Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 23, Pages 6582-6584Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.029
Keywords
Enzyme inhibitors; Anti-parasite therapeutics; Chagas disease; Lanosterol 14 alpha-demethylase; Sterol biosynthesis
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Funding
- National Institutes of Health [AI070218]
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We developed a synthetic route to prepare isoquinoline analogs of the cancer drug clinical candidate tipifarnib. We show that these compounds kill Trypanosoma cruzi amastigotes grown in mammalian host cells at concentrations in the low nanomolar range. These isoquinolines represent new leads for the development of drugs to treat Chagas disease. (C) 2009 Elsevier Ltd. All rights reserved.
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