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Synthesis,Molecular Modeling,and Biological Evaluation of Novel Chiral Thiosemicarbazone Derivatives as Potent Anticancer Agents
Authors:Demet Tademir  Ayegül Karaküük‐&#x;yidoan  Mustafa Ulali  Tuba Takin‐Tok  Em&#x;ne El&#x;n Oru‐Emre  Hasan Bayram
Abstract:A series of new chiral thiosemicarbazones derived from homochiral amines in both enantiomeric forms were synthesized and evaluated for their in vitro antiproliferative activity against A549 (human alveolar adenocarcinoma), MCF‐7 (human breast adenocarcinoma), HeLa (human cervical adenocarcinoma), and HGC‐27 (human stomach carcinoma) cell lines. Some of compounds showed inhibitory activities on the growth of cancer cell lines. Especially, compound 17b exhibited the most potent activity (IC50 4.6 μM) against HGC‐27 as compared with the reference compound, sindaxel (IC50 10.3 μM), and could be used as a lead compound to search new chiral thiosemicarbazone derivatives as antiproliferative agents. Chirality 27:177–188, 2015. © 2014 Wiley Periodicals, Inc.
Keywords:chiral amine  hydrazinecarbothioamide  cytotoxicity  HipHop  pharmacophore model
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