Synthesis, molecular modeling, and biological evaluation of novel chiral thiosemicarbazone derivatives as potent anticancer agents.
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 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.
Gaziantep University, Faculty of Science and Arts, Department of Chemistry, Gaziantep, Turkey.
Demet
D
Taşdemir
Ayşegül
A
Karaküçük-İyidoğan
Mustafa
M
Ulaşli
Tuğba
T
Taşkin-Tok
Emİne Elçİn
EE
Oruç-Emre
Hasan
H
Bayram
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells / Q000187:drug effects; D008958:Models, Molecular; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000737:chemistry*
D000970:Antineoplastic Agents; D013882:Thiosemicarbazones
HipHop; chiral amine; cytotoxicity; hydrazinecarbothioamide; pharmacophore model