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

Eur J Med Chem. 2007 Mar;42(3):320-6. doi: 10.1016/j.ejmech.2006.10.012. Epub 2006 Dec 4.

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, (1)H NMR, (13)C 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).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Drug Screening Assays, Antitumor
  • Humans
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology*
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Male
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / pathology
  • Spectrometry, Mass, Electrospray Ionization
  • Spectrophotometry, Infrared
  • Thiazoles / chemical synthesis*
  • Thiazoles / pharmacology*

Substances

  • Antineoplastic Agents
  • Imidazoles
  • Indicators and Reagents
  • Thiazoles