title: Synthesis and in vitro anticancer activity of 2,4-azolidinedione-acetic acids derivatives.
abstract: The synthesis and evaluation of anticancer activity of 2,4-thia(imida)zolidinedione-3- and 5-acetic acids amides were described. The structures of compounds were determined by IR, (1)H NMR, and MS analysis. In vitro anticancer activity of these compounds has been tested in National Cancer Institute (NCI) and the relationships between structure and anticancer activity are discussed. Among 2,4-azolidinedione-acetic acids derivatives 2-[5-(4-chlorobenzylidene)-2,4-dioxo-imidazolidin-3-yl]-N-(2-trifluoromethyl-phenyl)-acetamide (Ic) was superior to other related compounds in terms of high selectivity for the leukemia CCRF-CEM (logGI(50)=-6.06), HL-60(TB) (logGI(50)=-6.53), MOLT-4 (logGI(50)=-6.52) and SR (logGI(50)=-6.51) cell lines.
authors.affiliation: Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, Lviv 79010, Ukraine.
authors.forename: Danylo
authors.initials: D
authors.lastname: Kaminskyy
authors.forename: Borys
authors.initials: B
authors.lastname: Zimenkovsky
authors.forename: Roman
authors.initials: R
authors.lastname: Lesyk
mesh_terms: D019342:Acetic Acid / Q000737:chemistry; D000577:Amides / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D048289:Imidazolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D048289:Imidazolidines; D045162:Thiazolidinediones; C089946:2,4-thiazolidinedione; D019342:Acetic Acid