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- Title
Regioselective synthesis and biological studies of novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives as potential antiproliferative agents.
- Authors
Ananda, Hanumappa; Sharath Kumar, Kothanahally; Nishana, Mayilaadumveettil; Hegde, Mahesh; Srivastava, Mrinal; Byregowda, Raghava; Choudhary, Bibha; Raghavan, Sathees; Rangappa, Kanchugarakoppal
- 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, H NMR, C 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.
- Subjects
PYRAZOLES; HETEROCYCLIC compounds synthesis; CELL-mediated cytotoxicity; MITOCHONDRIAL membranes; LEUKEMIA treatment
- Publication
Molecular & Cellular Biochemistry, 2017, Vol 426, Issue 1/2, p149
- ISSN
0300-8177
- Publication type
Article
- DOI
10.1007/s11010-016-2887-7