title: Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines.
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.
authors.affiliation: Department of Chemistry, University of Louisville, Louisville, KY 40292, USA.
authors.forename: José C
authors.initials: JC
authors.lastname: Aponte
authors.forename: Abraham J
authors.initials: AJ
authors.lastname: Vaisberg
authors.forename: Denis
authors.initials: D
authors.lastname: Castillo
authors.forename: German
authors.initials: G
authors.lastname: Gonzalez
authors.forename: Yannick
authors.initials: Y
authors.lastname: Estevez
authors.forename: Jorge
authors.initials: J
authors.lastname: Arevalo
authors.forename: Miguel
authors.initials: M
authors.lastname: Quiliano
authors.forename: Mirko
authors.initials: M
authors.lastname: Zimic
authors.forename: Manuela
authors.initials: M
authors.lastname: Verástegui
authors.forename: Edith
authors.initials: E
authors.lastname: Málaga
authors.forename: Robert H
authors.initials: RH
authors.lastname: Gilman
authors.forename: Juan M
authors.initials: JM
authors.lastname: Bustamante
authors.forename: Rick L
authors.initials: RL
authors.lastname: Tarleton
authors.forename: Yuehong
authors.initials: Y
authors.lastname: Wang
authors.forename: Scott G
authors.initials: SG
authors.lastname: Franzblau
authors.forename: Guido F
authors.initials: GF
authors.lastname: Pauli
authors.forename: Michel
authors.initials: M
authors.lastname: Sauvain
authors.forename: Gerald B
authors.initials: GB
authors.lastname: Hammond
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D045744:Cell Line, Tumor; D006801:Humans; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D021261:Parasitic Sensitivity Tests; D011743:Pyrimidines / Q000737:chemistry* / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000981:Antiprotozoal Agents; D000995:Antitubercular Agents; D011743:Pyrimidines