Regioselective synthesis and biological studies of novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives as potential antiproliferative agents

Ananda, H. and Sharath Kumar, K. S. and Nishana, M. and Hegde, Mahesh and Srivastava, Mrinal and Raghava, B. and Choudhary, Bibha and Raghavan, S. C. and Rangappa, K. S. (2017) Regioselective synthesis and biological studies of novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives as potential antiproliferative agents. Molecular and Cellular Biochemistry, 426 (1). pp. 149-160. ISSN 1573-4919

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Abstract

Pyrazole moiety represents an important category of heterocyclic compound in pharmaceutical and medicinal chemistry. The novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives were synthesized with complementary regioselectivity. The chemical structures were confirmed by IR, 1H NMR, 13C NMR, and mass spectral analysis. The chemical entities were screened in various cancer cell lines to assess their cell viability activity. Results showed that the compound 3-(1-(4-bromophenyl)-5-phenyl-1H-pyrazol-3-yl) pyridine (5d) possessed maximum cytotoxic effect against breast cancer and leukemic cells. The cytotoxicity was confirmed by live--dead cell assay and cell cycle analysis. Mitochondrial membrane potential, Annexin V-FITC staining, DNA fragmentation, Hoechst staining, and western blot assays revealed the ability of compound 5d to induce cell death by activating apoptosis in cancer cells. Thus, the present study demonstrates that compound 5d could be an attractive chemical entity for the development of small molecule inhibitors for treatment of leukemia and breast cancer.

Item Type:	Article
Uncontrolled Keywords:	Pyrazole, Regioselectivity, Dithioesters, Breast cancer, MCF7, Apoptosis
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	C Swapna Library Assistant
Date Deposited:	14 Jun 2019 09:20
Last Modified:	28 Jun 2019 05:18
URI:	http://eprints.uni-mysore.ac.in/id/eprint/3090

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