Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 5, Pages 1816-1821Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.01.053
Keywords
1,2,4-triazin-5-ones; Small molecules; Leukemia; K-562; Rule-of-five; log P; Imatinib; Serum albumin binding
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A series of novel small molecules with a 1,2,4-triazine scaffold was obtained according to a recently published and highly efficient synthetic route. Screening for antiproliferative and cytotoxic activity revealed distinct anticancer effects against the human leukemia cell line K-562 combined with a remarkable low cytotoxicity. All compounds were in agreement with the 'rule-of-five' claims by Lipinski and calculated log P(calc) values were experimentally confirmed (log P(exp)). For the most active compounds, in vitro serum albumin binding was investigated and structure-activity relationships were established. (C) 2010 Elsevier Ltd. All rights reserved.
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