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Home ยป Isoquinoline-based analogs of the cancer drug clinical candidate tipifarnib as anti-Trypanosoma cruzi agents.

Isoquinoline-based analogs of the cancer drug clinical candidate tipifarnib as anti-Trypanosoma cruzi agents.

TitleIsoquinoline-based analogs of the cancer drug clinical candidate tipifarnib as anti-Trypanosoma cruzi agents.
Publication TypeJournal Article
Year of Publication2009
AuthorsChennamaneni, NKumar, Arif, J, Buckner, FS, Gelb, MH
JournalBioorg Med Chem Lett
Volume19
Issue23
Pagination6582-4
Date Published2009 Dec 1
ISSN1464-3405
KeywordsAnimals, Antineoplastic Agents, Chagas Disease, Drug Evaluation, Preclinical, Mice, Molecular Conformation, Parasitic Sensitivity Tests, Quinolones, Stereoisomerism, Structure-Activity Relationship, Trypanocidal Agents, Trypanosoma cruzi
Abstract

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.
DOI10.1016/j.bmcl.2009.10.029
Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID19875282