Key Laboratory of Structure Based Drugs Design and Discovery of Ministry of Education

Laboratory of, China

Key Laboratory of Structure Based Drugs Design and Discovery of Ministry of Education

Laboratory of, China

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Wen J.-C.,Key Laboratory of Structure Based Drugs Design and Discovery of Ministry of Education | Jiang T.,Key Laboratory of Structure Based Drugs Design and Discovery of Ministry of Education | Bao Y.,Shenyang Pharmaceutical University | Lin X.-J.,Key Laboratory of Structure Based Drugs Design and Discovery of Ministry of Education | And 3 more authors.
Yaoxue Xuebao | Year: 2014

To simplify the macrocyclic fragment and to modify the zinc binding group of the natural product apicidin, two series of 5-hexyl (heptyl) ethanethioate derivatives were designed and synthesized. Twenty-six compounds were synthesized and confirmed with 1H NMR, IR, MS and HR-MS spectrum, which were not reported. Take vorinostat as control, their antiporliferative activities against cancer cell lines, MCF-7 and HL-60, were tested with MTT assay or trypan blue staining method. Generally in both series it was found that, the chiral carbon atom at 7 position is not necessary, compounds II-1, II-3, II-6 and 11-13 showed good activity on HL-60 cells in vitro, with the IC50 values less than 10 μmol·L-1. II-7 and II-8 showed stronger activity against MCF-7 than Vorinostat, with the IC50 of 3.19 and 6.29 μmol·L-1, respectively.

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