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Synthesis and Antiproliferative Activity of Novel 3‐(Indazol‐3‐yl)‐quinazolin‐4(3 H )‐one and 3‐(Indazol‐3‐yl)‐benzotriazin‐4(3 H )‐one Derivatives
Author(s) -
Raffa Demetrio,
Daidone Giuseppe,
Maggio Benedetta,
Schillaci Domenico,
Plescia Fabiana
Publication year - 1999
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/(sici)1521-4184(19999)332:9<317::aid-ardp317>3.0.co;2-r
Subject(s) - chemistry , indazole , k562 cells , in vitro , stereochemistry , cell culture , ic50 , growth inhibition , derivative (finance) , biochemistry , biology , economics , financial economics , genetics
Several new 3‐(indazol‐3‐yl)‐quinazolin‐4(3 H )‐one and 3‐(indazol‐3‐yl)‐benzotriazin‐4(3 H )‐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 μM, which was higher than that showed by the unsubstituted derivative 5a previously synthesized. For the most active compounds 5d, 5f, and 5g the IC 50 were recorded.