{"id":4402,"date":"2023-12-08T14:15:54","date_gmt":"2023-12-08T14:15:54","guid":{"rendered":"https:\/\/en.copharm.uobaghdad.edu.iq\/?p=4402"},"modified":"2023-12-09T14:18:10","modified_gmt":"2023-12-09T14:18:10","slug":"discussion-the-design-synthesis-and-biological-evaluation-of-novel-n-hydroxyurea-derivatives-as-possible-dual-hdac-bet-inhibitors","status":"publish","type":"post","link":"https:\/\/en.copharm.uobaghdad.edu.iq\/?p=4402","title":{"rendered":"Discussion the Design, Synthesis, and Biological Evaluation of Novel N-Hydroxyurea Derivatives as Possible Dual HDAC\/BET Inhibitors"},"content":{"rendered":"<div class=\"wpb-content-wrapper\"><p>[vc_row][vc_column][vc_column_text]<\/p>\n<p style=\"text-align: justify;\"><span style=\"font-size: 19px;\">The Faculty of Pharmacy discussed the MSc thesis entitled \u201cDesign, Synthesis, and Biological Evaluation of Novel N-Hydroxyurea Derivatives as Possible Dual HDAC\/BET Inhibitors\u201d by Hayjaa Mohesen Mousa and her supervisor, Assistant Professor Dr. Ayad Abed Ali Al-Hamashi in the Pharmaceutical Chemistry Department.\u00a0The study aimed to design new N-hydroxyurea-based potential histone deacetylase (HDAC) inhibitors that were docked against different isoforms using the Schrodinger modeling suite. Compounds with the N-hydroxyurea moiety were linked to the cap and linker to give the final compounds that showed virtual bidentate zinc chelation in the HDACs active site, which is important for the inhibition.\u00a0Compounds containing urea hydroxylates as a linking group for zinc were manufactured, and zinc is considered important in inhibiting the activity of the histone deacetylase enzyme. The reactions were monitored using thin-layer chromatography to ensure the completion of the reactions, and the compounds were purified using column chromatography and Combiflash.\u00a0The final compounds were characterized using IR spectroscopy and NMR spectroscopy, and the results showed good agreement with the synthesized compounds. An evaluation of preliminary antiproliferative activities against colon cancer cell lines showed that the compounds with N-hydroxyurea molecules showed superior colon cancer cell line (LS-174T) growth inhibition efficacy compared to the FDA-approved HDAC inhibitor Vorinostat.<\/span><\/p>\n<p>[\/vc_column_text][\/vc_column][\/vc_row][vc_row][vc_column]<div id=\"cz_21747\" class=\"cz_grid_p cz_21747\"><div class=\"cz_grid cz_grid_1 clr cz_grid_c2 cz_grid_1_no_title cz_grid_1_mid tac cz_tooltip cz_grid_1_no_title\"><div class=\"cz_grid_item cz_grid_first\"><\/div><div class=\"cz_grid_item \"><div data-title=\"1\"><a class=\"cz_grid_link \" href=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2023\/12\/1-2.jpg\" data-xtra-lightbox><img loading=\"lazy\" decoding=\"async\" width=\"600\" height=\"600\" src=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2023\/12\/1-2-600x600.jpg\" class=\"attachment-codevz_600_600\" alt=\"\" title=\"1\" srcset=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2023\/12\/1-2-600x600.jpg 600w, https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2023\/12\/1-2-150x150.jpg 150w\" sizes=\"auto, (max-width: 600px) 100vw, 600px\" \/><div class=\"cz_grid_details\"><i class=\"fa fa-search cz_grid_icon\"><\/i><\/div><\/a><\/div><\/div><div class=\"cz_grid_item \"><div data-title=\"2\"><a class=\"cz_grid_link \" href=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2023\/12\/2-2.jpg\" data-xtra-lightbox><img loading=\"lazy\" decoding=\"async\" width=\"600\" height=\"597\" src=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2023\/12\/2-2-600x597.jpg\" class=\"attachment-codevz_600_600\" alt=\"\" title=\"2\" srcset=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2023\/12\/2-2-600x597.jpg 600w, https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2023\/12\/2-2-150x150.jpg 150w\" sizes=\"auto, (max-width: 600px) 100vw, 600px\" \/><div class=\"cz_grid_details\"><i class=\"fa fa-search cz_grid_icon\"><\/i><\/div><\/a><\/div><\/div><\/div><\/div>[\/vc_column][\/vc_row]<\/p>\n<\/div>","protected":false},"excerpt":{"rendered":"<p>[vc_row][vc_column][vc_column_text] The Faculty of Pharmacy discussed the MSc thesis entitled \u201cDesign, Synthesis, and Biological Evaluation of Novel N-Hydroxyurea Derivatives as &#8230; <a class=\"cz_readmore\" href=\"https:\/\/en.copharm.uobaghdad.edu.iq\/?p=4402\"><i class=\"fa czico-132-arrows-8\" aria-hidden=\"true\"><\/i><span>more<\/span><\/a><\/p>\n","protected":false},"author":9,"featured_media":4404,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_lmt_disableupdate":"","_lmt_disable":"","footnotes":""},"categories":[3,7],"tags":[],"class_list":["post-4402","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-latest-news","category-dissuasion"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v25.8 - 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