Abstract
The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C16 position on human cancer cells. The cancer cells used in the present study were A549, Hela, HepG-2, BEL7402, MCF-7, and HCT116. Several of the synthesised compounds exhibited potent antiproliferative effects. The most promising compound was (E)-3-hydroxy-16-((1-(4-iodophenyl)-1H-1,2,3-triazole-4-yl)methylene)-10,13-dimet-hyl-1,3,4,7,8,9,10,11,12,13,15,16-dodecahydro-2H-cyclopenta[a]phenanthren-17(14)-one (compound 2n), which showed considerably high antiproliferative activity in the HepG-2 cell line, with an IC50 value of 9.10 µM, and considerably high activity against the MCF-7 cell line, with an IC50 value of 9.18 µM. Flow cytometry assays demonstrated that compound 2n exerted antiproliferative effects by arresting cells in the G2 phase of the cell cycle and inducing apoptosis.
Highlights
Cancer is one of the leading causes of death worldwide [1]
Several anticancer drugs have been developed with excellent cytotoxicity such as paclitaxel and cisplatin [2]
A mixture of dehydroepiandrosterone (DHEA) (2.0 mmol), aromatic aldehydes (2.1 mmol), and reaction as evident from thin-layer chromatography (TLC), the reaction solution was condensed under reduced pressure and the KOH (2.0 mmol) in EtOH (20 mL) was heated under reflux for about 1 h
Summary
Cancer is one of the leading causes of death worldwide [1]. Because of its severity, cancer is considered one of the greatest social and economic concerns for the public health-care system [2].Over the years, several anticancer drugs have been developed with excellent cytotoxicity such as paclitaxel and cisplatin [2].Many anticancer drugs are nonselective, with paclitaxel and cisplatin being no exception.their use is limited because of their inability to differentiate between normal cells and cancerous cells. Cancer is one of the leading causes of death worldwide [1]. Several anticancer drugs have been developed with excellent cytotoxicity such as paclitaxel and cisplatin [2]. Many anticancer drugs are nonselective, with paclitaxel and cisplatin being no exception. Their use is limited because of their inability to differentiate between normal cells and cancerous cells. Despite several advances made towards the diagnosis, prevention, and cure of cancer, it remains one of the major causes of human morbidity and mortality worldwide. There is a requirement for safer and more effective anticancer drugs, which is a challenge for medicinal chemists [3]
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