Affordable Access

Substituted thiazoles VI. Synthesis and antitumor activity of new 2-acetamido- and 2 or 3-propanamido-thiazole analogs

Authors
Journal
European Journal of Medicinal Chemistry
0223-5234
Publisher
Elsevier
Volume
54
Identifiers
DOI: 10.1016/j.ejmech.2012.06.013
Keywords
  • Synthesis
  • Antitumor Screening
  • Substituted-Thiazoles
  • 1H &13C Nmr
  • Mass Spectrometry
Disciplines
  • Design

Abstract

Abstract A novel series of 2-acetamido and 2 or 3-propanamido derivatives of 4- or 5-substituted-thiazoles was designed and synthesized. Structure elucidation of the new synthesized compounds was attained by the use of 1H &13C NMR, and Mass spectrometry. Compounds were subjected to NCI in vitro assessment for their antitumor activity, at a single dose of 10μM of test compounds. Compounds bearing straight chain substituent or 4-phenyl function proved to be more active than their branched or 4-methyl congeners. Compounds 37, 41 and 42 exhibited broad spectrum antitumor activity. Compounds 23 and 27 proved lethal while compounds 18, 21, 32 and 37 showed remarkable GI values of 75.5, 69.3, 96.2 and 92.7% to the Leukemia CCRF-CEM cell line, respectively.

There are no comments yet on this publication. Be the first to share your thoughts.