Design and synthesis of a novel water soluble benzotetrazepinone

Authors
Dumont-Hornebeck, B Strube, YN Vasilescu, D Jean-Claude, BJ
Citation
B. Dumont-hornebeck et al., Design and synthesis of a novel water soluble benzotetrazepinone, BIOORG MED, 10(20), 2000, pp. 2325-2327
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
20
Year of publication
2000
Pages
2325 - 2327
Database
ISI
SICI code
0960-894X(20001016)10:20<2325:DASOAN>2.0.ZU;2-G
Abstract
In order to confer water solubility to the benzotetrazepinone ring system, the synthesis of 12 was undertaken. The design and synthesis of 12 were bas ed upon previously established structural requirements for the stability of the 1,2,3,5-tetrazepin-4-one ring system. Tetrazepinone 12 was extremely w ater soluble and was 10-fold more potent than its imidazo-1,2,3,5-tetrazin- 4-one counterpart la, against the human MCF-7 breast cancer cell line. (C) 2000 Elsevier Science Ltd. All rights reserved.