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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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