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
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.