Synthesis, cytotoxicity, and molecular properties prediction of novel 1,3-diarylpyrazole derivatives

BAYTAŞ S., Inceler N., Yilmaz A.

MEDICINAL CHEMISTRY RESEARCH, vol.22, no.10, pp.4893-4908, 2013 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 22 Issue: 10
  • Publication Date: 2013
  • Doi Number: 10.1007/s00044-013-0505-8
  • Journal Name: MEDICINAL CHEMISTRY RESEARCH
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.4893-4908
  • Keywords: Synthesis, Anticancer activity, 1H-Pyrazoles, Pyridine, MTT, PRELIMINARY BIOLOGICAL EVALUATION, RAPID COLORIMETRIC ASSAY, HYDRAZONE DERIVATIVES, PYRAZOLE DERIVATIVES, POTENTIAL AGENTS, APOPTOSIS, DISCOVERY, DESIGN, GROWTH, CELLS
  • Gazi University Affiliated: Yes

Abstract

A novel combinatorial library of ester and amide derivatives of 1,3-diarylpyrazoles was designed and synthesized. Anticancer activities of these compounds were assessed against MCF7, MDA-MB-231, HeLa, Raji, and HL60 human cancer cells by MTT assay. Out of these, compounds 4c and 5f were found as the most promising anticancer agents with IC50 values of 8.12 and 9.63 mu M in Raji cells, respectively. All compounds exhibited suitable drug-like characteristics according to Lipinski's rule.