title: Synthesis of 6-N-R-Tetrazolo[1,5-c]quinazolin-5(6H)-ones and Their Anticancer Activity.
abstract: Chemical compounds with tetrazole ring are very interesting systems that can be valuable in pharmaceutical and clinical applications, especially as anticancer agents. In this work, novel 6-N-R-tetrazolo[1,5-c]quinazolin-5(6H)-ones were synthesized. A large set of IR, LC-, EI-MS, 1H, 13C NMR and elemental analysis data were collected and evaluated for their structures and purity. Details of synthesis, namely the N-alkylation, are discussed, including reactions with secondary and tertiary amides. Four new synthesized compounds (2.7, 3.2, 5.2, 5.3) were tested in vitro for anticancer activity at 10 μM against 60 cell lines of nine different cancer types: leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers. Further synthesis of substances within the series of substituted tetrazolo[1,5-c]quinazoline systems will be attempted to develop improved compounds with better anticancer activity.
authors.forename: Oleksii
authors.initials: O
authors.lastname: Antypenko
authors.forename: Sergiy
authors.initials: S
authors.lastname: Kovalenko
authors.forename: Bakhtiyor
authors.initials: B
authors.lastname: Rasulev
authors.forename: Jerzy
authors.initials: J
authors.lastname: Leszczynski
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002853:Chromatography, Liquid; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013057:Spectrum Analysis / Q000379:methods
chemical_list: D000970:Antineoplastic Agents; D052999:Quinazolinones