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


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.

SUBMITTER: Chennamaneni NK 

PROVIDER: S-EPMC2783978 | biostudies-literature | 2009 Dec

REPOSITORIES: biostudies-literature

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

Chennamaneni Naveen Kumar NK   Arif Jenifer J   Buckner Frederick S FS   Gelb Michael H MH  

Bioorganic & medicinal chemistry letters 20091013 23


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. ...[more]

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