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

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Resumen

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.

Idioma original	Inglés
Páginas (desde-hasta)	2880-2886
Número de páginas	7
Publicación	Bioorganic and Medicinal Chemistry
Volumen	18
N.º	8
DOI	https://doi.org/10.1016/j.bmc.2010.03.018
Estado	Publicada - 15 abr. 2010
Publicado de forma externa	Sí

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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.",

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.\}",

year = "2010",

month = apr,

day = "15",

doi = "10.1016/j.bmc.2010.03.018",

language = "Ingl{\'e}s",

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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, n.º 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

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