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

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal

2 Scopus Citations
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Author(s)

  • Ahsan Iqbal
  • Zulfiqar Ali Khan
  • Sohail Anjum Shahzad
  • Syed Ali Raza Naqvi
  • Ayesha Bari
  • Hira Amjad
  • Muhammad Ihtisham Umar

Related Research Unit(s)

Detail(s)

Original languageEnglish
Pages (from-to)271-281
Number of pages10
Journal / PublicationJournal of Molecular Structure
Volume1197
Online published10 Jul 2019
Publication statusPublished - 5 Dec 2019

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; Ahmad Khan, Shakeel; Raza Naqvi, Syed Ali; Bari, Ayesha; Amjad, Hira; Umar, Muhammad Ihtisham.

In: Journal of Molecular Structure, Vol. 1197, 05.12.2019, p. 271-281.

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal