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

BAYTAŞ S., Inceler N., Yilmaz A.

MEDICINAL CHEMISTRY RESEARCH, cilt.22, sa.10, ss.4893-4908, 2013 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 22 Sayı: 10
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1007/s00044-013-0505-8
  • Dergi Adı: MEDICINAL CHEMISTRY RESEARCH
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.4893-4908
  • Anahtar Kelimeler: 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 Üniversitesi Adresli: Evet

Özet

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.