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  • Title: Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors.
    Author: Li Y, Wang Y, Xie N, Xu M, Qian P, Zhao Y, Li S.
    Journal: Eur J Med Chem; 2015 Jul 15; 100():270-6. PubMed ID: 26140961.
    Abstract:
    Guided by the principle of nonclassical electronic isosterism and structural optimization, a series of novel HDAC inhibitors bearing a bicyclic heterocycle moiety were designed and synthesized based on the lead compound of MS-275. All the prepared compounds were evaluated for their in vitro antiproliferative activities against HCT-116, MCF-7 and A549 human cancer cell lines, all compounds exerted excellent antitumor activities. Moreover, the compound 4a exhibited an acceptable pharmacokinetic profile with bio-availability in rat of 76% and could be considered as a candidate compound for further development.
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