Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity.

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Krauth F, Dahse HM, Ruttinger HH, Frohberg P

Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity.

Bioorg Med Chem. 2010 Mar 1;18(5):1816-21. doi: 10.1016/j.bmc.2010.01.053. Epub 2010 Jan 25.

PubMed ID

20153202 [ View in PubMed

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Abstract

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 logP(calc) values were experimentally confirmed (logP(exp)). For the most active compounds, in vitro serum albumin binding was investigated and structure-activity relationships were established.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Imatinib	Serum albumin	Kd (nM)	78640	N/A	N/A	Details