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Design and Synthesis of Novel Cytotoxic Indole-Thiosemicarbazone Derivatives: Biological Evaluation and Docking Study Publisher Pubmed

Summary: A study found a new compound fights lung and liver cancer cells effectively, surpassing standard drugs. #CancerResearch #NewTreatments

Bakherad Z1 ; Safavi M2 ; Fassihi A1 ; Sadeghialiabadi H1 ; Bakherad M3 ; Rastegar H4 ; Saeedi M5, 6 ; Ghasemi JB7 ; Saghaie L1 ; Mahdavi M8
Authors

Source: Chemistry and Biodiversity Published:2019


Abstract

In this work, two novel series of indole-thiosemicarbazone derivatives were designed, synthesized, and evaluated for their cytotoxic activity against MCF-7, A-549, and Hep-G2 cell lines in comparison to etoposide and colchicine as the reference drugs. Generally, the synthesized compounds showed better cytotoxicity towards A-549 and Hep-G2 than MCF-7. Among them, (2E)-2-{[2-(4-chlorophenyl)-1H-indol-3-yl]methylidene}-N-(4-methoxyphenyl)hydrazinecarbothioamide (8l) was found to be the most potent compound against A-549 and Hep-G2, at least three times more potent than etoposide. The morphological analysis by the acridine orange/ethidium bromide double staining test and flow cytometry analysis indicated that compound 8l induced apoptosis in A-549 cells. Moreover, molecular docking methodology was exploited to elucidate the details of molecular interactions of the studied compounds with putative targets. © 2019 Wiley-VHCA AG, Zurich, Switzerland
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