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Abstract:

We have investigated the effect of a series of bisphosphonates derived from fatty acids against Trypanosoma cruzi proliferation in in vitro assays. Some of these drugs proved to be potent inhibitors against the intracellular form of the parasite exhibiting IC50 values at the low micromolar level. As bisphosphonates are FDA clinically approved for treatment of bone resorption, their potential innocuousness makes them good candidates to control tropical diseases. © 2001 Elsevier Science Ltd.

Registro:

Documento: Artículo
Título:Bisphosphonates derived from fatty acids are potent growth inhibitors of Trypanosoma cruzi
Autor:Szajnman, S.H.; Bailey, B.N.; Docampo, R.; Rodriguez, J.B.
Filiación:Departamento de Química Orgánica, Fac. de Cie. Exact. y Nat., Univ. de Buenos Aires, Pabellon 2, Cd. Univ., 1428 Buenos Aires, Argentina
Laboratory of Molecular Parasitology, Dept. of Pathobiology, Univ. of Illinois at Urbana-Champaign, 2001 S. Lincoln Ave., Urbana, IL 61802, United States
Palabras clave:bisphosphonic acid derivative; fatty acid derivative; article; Chagas disease; concentration response; drug approval; drug effect; drug potency; drug structure; drug synthesis; food and drug administration; IC 50; nonhuman; osteolysis; parasite development; reaction analysis; structure analysis; tropical disease; Trypanosoma cruzi; Animals; Bone Resorption; Diphosphonates; Fatty Acids; Humans; Inhibitory Concentration 50; Parasitic Sensitivity Tests; Trypanocidal Agents; Trypanosoma cruzi; United States; United States Food and Drug Administration; Trypanosoma; Trypanosoma cruzi
Año:2001
Volumen:11
Número:6
Página de inicio:789
Página de fin:792
DOI: http://dx.doi.org/10.1016/S0960-894X(01)00057-9
Título revista:Bioorganic and Medicinal Chemistry Letters
Título revista abreviado:Bioorg. Med. Chem. Lett.
ISSN:0960894X
CODEN:BMCLE
CAS:Diphosphonates; Fatty Acids; Trypanocidal Agents
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v11_n6_p789_Szajnman

Referencias:

