Synthesis and antiproliferative activity of novel 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)-benzotriazin-4(3H)-one derivatives

Citation
D. Raffa et al., Synthesis and antiproliferative activity of novel 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)-benzotriazin-4(3H)-one derivatives, ARCH PHARM, 332(9), 1999, pp. 317-320
Citations number
12
Categorie Soggetti
Pharmacology & Toxicology
Journal title
ARCHIV DER PHARMAZIE
ISSN journal
03656233 → ACNP
Volume
332
Issue
9
Year of publication
1999
Pages
317 - 320
Database
ISI
SICI code
0365-6233(199909)332:9<317:SAAAON>2.0.ZU;2-T
Abstract
Several new 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)-benz otriazin-4(3H)-one derivatives 5 and 6 were synthesized and tested for thei r in vitro, antiproliferative activity against Raji, K562, and K562-R cell lines. The pharmacological screening showed that some 2, 6, or 7-substitute d quinazolinones 5 posses a significant antiproliferative activity, with a percentage growth inhibition ranging from 44.8% to 100% at 50 mu M, which w as higher than that showed by the unsubstituted derivative 5a previously sy nthesized. For the most active compounds 5d, 5f, and 5g the IC50 were recor ded.