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Evaluation of Ligustrazine-Based Synthetic Compounds for their Antiproliferative Effects

Author(s):

Syed Nasir Abbas Bukhari*, Nasser Hadal Alotaibi, Waqas Ahmad, Khalid Saad Alharbi, Mohamed A. Abdelgawad, Mohammad M. Al-Sanea, Muhammad Masood Ahmad, Muhammad Wahab Amjad, Maria Abdul Ghafoor Raja and Muhammad Ajaz Hussain   Pages 1 - 7 ( 7 )

Abstract:


Background: Ligustrazine and chalcones have been reported previously for various biological activities including anticancer effects.

Objectives: Based on the multitargeted biological activities approach of ligustrazine based chalcones, in current study 18 synthetic ligustrazine-containing α, β-unsaturated carbonyl-based 1, 3-Diphenyl-2-propen-1-one derivatives were evaluated for their inhibitory effects on growth of five different types of cancer cells.

Methods: All compounds were evaluated for anticancer effects on various cancer cell lines by propidium iodide fluorescence assay and various other assays were performed for mechanistic studies.

Results: Majority of compounds exhibited strong inhibition of cancer cells especially synthetic compounds 4a and 4b bearing 1-Pyridin-3-yl-ethanone as a ketone moiety in main structural backbone were found most powerful inhibitors of cancer cell growth. Most active 9 compounds among whole series were selected for further studies related to different cancer targets including EGFR TK kinases, tubulin polymerization, KAF and BRAFV600E.

Conclusion: Synthetic derivatives including 4a-b and 5a-b showed multitarget approach and showed strong inhibitory effects on EGFR, FAK and BRAF while three compounds including 3e bearing methoxy substitution, 4a and 4b with 1- pyridin-3-yl-ethanone moiety showed the inhibition of tubulin polymerization.

Keywords:

Claisen-Schmidt condensation, Organic synthesis, Chalcones, Cell lines, Antiproliferative.

Affiliation:

Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Aljouf, Sakaka, 2014, Department of Clinical Pharmacy, College of Pharmacy, Jouf University, Aljouf, Sakaka, 2014, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Minden, Penang, Department of Pharmacology, College of Pharmacy, Jouf University, Aljouf, Sakaka, 2014, Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Aljouf, Sakaka, 2014, Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Aljouf, Sakaka, 2014, Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Aljouf, Sakaka, 2014, College of Pharmacy, Northern Border University, Rafha, College of Pharmacy, Northern Border University, Rafha, Department of Chemistry, University of Sargodha, Sargodha 40100



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