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

Ghada S Hassan; Shahenda M El-Messery; Fatmah A M Al-Omary; Hussein I El-Subbagh

doi:10.1016/j.bmcl.2012.08.095

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. Epub 2012 Sep 3.

Authors

Ghada S Hassan¹, Shahenda M El-Messery, Fatmah A M Al-Omary, Hussein I El-Subbagh

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.

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Humans
Neoplasms / drug therapy
Structure-Activity Relationship
Thiazoles / chemical synthesis
Thiazoles / chemistry*
Thiazoles / pharmacology*

Substances

Antineoplastic Agents
Thiazoles