  • Control of Chaga's Disease (1991) WHO Technical Report Series, , Geneva, World Health Organization, No. 811
  • Moncayo, A., (1993) Eleventh Programme Report of the UNPD/World Bank/WHO Special Programme for Research and Training in Tropical Diseases (TDR), pp. 67-75. , World Health Organization, Geneva
  • Burleigh, B.A., Andrews, N.W., (1995) Annu. Rev. Microbiol., 49, p. 175
  • Brener, Z., (1973) Annu. Rev. Microbiol., 27, p. 347
  • De Souza, W., (1984) Int. Rev. Cytol., 86, p. 197
  • Kirchhoff, L.V., (1993) N. Engl. J. Med., 329, p. 639
  • Galel, S.A., Kirchhoff, L.V., (1996) Transfusion, 36, p. 227
  • Shulman, I.A., Appleman, M.D., Saxena, S., Hiti, A.L., Kirchhoff, L.V., (1997) Transfusion, 37, p. 727
  • De Castro, S.L., (1993) Acta Tropica, 53, p. 83
  • Brener, Z., (1979) Pharmacol. Ther., 7, p. 71
  • Rodriguez, J.B., Gros, E.G., (1995) Curr. Med. Chem., 2, p. 723
  • Docampo, R., Moreno, S.N.J., (1985) Rev. Biochem. Toxicol., 7, p. 159
  • Scott, D.A., Docampo, R., Dvorak, J.A., Shi, S., Leapman, R., (1997) J. Biol. Chem., 272, p. 28020
  • Scott, D.A., De Souza, W., Benchimol, M., Zhong, L., Lu, H.-G., Moreno, S.N.J., Docampo, R., (1998) J. Biol. Chem., 273, p. 22151
  • Urbina, J.A., Moreno, B., Vierkotter, S., Oldfield, E., Payares, G., Sanoja, C., Bailey, B.N., Docampo, R., (1999) J. Biol. Chem., 274, p. 33609
  • Rogers, M.J., Watts, D.J., Russell, R.G.G., (1997) Cancer, 80, p. 1652
  • Rodan, G.A., (1998) Annu. Rev. Pharmacol. Toxicol., 38, p. 375
  • Yokoyama, K., Trobridge, P., Buckner, F.S., Scholten, J., Stuart, K.D., Van Voorhis, W.C., Gelb, M.H., (1998) Mol. Biochem. Parasitol., 94, p. 87
  • Glomset, J.A., Farnswort, C.C., (1994) Annu. Rev. Cell. Biol., 10, p. 181
  • Casey, P.J., Seabra, M., (1996) J. Biol. Chem., 271, p. 5289
  • Leonard, D.M., (1997) J. Med. Chem., 40, p. 2971
  • Van Beek, E., Pieterman, E., Cohen, L., Lowik, C., Papapoulos, S., (1999) Biochem. Biophys. Res. Commun., 264, p. 108
  • Keller, R.K., Fliesler, S.J., (1999) Biochem. Biophys. Res. Commun., 266, p. 560
  • Bergstrom, J.D., Bostedor, R.G., Masarachia, P.J., Reszka, A.A., Rodan, G., (2000) Arch. Biochem. Biophys., 373, p. 231
  • Cromartie, T.H., Fisher, K.J., Grossman, J.N., (1999) Pest Biochem. Physiol., 63, p. 114
  • Grove, J.E., Brown, R.J., Watts, D.J., (2000) J. Bone Miner. Res., 15, p. 971
  • Fisher, J.E., Rogers, M.J., Halasy, J.M., Luckman, S.P., Hughes, D.E., Masarachia, P.J., Wesolowski, G., Reszka, A.A., (1999) Proc. Natl. Acad. Sci. U.S.A., 96, p. 133
  • Martin, M.B., Arnold, W., Heath III, H.T., Urbina, J.A., Oldfield, E., (1999) Biochem. Biophys. Res. Commun., 263, p. 754
  • Szajnman, S.H., Yan, W., Bailey, B.N., Docampo, R., Elhalem, E., Rodriguez, J.B., (2000) J. Med. Chem., 43, p. 1826
  • Cinque, G.M., Szajnman, S.H., Zhong, L., Docampo, R., Rodriguez, J.B., Gros, E.G., (1998) J. Med. Chem., 41, p. 1540
  • Kieczykowski, G.R., Jobson, R.B., Melillo, D.G., Reinhold, D.F., Grenda, V.J., Shinkai, I., (1995) J. Org. Chem., 60, p. 8310
  • Note; Note; Schvartzapel, A.J., Zhong, L., Docampo, R., Rodriguez, J.B., Gros, E.G., (1997) J. Med. Chem., 40, p. 2314
  • Yan, W., Moreno, S.N.J., (1998) J. Immunol. Methods, 220, p. 123
  • Soares, M.J., De Souza, W., (1991) Parasitol. Res., 77, p. 461
  • Rogers, M.J., Xiong, X., Ji, X., Mönkkönen, J., Russell, G.G., Williamson, M.P., Ebetino, F.H., Watts, D.J., (1997) Pharm. Res., 14, p. 625

Citas:

---------- APA ----------
Szajnman, S.H., Bailey, B.N., Docampo, R. & Rodriguez, J.B. (2001) . Bisphosphonates derived from fatty acids are potent growth inhibitors of Trypanosoma cruzi. Bioorganic and Medicinal Chemistry Letters, 11(6), 789-792.
http://dx.doi.org/10.1016/S0960-894X(01)00057-9
---------- CHICAGO ----------
Szajnman, S.H., Bailey, B.N., Docampo, R., Rodriguez, J.B. "Bisphosphonates derived from fatty acids are potent growth inhibitors of Trypanosoma cruzi" . Bioorganic and Medicinal Chemistry Letters 11, no. 6 (2001) : 789-792.
http://dx.doi.org/10.1016/S0960-894X(01)00057-9
---------- MLA ----------
Szajnman, S.H., Bailey, B.N., Docampo, R., Rodriguez, J.B. "Bisphosphonates derived from fatty acids are potent growth inhibitors of Trypanosoma cruzi" . Bioorganic and Medicinal Chemistry Letters, vol. 11, no. 6, 2001, pp. 789-792.
http://dx.doi.org/10.1016/S0960-894X(01)00057-9
---------- VANCOUVER ----------
Szajnman, S.H., Bailey, B.N., Docampo, R., Rodriguez, J.B. Bisphosphonates derived from fatty acids are potent growth inhibitors of Trypanosoma cruzi. Bioorg. Med. Chem. Lett. 2001;11(6):789-792.
http://dx.doi.org/10.1016/S0960-894X(01)00057-9