{"id":76324,"date":"2018-03-09T23:21:43","date_gmt":"2018-03-09T23:21:43","guid":{"rendered":"https:\/\/www.deberes.net\/tesis\/sin-categoria\/diseno-de-derivados-de-11-dioxido-de-benzo-b-tiofeno-sintesis-y-evaluacion-como-potenciales-farmacos\/"},"modified":"2018-03-09T23:21:43","modified_gmt":"2018-03-09T23:21:43","slug":"diseno-de-derivados-de-11-dioxido-de-benzo-b-tiofeno-sintesis-y-evaluacion-como-potenciales-farmacos","status":"publish","type":"post","link":"https:\/\/www.deberes.net\/tesis\/quimica\/diseno-de-derivados-de-11-dioxido-de-benzo-b-tiofeno-sintesis-y-evaluacion-como-potenciales-farmacos\/","title":{"rendered":"Dise\u00f1o de derivados de 1,1 dioxido de benzo (b) tiofeno, sintesis y evaluacion como potenciales farmacos"},"content":{"rendered":"<h2>Tesis doctoral de <strong> Raquel Villar Becares <\/strong><\/h2>\n<p>Se ha desarrollado un trabajo multidisciplinar  que ha llevado a la obtencion de derivados de 1,1- di\u00f3xido de benzo[b]tiofeno, activos en el campo famac\u00e9utico , mediante un dise\u00f1o racional utilizando diferentes m\u00e9todos te\u00f3ricos. Para esto se ha llevado a cabo la s\u00edntesis de 21 nuevas derivados de 1,1- di\u00f3xido de benzo[b]tiofenosulfonamida en las posiciones 5 y\/o 6 del anillo, 4 nuevas carboxamidas relacionadas, un sulfonato derivado y un derivado hidroxilado.  la determinaci\u00f3n de la citotoxicidad se ha llevado a cabo sobre 24 de los nuevos derivados de 1,1- di\u00f3xido de benzo[b]tiofeno utilizando un microensayo colorim\u00e9trico de la reducci\u00f3n de bromuro de 3- (4,5-dimetil-2-tiazolil)2, 5-difeniltetrazoilo (mtt) sobre una l\u00ednea de fibroblastos humanos de pulm\u00f3n y 6 l\u00edneas celulares de tumores humanos, representativas de tumores s\u00f3lidos, (htb-54; ht-29; mel-ac, hela) y leucemias (ccrf-cem; k-562). 23 de los 24 compuestos ensayados se han mostrado muy activos frente a una o varias de las l\u00edneas ensayas con valores de gi50 del rango m. Las l\u00edneas hela, ccrg-cem, htb-54 y hlfphtert han resultado las m\u00e1s sensibles. Los derivados sulfonamida y carboxamida son m\u00e1s activos que los correspondientes sulfonato o hidroxilo. La citotoxicidad no se ve afectada por la posici\u00f3n de la sulfonamida en el anillo pero se ve aumentada por la sustituci\u00f3n hidrof\u00f3bica de la sulfonamida y carboxamida. los compuestos m\u00e1s activos son los n-(4metoxi) fenil y n-(2-(4-metoxi)fenil)etil derivados de carboxamida y sulfonamida cuya citotoxicidad es comparable al compuesto comercial doxorrubicina. El n-(2-feniletil)-6-sulfonamida derivado inhibe la actividad nadh oxidasa asociada a tumor en condiciones reductoras con una ec50 de 0.1 nm.  los ensayos de inhibici\u00f3n de anhidrasas carb\u00f3nicas, han mostrado que los derivados de sulfonamida no sustituidos presentan una actividad excelente, mientras que la n-sustituci\u00f3n disminuye  la actividad. Los 3-butiloxi<\/p>\n<p>&nbsp;<\/p>\n<h3>Datos acad\u00e9micos de la tesis doctoral \u00ab<strong>Dise\u00f1o de derivados de 1,1 dioxido de benzo (b) tiofeno, sintesis y evaluacion como potenciales farmacos<\/strong>\u00ab<\/h3>\n<ul>\n<li><strong>T\u00edtulo de la tesis:<\/strong>\u00a0 Dise\u00f1o de derivados de 1,1 dioxido de benzo (b) tiofeno, sintesis y evaluacion como potenciales farmacos <\/li>\n<li><strong>Autor:<\/strong>\u00a0 Raquel Villar Becares <\/li>\n<li><strong>Universidad:<\/strong>\u00a0 P\u00fablica de navarra<\/li>\n<li><strong>Fecha de lectura de la tesis:<\/strong>\u00a0 23\/09\/2005<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n<h3>Direcci\u00f3n y tribunal<\/h3>\n<ul>\n<li><strong>Director de la tesis<\/strong>\n<ul>\n<li>V\u00edctor Mart\u00ednez Merino<\/li>\n<\/ul>\n<\/li>\n<li><strong>Tribunal<\/strong>\n<ul>\n<li>Presidente del tribunal: vicente Gotor santamar\u00eda <\/li>\n<li>ferran Sanz careras (vocal)<\/li>\n<li>Antonio Monge vega (vocal)<\/li>\n<li> Garcia laureiro Jos\u00e9 ignacio (vocal)<\/li>\n<\/ul>\n<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Tesis doctoral de Raquel Villar Becares Se ha desarrollado un trabajo multidisciplinar que ha llevado a la obtencion de derivados [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"","site-content-style":"default","site-sidebar-style":"default","ast-global-header-display":"","ast-banner-title-visibility":"","ast-main-header-display":"","ast-hfb-above-header-display":"","ast-hfb-below-header-display":"","ast-hfb-mobile-header-display":"","site-post-title":"","ast-breadcrumbs-content":"","ast-featured-img":"","footer-sml-layout":"","theme-transparent-header-meta":"","adv-header-id-meta":"","stick-header-meta":"","header-above-stick-meta":"","header-main-stick-meta":"","header-below-stick-meta":"","astra-migrate-meta-layouts":"default","ast-page-background-enabled":"default","ast-page-background-meta":{"desktop":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center 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