@article{274e455d3a044fd0a8cf22d92025d11c,
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.",
keywords = "Anticancer, Leishmania amazonensis, Mycobacterium tuberculosis, Tetrahydrobenzothienopyrimidine, Trypanosoma cruzi",
author = "Aponte, {Jos{\'e} C.} and Vaisberg, {Abraham J.} and Denis Castillo and German Gonzalez and Yannick Estevez and Jorge Arevalo and Miguel Quiliano and Mirko Zimic and Manuela Ver{\'a}stegui and Edith M{\'a}laga and Gilman, {Robert H.} and Bustamante, {Juan M.} and Tarleton, {Rick L.} and Yuehong Wang and Franzblau, {Scott G.} and Pauli, {Guido F.} and Michel Sauvain and Hammond, {Gerald B.}",
note = "Funding Information: G.B.H. and J.C.A. wish to acknowledge the early contribution of Mr. Devin Pantess (University of Louisville) and Dr. Rosario Rojas (Universidad Peruana Cayetano Heredia) in the synthesis of BTPs and their anti-tuberculosis screening. The authors are grateful to the USA Department of Defense Prostate Cancer Research Program (PCRP) of the Office of the Congressionally Directed Medical Research Programs (CDMRP) (Grant #W81XWH-07-1-0299 to G.B.H.), to the FINCYT-BID (Banco Interamericano para el Desarrollo) Program in Peru (grant #PIBAB03-084 to M.S.), to the Infectious Diseases Training Program in Peru # 5D43 TW006581 (R.H. G) and to the NIH grant P01-044979 (to R.L.T.) for their financial support. J.M.B and R.L.T. thank Adriana M. C. Canavaci at the CTEGD-University of Georgia for her technical assistance with the in vitro testing of drugs for T. cruzi . The skillful technical assistance of Mrs. Baojie Wan and Yuehong Wang, ITR, UIC College of Pharmacy, Chicago (IL), is gratefully acknowledged. ",
year = "2010",
month = apr,
day = "15",
doi = "10.1016/j.bmc.2010.03.018",
language = "English (US)",
volume = "18",
pages = "2880--2886",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Limited",
number = "8",
}