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

doi:10.1016/j.bmc.2010.03.018

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

University of Louisville
Facultad de Ciencias y Filosofía
Universidad Peruana Cayetano Heredia, Instituto de Medicina Tropical Alexander von Humboldt
Université Paul Sabatier Toulouse III
Bioinformatics Unit-Drug Design Group
Johns Hopkins University School of Public Health
University of Georgia
University of Illinois at Chicago

Research output: Contribution to journal › Article › peer-review

46 Scopus citations

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 language	English
Pages (from-to)	2880-2886
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	8
DOIs	https://doi.org/10.1016/j.bmc.2010.03.018
State	Published - 15 Apr 2010
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Anticancer
Leishmania amazonensis
Mycobacterium tuberculosis
Tetrahydrobenzothienopyrimidine
Trypanosoma cruzi

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10.1016/j.bmc.2010.03.018

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Aponte, J. C., Vaisberg, A. J., Castillo, D., Gonzalez, G., Estevez, Y., Arevalo, J., Quiliano, M., Zimic, M., Verástegui, M., Málaga, E., Gilman, R. H., Bustamante, J. M., Tarleton, R. L., Wang, Y., Franzblau, S. G., Pauli, G. F., Sauvain, M., & Hammond, G. B. (2010). Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines. Bioorganic and Medicinal Chemistry, 18(8), 2880-2886. https://doi.org/10.1016/j.bmc.2010.03.018

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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.",

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Aponte, JC, Vaisberg, AJ, Castillo, D, Gonzalez, G, Estevez, Y, Arevalo, J, Quiliano, M, Zimic, M, Verástegui, M, Málaga, E, Gilman, RH, Bustamante, JM, Tarleton, RL, Wang, Y, Franzblau, SG, Pauli, GF, Sauvain, M & Hammond, GB 2010, 'Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines', Bioorganic and Medicinal Chemistry, vol. 18, no. 8, pp. 2880-2886. https://doi.org/10.1016/j.bmc.2010.03.018

TY - JOUR

T1 - Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines

AU - Aponte, José C.

AU - Vaisberg, Abraham J.

AU - Castillo, Denis

AU - Gonzalez, German

AU - Estevez, Yannick

AU - Arevalo, Jorge

AU - Quiliano, Miguel

AU - Zimic, Mirko

AU - Verástegui, Manuela

AU - Málaga, Edith

AU - Gilman, Robert H.

AU - Bustamante, Juan M.

AU - Tarleton, Rick L.

AU - Wang, Yuehong

AU - Franzblau, Scott G.

AU - Pauli, Guido F.

AU - Sauvain, Michel

AU - Hammond, Gerald B.

PY - 2010/4/15

Y1 - 2010/4/15

N2 - 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.

AB - 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.

KW - Anticancer

KW - Leishmania amazonensis

KW - Mycobacterium tuberculosis

KW - Tetrahydrobenzothienopyrimidine

KW - Trypanosoma cruzi

UR - https://www.scopus.com/pages/publications/77950520679

U2 - 10.1016/j.bmc.2010.03.018

DO - 10.1016/j.bmc.2010.03.018

M3 - Artículo

C2 - 20356752

AN - SCOPUS:77950520679

SN - 0968-0896

VL - 18

SP - 2880

EP - 2886

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 8

ER -

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

Abstract

UN SDGs

Keywords

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