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Open AccessCommunication

Design, Synthesis and Biological Evaluation of Jahanyne Analogs as Cell Cycle Arrest Inducers

1
The State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, China
2
Accendatech Co., Ltd., Tianjin 300384, China
3
Collaborative Innovation Center of Chemical Science and Engineering, Tianjin 300350, China
*
Authors to whom correspondence should be addressed.
Mar. Drugs 2020, 18(3), 176; https://doi.org/10.3390/md18030176 (registering DOI)
Received: 4 March 2020 / Revised: 17 March 2020 / Accepted: 19 March 2020 / Published: 23 March 2020
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. View Full-Text
Keywords: jahanyne; α-fluoromethyl ketone; lipopeptide; G0/G1 phase arrest jahanyne; α-fluoromethyl ketone; lipopeptide; G0/G1 phase arrest
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Ye, B.; Gong, J.; Li, Q.; Bao, S.; Zhang, X.; Chen, J.; Meng, Q.; Chen, B.; Jiang, P.; Wang, L.; Chen, Y. Design, Synthesis and Biological Evaluation of Jahanyne Analogs as Cell Cycle Arrest Inducers. Mar. Drugs 2020, 18, 176.

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