Synthesis and primary cytotoxicity evaluation of new imidazo[2,1-b]thiazole derivatives

Gursoy E., Guzeldemirci N. U.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol.42, no.3, pp.320-326, 2007 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 42 Issue: 3
  • Publication Date: 2007
  • Doi Number: 10.1016/j.ejmech.2006.10.012
  • Journal Name: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.320-326
  • Keywords: imidazo[2,1-b]thiazole, arylidenehydrazide, cytotoxicity, NATIONAL-CANCER-INSTITUTE, ANTI-TUMOR AGENTS, DRUG DISCOVERY, IMIDAZO<2,1-B>THIAZOLES
  • Istanbul University Affiliated: Yes

Abstract

A series of arylidenehydrazides (3a-3i) were synthesized from [6-(4-bromophenyl)imidazo[2,1-b] thiazol-3-yl] acetic acid hydrazide. The structures of new compounds were determined by analytical and spectral (IR, H-1 NMR, C-13 NMR, EIMS) methods. The synthesized compounds (3a-3i) were evaluated in the National Cancer Institute's 3-cell line, one dose in vitro primary cytotoxicity assay. Compounds 3a-3c, 3h and 3i which passed the criteria for activity in this assay were scheduled automatically for evaluation against the full panel of 60 human tumour cell lines at a minimum of five concentrations at 10-fold dilutions. Compounds 3c demonstrated the most marked effects on a prostate cancer cell line (PC-3, log(10) GI(50) value < -8.00). (c) 2006 Elsevier Masson SAS. All rights reserved.