Synthesis and biological evaluation of new imidazo[2,1-b]thiazole derivatives as anticancer agents

Karaman B., Guzeldemirci N.

MEDICINAL CHEMISTRY RESEARCH, vol.25, no.11, pp.2471-2484, 2016 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 25 Issue: 11
  • Publication Date: 2016
  • Doi Number: 10.1007/s00044-016-1684-x
  • Journal Name: MEDICINAL CHEMISTRY RESEARCH
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.2471-2484
  • Keywords: Anticancer activity, Imidazo[2, 1-b] thiazole, Arylidenehydrazide, NATIONAL-CANCER-INSTITUTE, HEPATOCELLULAR-CARCINOMA, ANTIMICROBIAL EVALUATION, ANTITUMOR-ACTIVITY, ADJUVANT THERAPY, DRUG DISCOVERY, TUMOR-CELLS, INHIBITORS, DESIGN, MECHANISMS
  • Istanbul University Affiliated: Yes

Abstract

A series of arylidenehydrazide compounds (3a-3j) were synthesized from [6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]acetic acid hydrazide. The newly synthesized compounds 3b and 3h were subjected to the National Cancer Institute's in vitro disease-oriented antitumor screening to be evaluated for antitumor activity. Compound 3b, the most potent compound examined, displayed broad spectrum antiproliferative activity against all of the tested cell lines with log(10)GI(50) values between -4.41 and -6.44. The greatest growth inhibitions were observed against an ovarian cancer cell line(OVCAR-3), a colon cancer cell line (HCT-15), two renal cancer cell lines (CAKI-1 and UO-31) and two leukemia cell lines (CCRF-CEM and SR) with log(10)GI(10) values -6.44, -6.33, -6.11, -6.30, -6.13 and -6.22, respectively.