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N-hydroxyethyl-4-aza-didehydropodophyllotoxin derivatives as potential antitumor agents.


ABSTRACT: Three different series of N-hydroxyethyl aza-podophyllotoxin derivatives containing (i) a five-membered methylenedioxy ring (7a-f), (ii) a five-membered ring with no heteroatom (8a-f) or (iii) a six membered ethylenedioxy ring (9a-f) as ring A were synthesized using a convenient one-pot multi-component reaction. Further variation on ring E was done by decorating it with methoxy and hydroxy groups at different positions. Calculation of logP values of these compounds indicates them to be better soluble than corresponding non-hydroxy derivatives. These novel aza-podophyllotoxin derivatives were screened for their cytostatic and cytotoxic activities on National Cancer Institute's 60 human tumor cell lines to study the structure activity relationship. The overall anticancer activity of these co

SUBMITTER: Kumar A 

PROVIDER: S-EPMC3278235 | biostudies-literature | 2011 Sep

REPOSITORIES: biostudies-literature