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Design, synthesis and biological evaluation of novel riccardiphenol analogs

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Title Design, synthesis and biological evaluation of novel riccardiphenol analogs
 
Creator KUMAR, SK
AMADOR, M
HIDALGO, M
BHAT, SV
KHAN, SR
 
Subject liverwort bazzania-tridens
absolute-configuration
lithiation reactions
convenient synthesis
new-zealand
key step
alkylation
hydroquinones
3-sulfolenes
terpenoids
anti-tumor
riccardiphenol
sulfolene
diels-alder reaction
 
Description A novel, facile, high yield, and less cumbersome synthesis of riccardiphenol, analogs is described. The synthesized compounds were characterized and assessed for its in vitro activity in a panel of human cancer cell lines of differing origin: HuCCT-1, BxPC3, Panc-1, Mia-Paca, A431, Hep2, and HN006. HuCCT-1 was derived from an intrahepatic cholangiocarcinoma; BxPC3, Mia-Paca, and Panc-1 were derived from pancreatic cancers; A431 was derived from a vulvar epithelial carcinoma; and Hep2 and HN006 were derived from squamous cell carcinomas of the head and neck. The cytotoxicity of a newly developed riccardiphenol analog against human cancer cell lines was assessed. The cancer cells exhibited varying sensitivities to the compound, with IC50 values from 30 to 50 mu M. This susceptibility was particularly interesting in the case of lines such as Hep2 and BxPC3 that are resistant to classic cytotoxic drugs as well as some targeted agents. These results demonstrate that the novel riccardiphenol analog has effective action against human-derived cancer cell in vitro. (c) 2005
 
Publisher PERGAMON-ELSEVIER SCIENCE LTD
 
Date 2011-08-24T00:36:07Z
2011-12-26T12:56:40Z
2011-12-27T05:45:43Z
2011-08-24T00:36:07Z
2011-12-26T12:56:40Z
2011-12-27T05:45:43Z
2005
 
Type Article
 
Identifier BIOORGANIC & MEDICINAL CHEMISTRY, 13(8), 2873-2880
0968-0896
http://dx.doi.org/10.1016/j.bmc.2005.02.010
http://dspace.library.iitb.ac.in/xmlui/handle/10054/10703
http://hdl.handle.net/10054/10703
 
Language en