Synthesis and Antitumour Activity of a Series of Cyclic Amidines of 2,3-Dihydro-1H-1,5-benzodiazepines

Autor:	Domkus, Stumbreviciūte Z, Ragaleviciene, Bukelskiene, Janciene R, Kosychova L, Puodziūnaite Bd
Rok vydání:	2011
Předmět:	Screening test Established cell line Cell culture Chemistry Cell growth Drug Discovery Lipophilicity Nucleophilic substitution Medicinal chemistry Chemical synthesis In vitro
Zdroj:	Arzneimittelforschung. 52:475-481
ISSN:	1616-7066 0004-4172
DOI:	10.1055/s-0031-1299917
Popis:	2,3-Dihydro-1H-1,5-benzodiazepine amidines were prepared by nucleophilic substitution of 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-2-thiones. Evaluation of the 13 synthesised amidines as antitumour agents was carried out in vitro against 60 human tumour cell lines at the National Cancer Institute, Bethesda, USA. The screening revealed a moderate cell growth inhibition of two derivatives on all cell lines at concentrations ranging from 10(-5) to 10(-4) mol/l. Log P values were theoretically calculated. The more active derivatives were found to exhibit a higher lipophilicity.
Databáze:	OpenAIRE
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