Abstract
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.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
