Synthesis of 5-substituted quinazolinone derivatives and their inhibitory activity in vitro

Authors
Baek, DJ Park, YK Heo, HI Lee, MH Yang, ZY Choi, MH
Citation
Dj. Baek et al., Synthesis of 5-substituted quinazolinone derivatives and their inhibitory activity in vitro, BIOORG MED, 8(23), 1998, pp. 3287-3290
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
23
Year of publication
1998
Pages
3287 - 3290
Database
ISI
SICI code
0960-894X(199812)8:23<3287:SO5QDA>2.0.ZU;2-5
Abstract
Quinazolinone derivatives I and their methyl esters were synthesized and ev aluated as nonclassical lipophilic inhibitors of thymidylate synthase. Comp ounds Ib and Ic containing OH and CO2H as R substituents, respectively, wer e most effective, indicating that hydrogen bonding may contribute to the in creased inhibitory activity. These compounds further showed high cytotoxic activity against tumor cells in culture. (C) 1998 Elsevier Science Ltd. All rights reserved.