title: Synthesis and antitumor activity of novel pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-5-one derivatives.
abstract: A series of new pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidines with different substituents at position 3 were synthesized. The effect of the newly synthesized compounds was tested in vitro on human breast adenocarcinoma cell line (MCF7). Some of the synthesized compounds exploited potent antitumor activity, especially the 3-amino derivative 12 which displayed the highest activity among the test compounds with IC50 equal to 3.74 μg/mL.
authors.affiliation: Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 33 Kasr El-Aini Street, Cairo 11562, Egypt. hala_bakr@hotmail.com
authors.forename: Hala B
authors.initials: HB
authors.lastname: El-Nassan
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D011744:Pyrimidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C560935:3-amino-6-(4-chlorophenyl)-8-phenyl-1H-pyrido(2,3-d)(1,2,4)triazolo(4,3-a)pyrimidin-5-one; D000970:Antineoplastic Agents; D011744:Pyrimidinones; D014230:Triazoles