2. Academic Validation
  3. Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs

Substituted thiazoles VII. Synthesis and antitumor activity of certain 2-(substituted amino)-4-phenyl-1,3-thiazole analogs

  • Bioorg Med Chem Lett. 2012 Oct 15;22(20):6318-23. doi: 10.1016/j.bmcl.2012.08.095.
Ghada S Hassan 1,  Shahenda M El-Messery,  Fatmah A M Al-Omary,  Hussein I El-Subbagh
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
PMID: 22995621 DOI: 10.1016/j.bmcl.2012.08.095
Abstract

A novel series of 2-acetamido- or 2-propanamido-4-(4-substituted phenyl)-1,3-thiazoles (11-34) was designed and synthesized. Compounds were subjected to National Cancer Institute (NCI) in vitro assessment for their antitumor activity, at a single dose of 10 μM. Most of the investigated compounds exhibited broad-spectrum antitumor activity. Compounds 19 and 28 believed to be the most active members in this study, with MG-MID GI(50), TGI, and LC(50) values of 2.8, 11.4, 44.7; and 3.3, 13.1, 46.8, respectively. Compounds 19 and 28 proved to be nine and sevenfold more active than the standard antitumor drug 5-FU, respectively.

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