic research and scientific papers
Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors
Hu, Rong,Liu, Zhi-Hao,Wang, Ning-Yu,Wang, Wan-Li,Xu, Ying,Yu, Luo-Ting,Zhu, Yong-Xia,Zuo, Wei-Qiong
supporting information, (2020/08/14)
Two classes of piperazinone-containing thieno[3,2-d]pyrimidines were designed and synthesized as new PI3Kδ inhibitors in this study. Detailed SAR study with respect to the piperazinone substituents at the 6-position of thieno[3,2-d]pyrimidine core demonstrated that piperazinone-containing thieno[3,2-d]pyrimidines would be more potent and selective for PI3Kδ than their piperazine counterparts, which led to the discovery of several potent PI3Kδ inhibitors with comparable or better antiproliferative activity against a panel of non-Hodgkin lymphoma (NHL) cell lines as compared with idelalisib. Our study will promote the development of new PI3Kδ inhibitors based on piperazinone-containing thieno[3,2-d]pyrimidine scaffold.
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors
Cumming,Le,Babu,Carroll,Chen,Favreau,Gaspari,Guo,Hobbs,Huang,Iserloh,Kennedy,Kuvelkar,Li,Lowrie,McHugh,Ozgur,Pan,Parker,Saionz,Stamford,Strickland,Tadesse,Voigt,Wang,Wu,Zhang,Zhang
experimental part, p. 3236 - 3241 (2009/04/07)
Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2′ pocket.
