Synthesis,Molecular Modeling,and Biological Evaluation of Novel Chiral Thiosemicarbazone Derivatives as Potent Anticancer Agents |
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Authors: | Demet Taş demir,Ayş egü l Karakü ç ü k‐İ yidoğ an,Mustafa Ulaş li,Tuğ ba Taş kin‐Tok,Emİ ne Elç İ n Oruç ‐Emre,Hasan Bayram |
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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. |
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Keywords: | chiral amine hydrazinecarbothioamide cytotoxicity HipHop pharmacophore model |
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