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2,3-Disubstituted-1,4-naphthoquinones, 12H-benzo[b]phenothiazine-6, 11-diones and related compounds: Synthesis and Biological evaluation as potential antiproliferative and antifungal agents

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Title 2,3-Disubstituted-1,4-naphthoquinones, 12H-benzo[b]phenothiazine-6, 11-diones and related compounds: Synthesis and Biological evaluation as potential antiproliferative and antifungal agents
 
Creator TANDON, VK
MAURYA, HK
TRIPATHI, A
SHIVAKESHAVA, GB
SHUKLA, PK
SRIVASTAVA, P
PANDA, D
 
Subject 1,4-naphthoquinone derivatives
naphthoquinone derivatives
antiallergic activities
antibacterial agents
cell-proliferation
anticancer agents
cytotoxicity
antiplatelet
inhibitors
mitosis
antiproliferative
1,4-naphthoquinone derivatives
cytotoxic
human cervical cancer (hela) cells
antifungal
 
Description A series of 2-chloro-3-arylsulfanyl-[1,4]naphthoquinones (2), 2,3-bis-arylsulfanyl-[1,4]naphthoquinones (3) and 12H-benzo[b]phenothiazine-6,11-diones and their analogs 6-8 were synthesized and evaluated for their antiproliferative activity against human cervical cancer (HeLa) cells. Compounds 3a and 3b were found to possess most potent antiproliferative and cell killing ability. Compounds 1-8 were also evaluated for antifungal activities. The structure-activity relationship of these compounds was studied and the results show that compound 2a (MIC(50) = 1.56 mu g/mL) exhibited in vitro potent antifungal activity compared to the clinically useful antifungal. drug Fluconazole (MIC(50) = 2.0 mu g/mL) against Sporothrix. schenckii. Compound 2a (MIC(50) = 1.56 mu g/mL) also exhibited same antifungal activity compared to clinically useful drug Amphotericin-B (MIC(50) = 1.56 mu g/mL) against Trichophyton. mentagraphytes. (C) 2008 Elsevier Masson SAS. .
 
Publisher ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
 
Date 2011-07-21T16:11:00Z
2011-12-26T12:52:04Z
2011-12-27T05:39:03Z
2011-07-21T16:11:00Z
2011-12-26T12:52:04Z
2011-12-27T05:39:03Z
2009
 
Type Article
 
Identifier EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 44(3), 1086-1092
0223-5234
http://dx.doi.org/10.1016/j.ejmech.2008.06.025
http://dspace.library.iitb.ac.in/xmlui/handle/10054/5918
http://hdl.handle.net/10054/5918
 
Language en