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Synthesis and Biological Evaluation of Some Hydrazide-Hydrazone Derivatives as Anticancer Agents

Kadriye Akdağ, Fatih Tok, Sevgi Karakuş, Ömer Erdoğan, Özge Çevik, Bedia Koçyiğit-Kaymakçıoğlu

Abstract


In this study, a series of hydrazide-hydrazone derivatives (3a-3u) were synthesized and evaluated for their anticancer activities against prostate cancer cell line (PC-3), breast cancer cell line (MCF-7), colon cancer cell line (HT-29) and human umbilical vein endothelial cells (HUVEC) using MTT assay. In particular, compound 3h having a pyrrole ring was found to be the most potent derivative with IC50 = 1.32, 2.99, 1.71 µM against PC-3, MCF-7, HT-29 cancer cell lines respectively using paclitaxel as a standard compound. Furthermore, compound 3h was subjected to further biological studies such as caspase-3 activity and Annexin-V assay to evaluate their inhibitory potentials. The activity results displayed that compound 3h increased caspase-3 activation and the number of cells to early apoptosis. The additional studies like pharmacokinetics, bioavailability scores and drug-likeness properties were also evaluated. The in silico pharmacokinetics predictions displayed that the bioavailability of these compounds may be high.

 


Keywords


Hydrazone; anticancer; apoptosis; drug-likeness; MCF-7.

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DOI: http://dx.doi.org/10.17344/acsi.2022.7614

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Copyright (c) 2022 Kadriye Akdağ, Fatih Tok, Sevgi Karakuş, Ömer Erdoğan, Özge Çevik, Bedia Koçyiğit-Kaymakçıoğlu

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