Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines

José C. Aponte, Abraham J. Vaisberg, Denis Castillo, German Gonzalez, Yannick Estevez, Jorge Arevalo, Miguel Quiliano, Mirko Zimic, Manuela Verástegui, Edith Málaga, Robert H. Gilman, Juan M. Bustamante, Rick L. Tarleton, Yuehong Wang, Scott G. Franzblau, Guido F. Pauli, Michel Sauvain, Gerald B. Hammond

Research output: Contribution to journalArticlepeer-review

Abstract

The synthesis of 2-(5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)hydrazone-derivatives (BTPs) and their in vitro evaluation against Trypanosoma cruzi trypomastigotes, Mycobacterium tuberculosis, Leishmania amazonensis axenic amastigotes, and six human cancer cell lines is described. The in vivo activity of the most active and least toxic compounds against T. cruzi and L. amazonensis was also studied. BTPs constitute a new family of drug leads with potential activity against infectious diseases. Due to their drug-like properties, this series of compounds can potentially serve as templates for future drug-optimization and drug-development efforts for use as therapeutic agents in developing countries.

Original languageEnglish (US)
Pages (from-to)2880-2886
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number8
DOIs
StatePublished - Apr 15 2010

Keywords

  • Anticancer
  • Leishmania amazonensis
  • Mycobacterium tuberculosis
  • Tetrahydrobenzothienopyrimidine
  • Trypanosoma cruzi

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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