Author:
Ye Baijun,Gong Jianmiao,Li Qiuying,Bao Shiqi,Zhang Xuemei,Chen Jing,Meng Qing,Chen Bolin,Jiang Peng,Wang Liang,Chen Yue
Abstract
Jahanyne, a lipopeptide with a unique terminal alkynyl and OEP (2-(1-oxo-ethyl)-pyrrolidine) moiety, exhibits anticancer activity. We synthesized jahanyne and analogs modified at the OEP moiety, employing an α-fluoromethyl ketone (FMK) strategy. Preliminary bioassays indicated that compound 1b (FMK–jahanyne) exhibited decreased activities to varying degrees against most of the cancer cells tested, whereas the introduction of a fluorine atom to the α-position of a hydroxyl group (2b) enhanced activities against all lung cancer cells. Moreover, jahanyne and 2b could induce G0/G1 cell cycle arrest in a concentration-dependent manner.
Funder
Fundamental Research Funds for the Central Universities
National Natural Science Foundation of China
National Science Fund for Distinguished Young Scholars
Subject
Drug Discovery,Pharmacology, Toxicology and Pharmaceutics (miscellaneous),Pharmaceutical Science
Cited by
5 articles.
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