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Synthesis, modeling studies and evaluation of E-stilbene hydrazides as potent anticancer agents

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Abstract A group of new thermodynamically more stable E -2-styrylbenzohydrazide derivatives ( 5a-i ) were synthesized via palladium catalyzed Mizoroki-Heck reaction conditions. All synthesized compounds were characterized by UV-visible, FT-IR,… Click to show full abstract

Abstract A group of new thermodynamically more stable E -2-styrylbenzohydrazide derivatives ( 5a-i ) were synthesized via palladium catalyzed Mizoroki-Heck reaction conditions. All synthesized compounds were characterized by UV-visible, FT-IR, 1 H NMR, 13 C NMR, mass spectrometry and elemental analysis. Anticancer potential of all synthesized E -stilbene analogues ( 5a-i ) were investigated via cell proliferation assay and apoptosis by Hoechst 33258 staining assay. The most active compound ( 5e) showed significant anticancer potential against estrogen dependent human breast cancer cells (MCF-7). The cell viability and apoptosis of compound ( 5e ) was found 56 ± 0.06% and 80.09 ± 0.07% respectively as compared to standard drug (Doxorubicin) with cell viability of 62 ± 0.03% and apoptosis 73.69 ± 0.05%. Docking studies revealed higher efficacy of compound ( 5e ) owing to its better binding affinity and ligand efficiency scores (Ki = 0.000076 nMol). All stilbene hydrazides ( 5a-i ) exhibited significant anticancer activity against human breast cancer cells (MCF-7). Therefore, stilbene analogues with hydrazide moiety may offer immense potential for future therapeutic and pharmaceutical applications.

Keywords: evaluation stilbene; modeling studies; studies evaluation; stilbene hydrazides; synthesis modeling; stilbene

Journal Title: Journal of Molecular Structure
Year Published: 2019

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