- 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...
Expand abstract - Publication status:
- Published
- 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
- Language:
- English
- Keywords:
- Copyright date:
- 2010
Journal article
Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents.
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