6267-37-4Relevant articles and documents
Discovery of Carboline Derivatives as Potent Antifungal Agents for the Treatment of Cryptococcal Meningitis
Tu, Jie,Li, Zhuang,Jiang, Yanjuan,Ji, Changjin,Han, Guiyan,Wang, Yan,Liu, Na,Sheng, Chunquan
, p. 2376 - 2389 (2019/03/07)
Clinical treatment of cryptococcal meningitis (CM) remains a significant challenge because of the lack of effective and safe drug therapies. Developing novel CM therapeutic agents with novel chemical scaffolds and new modes of action is of great importanc
Discovery and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors
Luan, Shenglin,Ge, Qi,Chen, Yedong,Dai, Mingyang,Yang, Jinyu,Li, Kun,Liu, Dan,Zhao, Linxiang
supporting information, p. 1943 - 1948 (2017/04/07)
Myeloid cell leukemia-1 (Mcl-1) is an important antiapoptotic protein functioning through protein-protein interactions. We discovered LSL-A6 (2-((2-carbamoyl-1-(3-(4-methoxyphenoxy)propyl)-1H-indol-6-yl)oxy)acetic acid) with a novel N-substituted indole scaffold to interfere Mcl-1 binding as a novel Mcl-1 inhibitor. Molecular modeling indicated that this compound binds with Mcl-1 by interaction with P2 and R263 hot-spots. Structure modification focused on several moieties including indole core, hydrophobic tail and acidic chain were conducted and structure-activity relationship was analyzed. The most potent compound 24d which exhibited Ki value of 110?nM for interfering Mcl-1 binding was obtained after hit-to-lead modification.
Multifunctional Probe Based on Cationic Conjugated Polymers for Nitroreductase-Related Analysis: Sensing, Hypoxia Diagnosis, and Imaging
Zhang, Xiaoqian,Zhao, Qi,Li, Yanru,Duan, Xinrui,Tang, Yanli
, p. 5503 - 5510 (2017/06/19)
Nitroreductase (NTR) is overexpressed in hypoxic tumors. Moreover, hypoxia is usually considered as the most important feature of various diseases. Thus, it is important to build a sensitive and selective method for NTR detection and hypoxia diagnosis. He