Abstract:
:A series of novel benzo[4,5]canthin-6-ones, bearing the N'-(substituted benzylidene)-carbohydrazide (11a-e) and N-alkylcarboxamide (13a-g) moieties at position-2, were synthesized and screened for their in vitro antitumor activity, against seven human cancer cell lines, and for antitrypanosomal and antileishmanial activities against Trypanosoma cruzi and Leishmania amazonensis. The results indicated that N-methylpiperazyl-6-oxobenzo[4,5]canthine-2-carboxamide (13f) displayed potent antitumor activity with IC(50) values in the range of 1.15-8.46 µM for all cell lines tested. Compounds 13f and 13g bearing an N-methylpiperazylcarboxamide and N-morpholylcarboxamide at C-2, respectively, showed potent activities towards both Trypanosoma cruzi and Leishmania amazonensis parasites, with IC(50) in the range of 0.4 to 16.70 µM.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Leite Silva CM,Garcia FP,Rodrigues JH,Nakamura CV,Ueda-Nakamura T,Meyer E,Ruiz AL,Foglio MA,de Carvalho JE,da Costa WF,Sarragiotto MHdoi
10.1248/cpb.c12-00356subject
Has Abstractpub_date
2012-01-01 00:00:00pages
1372-9issue
11eissn
0009-2363issn
1347-5223pii
DN/JST.JSTAGE/cpb/c12-00356journal_volume
60pub_type
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