✦ LIBER ✦

Synthesis and Antiproliferative Activity of Novel 3-(Indazol-3-yl)-quinazolin-4(3H)-one and 3-(Indazol-3-yl)-benzotriazin-4(3H)-one Derivatives

✍ Scribed by Demetrio Raffa; Giuseppe Daidone; Benedetta Maggio; Domenico Schillaci; Fabiana Plescia

Publisher: John Wiley and Sons
Year: 1999
Tongue: English
Weight: 42 KB
Volume: 332
Category: Article
ISSN: 0365-6233
DOI: 10.1002/(sici)1521-4184(19999)332:9<317::aid-ardp317>3.0.co;2-r

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✦ Synopsis

Several new 3-(indazol-3-yl)-quinazolin-4(3H)-one and 3-(indazol-3-yl)-benzotriazin-4(3H)-one derivatives 5 and 6 were synthesized and tested for their in vitro antiproliferative activity against Raji, K562, and K562-R cell lines. The pharmacological screening showed that some 2, 6, or 7-substituted quinazolinones 5 posses a significant antiproliferative activity, with a percentage growth inhibition ranging from 44.8% to 100% at 50 microM, which was higher than that showed by the unsubstituted derivative 5a previously synthesized. For the most active compounds 5d, 5f, and 5g the IC50 were recorded.

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