Synthesis of Hybrids of Dihydropyrimidine and Pyridazinone as potential Anti-Breast Cancer Agents

Author(s): Wasim Akhtar, Garima Verma, Mohemmed Faraz Khan, Mohammad Shaquiquzzaman, Arpana Rana, Tarique Anwer, Mymoona Akhter, M. Mumtaz Alam*.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 18 , Issue 4 , 2018

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Abstract:

Background: Different 3-aroylpropionic acids and dihydropyrimidine hydrazine derivatives were condensed together to yield a series of dihydropyrimidine and pyridazinone hybrids (5a-u).

Objective: This was done in order to develop therapeutic agents for the treatment of breast cancer with improved Cycloxygenase-2 (COX-2) selectivity. In-vitro anticancer evaluation for these compounds was done against human breast cancer cell lines (MCF-7, MDA-MB-231) and normal human keratinocytes (HaCaT).

Conclusion: Amongst all the developed analogs, compound 5l emerged as the most potent agent against both these cell lines with IC50 values of 3.43 and 2.56 µM respectively. The synthesized compounds were also evaluated for COX-2 selectivity. To observe the binding pattern of the compounds with COX-2, a docking study was performed using PDB ID: 1CX2.

Keywords: Anticancer agent, breast cancer, COX-2 inhibitors, cyanopyrimidne, hybrid, pyridazinone.

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Article Details

VOLUME: 18
ISSUE: 4
Year: 2018
Page: [369 - 379]
Pages: 11
DOI: 10.2174/1389557517666170220153456
Price: $58

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