title: Synthesis of 1-substituted 3-aryl-5-aryl(hetaryl)-2-pyrazolines and study of their antitumor activity.
abstract: Three series of novel 1,3,5-trisubstituted 2-pyrazoline derivatives containing thiophene and benzodioxol moieties as potential antitumor agents were synthesized. The in vitro antitumor activity of the obtained compounds was determined at the National Cancer Institute (NCI). The 5-(benzo[d][1,3]dioxol-5-yl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (9a) is the most prominent of the compounds due to its remarkable activity toward leukemia (RPMI-8226), renal cancer (UO-31) and prostate cancer (DU-145) cell lines with GI(50) values of 1.88, 1.91 and 1.94 µM, respectively.
authors: Heterocyclic Compounds Research Group, Department of Chemistry, Universidad del Valle, Cali, Colombia. braulio.insuasty@correounivalle.edu.co
authors: Braulio
authors: B
authors: Insuasty
authors: Leidy
authors: L
authors: Chamizo
authors: Jhon
authors: J
authors: Muñoz
authors: Alexis
authors: A
authors: Tigreros
authors: Jairo
authors: J
authors: Quiroga
authors: Rodrigo
authors: R
authors: Abonía
authors: Manuel
authors: M
authors: Nogueras
authors: Justo
authors: J
authors: Cobo
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D052117:Benzodioxoles / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor / Q000379:methods / Q000706:statistics & numerical data; D006801:Humans; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D052117:Benzodioxoles; D011720:Pyrazoles; D013876:Thiophenes