Design, Synthesis and Biological Evaluation of Jahanyne Analogs as Cell Cycle Arrest Inducers
Open Access
- 22 March 2020
- journal article
- research article
- Published by MDPI AG in Marine Drugs
- Vol. 18 (3), 176
- https://doi.org/10.3390/md18030176
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.Funding Information
- Fundamental Research Funds for the Central Universities (xxxxx)
- National Natural Science Foundation of China (81573282 and 81703350)
- National Science Fund for Distinguished Young Scholars (81625021)
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