Synthesis, modeling studies and evaluation of E-stilbene hydrazides as potent anticancer agents
Research output: Journal Publications and Reviews › RGC 21 - Publication in refereed journal › peer-review
Author(s)
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Detail(s)
Original language | English |
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Pages (from-to) | 271-281 |
Number of pages | 10 |
Journal / Publication | Journal of Molecular Structure |
Volume | 1197 |
Online published | 10 Jul 2019 |
Publication status | Published - 5 Dec 2019 |
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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, 1H NMR, 13C 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.
Research Area(s)
- Breast cancer, Docking study, Mizoroki-Heck reaction, Stilbene hydrazides
Citation Format(s)
Synthesis, modeling studies and evaluation of E-stilbene hydrazides as potent anticancer agents. / Iqbal, Ahsan; Khan, Zulfiqar Ali; Shahzad, Sohail Anjum et al.
In: Journal of Molecular Structure, Vol. 1197, 05.12.2019, p. 271-281.
In: Journal of Molecular Structure, Vol. 1197, 05.12.2019, p. 271-281.
Research output: Journal Publications and Reviews › RGC 21 - Publication in refereed journal › peer-review