title: Synthesis and biological evaluation of 2-phenylthiazole-4-carboxamide derivatives as anticancer agents.
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.
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.
authors.forename: Alireza
authors.initials: A
authors.lastname: Aliabadi
authors.forename: Fazel
authors.initials: F
authors.lastname: Shamsa
authors.forename: Seyed Nasser
authors.initials: SN
authors.lastname: Ostad
authors.forename: Saeed
authors.initials: S
authors.lastname: Emami
authors.forename: Abbas
authors.initials: A
authors.lastname: Shafiee
authors.forename: Jamshid
authors.initials: J
authors.lastname: Davoodi
authors.forename: Alireza
authors.initials: A
authors.lastname: Foroumadi
mesh_terms: D000577:Amides / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D053778:Thiazolidines; C024067:2-phenylthiazolidine-4-carboxylic acid