title: One-pot synthesis and in-vitro anticancer evaluation of 5-(2'-indolyl)thiazoles.
abstract: A series of 5-(2'-indolyl)thiazoles were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of thioamides 3 with 3-tosyloxypentane-2,4-dione 4 led to in situ formation of 5-acetylthiazole 5 which upon treatment with arylhydrazines 6 in polyphosphoric acid resulted in the formation of 5-(2'-indolyl)thiazoles 2. Among the synthesized 5-(2'-indolyl)thiazoles, compounds 2d-f, and 2h exhibited encouraging anticancer activity and also selectivity towards particular cell lines (IC50 = 10-30 μM). Further studies on the SAR of compound 2e may result in good anticancer activity.
authors.affiliation: Sustainable Technology Division, National Risk Management Research Laboratory, U.S. Environmental Protection Agency, 26 West Martin Luther King Drive, MS 483, Cincinnati, OH 45268, USA.
authors.forename: Buchi Reddy
authors.initials: BR
authors.lastname: Vaddula
authors.affiliation: Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India.
authors.forename: Mukund P
authors.initials: MP
authors.lastname: Tantak
authors.affiliation: Department of Natural Sciences, University of Houston - Downtown, Houston, TX 77002, USA.
authors.forename: Rachana
authors.initials: R
authors.lastname: Sadana
authors.affiliation: Sustainable Technology Division, National Risk Management Research Laboratory, U.S. Environmental Protection Agency, 26 West Martin Luther King Drive, MS 483, Cincinnati, OH 45268, USA.
authors.forename: Michael A
authors.initials: MA
authors.lastname: Gonzalez
authors.affiliation: Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, India.
authors.forename: Dalip
authors.initials: D
authors.lastname: Kumar
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor / Q000379:methods*; D045325:HCT116 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D008956:Models, Chemical; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D013844:Thiazoles