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Novel styryl-heterocyclic hybrids: Synthesis, characterization and anticancer activity

[Display omitted] •Novel styryl-heterocyclic hybrids have been evaluated for their anticancer activity against HepG2, MCF-7, and T47D.•All of the compounds have superior inhibitory activity than the parent compound resveratrol.•Compound (10d) showed the best potent cytotoxicity against HepG2 and MCF...

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Published in:Results in Chemistry 2024-01, Vol.7, p.101374, Article 101374
Main Authors: Al-lehaib, Lamya A., Ali, Ehab M.M., Al-Footy, Khalid O., El-Shishtawy, Reda M.
Format: Article
Language:English
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Summary:[Display omitted] •Novel styryl-heterocyclic hybrids have been evaluated for their anticancer activity against HepG2, MCF-7, and T47D.•All of the compounds have superior inhibitory activity than the parent compound resveratrol.•Compound (10d) showed the best potent cytotoxicity against HepG2 and MCF-7.•Compound (10c) exhibited the most potent cytotoxicity against T47D. Novel styryl-heterocyclic hybrids were designed and synthesized via Knoevenagel condensation reaction between 4-(4-((5-(((4-methyl-2-oxo-2H-chromen-7-yl)oxy)methyl)-1,3,4-oxadiazol-2-yl)methyl)piperazin-1-yl)benzaldehyde and indolenine (very good yield 85.79–91.64 %) or quinoline (fair yield 43.15 %) derivatives. The synthesized compounds were characterized by spectroscopic techniques: FTIR, 1H NMR, 13C NMR, DEPT-135, and high-resolution mass HRMS (ESI+). All target compounds were evaluated for their anticancer activity against three human cells (HepG2, MCF-7, and T47D) using the MTT assay in vitro. The bioassay showed that all target compounds exhibited superior inhibitory activity than the parent compound resveratrol and lower than the reference drug (cisplatin). Among them, compound 10d showed the best cytotoxic activity against HepG2 (IC50 = 11.80 μM) and MCF-7 (IC50 = 24.55 μM). In addition, compound10c displayed the best cytotoxic activity against T47D (IC50 = 43.24 μM) in comparison to the parent compound resveratrol. Based on these findings, the indolenine-based styryl scaffold is a novel chemotype for developing anticancer drugs, so further investigation is necessary.
ISSN:2211-7156
2211-7156
DOI:10.1016/j.rechem.2024.101374