2. Academic Validation
  3. Synthesis and biological evaluation of 2-phenylthiazole-4-carboxamide derivatives as anticancer agents

Synthesis and biological evaluation of 2-phenylthiazole-4-carboxamide derivatives as anticancer agents

  • Eur J Med Chem. 2010 Nov;45(11):5384-9. doi: 10.1016/j.ejmech.2010.08.063.
Alireza Aliabadi 1,  Fazel Shamsa,  Seyed Nasser Ostad,  Saeed Emami,  Abbas Shafiee,  Jamshid Davoodi,  Alireza Foroumadi
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.
PMID: 20846760 DOI: 10.1016/j.ejmech.2010.08.063
Abstract

A series of substituted 2-phenylthiazole-4-carboxamide derivatives were synthesized as potential cytotoxic agents and evaluated against three human Cancer cell lines including T47D (Breast Cancer), Caco-2 (Colorectal Cancer) and HT-29 (Colon Cancer). The SAR of the arylacetamido pendent connected to the para-position of 2-phenylthiazole were explored. It was found that substitution at the 4-position by a methoxy group led to improvement of activity against Caco-2 cells while 2-methoxy substituent could maintain the high activity against HT-29 and T47D cell lines. Also, 3-fluoro analog showed good cytotoxic activity profile against all cell lines with IC(50) values less than 10 μg/mL.

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