Journal
ARABIAN JOURNAL OF CHEMISTRY
Volume 14, Issue 1, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.arabjc.2020.11.020
Keywords
Pyridine; Thiosemicarbazone; Phenacyl bromide; Cytotoxicity; Molecular docking
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Funding
- Deanship of Scientific Research at Umm Al-Qura University [17-MED1-03-0007]
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Ten new pyridine-linked thiazole hybrids were synthesized using a specific strategy, and their cytotoxicity against various cancer cell lines was studied. Two of the compounds showed promising anticancer activity.
Ten new pyridine linked various substituted thiazole hybrids through (hydrazonomethyl) phenoxy-acetamide spacer were synthesized. The synthetic strategy was based on the reaction of the precursor 2-(4-((2-carbamothioylhydrazono)methyl)phenoxy)-N-(pyridin-2-yl)acetamide (3) with various alpha-halogenated carbonyl compounds (namely; phenacyl bromides, ethyl bromoacetate, diethyl bromomalonate and 3-chloropentane-2,4-dione). Moreover, the cytotoxicity properties of the synthesized compounds have been studied against liver carcinoma (HepG2), laryngeal carcinoma (Hep-2), prostate cancer (PC3), breast cancer (MCF-7) and normal fibroblast cells (W138). The pyridine-thiazole compounds 7 and 10 revealed promising anticancer activity against MCF-7 and HepG2 cell lines with IC50 values in the range 5.36-8.76 mu M compared to the activity of 5-fluorouracil. Docking study provided valuable insights for binding sites of the synthesized compounds with Rho-associated protein kinase (ROCK-1). (C) 2020 The Authors. Published by Elsevier B.V. on behalf of King Saud University.
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