Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 7, Pages 2639-2644Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.02.028
Keywords
5-Aminotetrazole; Tetrazolopyrimidine; Formyl salt; Anti-tumor cytotoxicity; EAC; HepG2; Apoptosis
Funding
- Faculty of Science, Beni-Suef University, Egypt
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An easy and efficient route for the synthesis of some tetrazolo[1,5-a]-pyrimidine derivatives was described through the reaction of sodium salts of formyl cycloalkanones with 5-aminotetrazole monohydrate. The derivative 6,7,8,9-tetrahydrotetrazolo[1,5-a]quinazoline (6b) has profound anti-tumor cytotoxic effects against Ehrlich ascites carcinoma (EAC) both in vivo and in vitro and against hepatocellular carcinoma (HepG2) cell line in vitro. These anti-tumor effects may be mediated via stimulation of cell cycle arrest and apoptosis through down-regulation of Bcl-2 and up-regulation of p53 transcription factors. (C) 2010 Elsevier Ltd. All rights reserved.
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