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Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents.

Abstract:

A potent class of anticancer, human farnesyltransferase (hFTase) inhibitors has been identified by "piggy-backing" on potent, antimalarial inhibitors of Plasmodium falciparum farnesyltransferase (PfFTase). On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating the extensive structure-activity relationship (SAR) study reported herein. Our most potent inhibitor is compound 1f, which exhibited an in vitro hFTase...

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Publication status:
Published

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Publisher copy:
10.1021/jm1001748

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Journal:
Journal of medicinal chemistry
Volume:
53
Issue:
19
Pages:
6867-6888
Publication date:
2010-10-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:6ac1adc0-40d3-4265-8f64-c958fc3941c9
Source identifiers:
117496
Local pid:
pubs:117496

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