{"id":92747,"date":"2009-03-04T00:00:00","date_gmt":"2009-03-04T00:00:00","guid":{"rendered":"https:\/\/www.deberes.net\/tesis\/sin-categoria\/sa%c2%adntesis-de-nuevos-retxinoides-e-inhibidores-e-inhibidores-de-histona-desaceliasa-basados-en-psammaplina-a\/"},"modified":"2009-03-04T00:00:00","modified_gmt":"2009-03-04T00:00:00","slug":"sa%c2%adntesis-de-nuevos-retxinoides-e-inhibidores-e-inhibidores-de-histona-desaceliasa-basados-en-psammaplina-a","status":"publish","type":"post","link":"https:\/\/www.deberes.net\/tesis\/compuestos-heterociclicos\/sa%c2%adntesis-de-nuevos-retxinoides-e-inhibidores-e-inhibidores-de-histona-desaceliasa-basados-en-psammaplina-a\/","title":{"rendered":"S\u00edntesis de nuevos ret(x)inoides e inhibidores e inhibidores de histona desaceliasa basados en psammaplina a"},"content":{"rendered":"<h2>Tesis doctoral de <strong> Jos\u00e9 Garc\u00eda Rodr\u00edguez <\/strong><\/h2>\n<p>Las alteraciones epigen\u00e9ticas del adn y de la cromatina est\u00e1n estrechamente relacionadas con la oncog\u00e9nesis y la progresi\u00f3n de tumores. Los receptores nucleares, a su vez, influyen en procesos involucrados en el crecimiento y la diferenciaci\u00f3n celulares, y la p\u00e9rdida de su funci\u00f3n est\u00e1 relacionada con la carcionog\u00e9nesis. Por esta raz\u00f3n, los f\u00e1rmacos moduladores de la cromatina y de los receptores nucleares son objetivos novedosos en la lucha contra el c\u00e1ncer. De entre estos moduladores, los inhibidores de las histona desacetilasas (hdacs) se presentan como uno de los grupos de agentes anticancer\u00edgenos m\u00e1s prometedores. La vitamina a y sus an\u00e1logos, ligandos del receptor del \u00e1cido retinoico rar, han mostrado actividad antitumoral y quimiopreventiva. En este trabajo se expone el dise\u00f1o y la s\u00edntesis de nuevas familias de retinoides y rexinoides cuya caracter\u00edstica com\u00fan es la presencia de estructuras heteroc\u00edclicas en el esqueleto. Se abordar\u00e1 la s\u00edntesis de nuevos retinoides que contienen un anillo de pirazina se llevar\u00e1 a cabo mediante reacciones de formaci\u00f3n de enlaces c-c catalizadas por pd. El n\u00facleo de pirazina tambi\u00e9n se incorporar\u00e1 a esqueletos de arotinoides adamant\u00edlicos para evaluar la capacidad inductora de apoptosis de esos retinoides at\u00edpicos. Los retinoides que incorporan un benzofurano presentan una mayor restricci\u00f3n de la libertad conformacional y una forma plegada que podr\u00eda adaptarse al bolsillo de rxr. Adem\u00e1s, se desarrolla la contribuci\u00f3n a la optimizaci\u00f3n de moduladores epigen\u00e9ticos inspirados en la estructura del producto natural psammaplina a. Se ha empleado una metodolog\u00eda sint\u00e9tica que pemite incorporar, de forma secuencial, diferentes sustituyentes a un n\u00facleo de pirazina usando reacciones de acoplamiento catalizadas por pd. Aplicando esta metodolog\u00eda, se ha sintetizado una familia de ligandos de rar con actividades que var\u00edan de antagonistas a agonistas inversos. Se ha desarrollado una s\u00edntesis eficaz para los rexinoides derivados de dibenzofurano que mostraron un incremento de la capacidad antagonista rxr al aumentar el tama\u00f1o del sustituyente del grupo \u00e9ter, aunque s\u00f3lo a concentraciones elevadas. Se ha dise\u00f1ado un ruta sint\u00e9tica vers\u00e1til que permite obtener psammaplina a y otros an\u00e1logos utilizando cmo materiales de partida derivados comerciales de tirosina. Se ha sintetizado una serie de an\u00e1logos de psammaplina a basados en un anillo de indol empleando una estrategia sint\u00e9tica vers\u00e1til y corta.<\/p>\n<p>&nbsp;<\/p>\n<h3>Datos acad\u00e9micos de la tesis doctoral \u00ab<strong>S\u00edntesis de nuevos ret(x)inoides e inhibidores e inhibidores de histona desaceliasa basados en psammaplina a<\/strong>\u00ab<\/h3>\n<ul>\n<li><strong>T\u00edtulo de la tesis:<\/strong>\u00a0 S\u00edntesis de nuevos ret(x)inoides e inhibidores e inhibidores de histona desaceliasa basados en psammaplina a <\/li>\n<li><strong>Autor:<\/strong>\u00a0 Jos\u00e9 Garc\u00eda Rodr\u00edguez <\/li>\n<li><strong>Universidad:<\/strong>\u00a0 Vigo<\/li>\n<li><strong>Fecha de lectura de la tesis:<\/strong>\u00a0 03\/04\/2009<\/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>Raquel Pereira Camaselle<\/li>\n<\/ul>\n<\/li>\n<li><strong>Tribunal<\/strong>\n<ul>\n<li>Presidente del tribunal: emilio Qui\u00f1oa cabana <\/li>\n<li>pilar Sanchez andrada (vocal)<\/li>\n<li>Jos\u00e9 Carlos Menendez ramos (vocal)<\/li>\n<li>Carlos Jim\u00e9nez gonz\u00e1lez (vocal)<\/li>\n<\/ul>\n<\/li>\n<\/ul>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Tesis doctoral de Jos\u00e9 Garc\u00eda Rodr\u00edguez Las alteraciones epigen\u00e9ticas del adn y de la cromatina est\u00e1n estrechamente relacionadas con la [&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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