Synthesis and antitumour activity of a series of cyclic amidines of 2,3-dihydro-1H-1,5-benzodiazepines.
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.
Sector of Application of Biologically Active Compounds, Institute of Biochemistry, Vilnius, Lithuania.
Regina
R
Janciene
Lidija
L
Kosychova
Virginija
V
Bukelskiene
Vigintas
V
Domkus
Zita
Z
Stumbreviciūte
Vida
V
Ragaleviciene
Benedikta D
BD
Puodziūnaite
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013058:Mass Spectrometry; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D001569:Benzodiazepines