22303-31-7Relevant articles and documents
Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors
Du, Lifei,Wang, Xiaoyu,Cui, Guonan,Xu, Bailing
supporting information, (2020/11/30)
Pin1 is a peptidyl prolyl cis-trans isomerase (PPIase) and inhibiting Pin1 is a potential way for discovering anti-tumor agents. With an aim to find potent Pin1 inhibitors with a novel scaffold, a series of thiazole derivatives with an alicyclic heterocycles on the 2-position were designed, synthesized and tested against human Pin1. Compound 9p bearing a 2-oxa-6-azaspiro [3,3] heptane moiety on the thiazole scaffold was identified as the most potent Pin1 inhibitor of this series with an IC50 value of 0.95 μM. The structure-activity relationship (SAR) and molecular modeling study indicated that introducing an alicyclic ring with an H-bond acceptor would be a viable way to improve the binding affinity.
Design and synthesis of 2-((1H-indol-3-yl)thio)-N-phenyl-acetamides as novel dual inhibitors of respiratory syncytial virus and influenza virus A
Zhang, Guo-Ning,Li, Qiang,Zhao, Jianyuan,Zhang, Xuandi,Xu, Zhuxin,Wang, Yujia,Fu, Yuanhui,Shan, Qi,Zheng, Yanpeng,Wang, Juxian,Zhu, Mei,Li, Ziqiang,Cen, Shan,He, Jinsheng,Wang, Yucheng
supporting information, (2019/11/26)
Respiratory syncytial virus (RSV) and influenza A virus (IAV) are two of the most common viruses that cause substantial morbidity and mortality in infants, young children, elderly persons, and immunocompromised individuals worldwide. Currently, there are
3-position functionalized N (O,S)-heteroindene derivatives and application thereof in resistance of respiratory syncytial virus
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Paragraph 0096; 0099; 0100, (2018/07/30)
The invention discloses 3-position functionalized N (O,S)-heteroindene derivatives and application thereof in resistance of respiratory syncytial virus. The structures of the derivatives are describedin the description, wherein n is 0 or 1; X represents a