{"id":8021,"date":"2024-11-07T04:42:54","date_gmt":"2024-11-07T04:42:54","guid":{"rendered":"https:\/\/en.copharm.uobaghdad.edu.iq\/?p=8021"},"modified":"2024-11-07T04:43:46","modified_gmt":"2024-11-07T04:43:46","slug":"design-synthesis-and-preliminary-cytotoxicity-evaluation-of-new-2-mercaptobenzimidazole-derivatives","status":"publish","type":"post","link":"https:\/\/en.copharm.uobaghdad.edu.iq\/?p=8021","title":{"rendered":"Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New\u00a02-Mercaptobenzimidazole Derivatives"},"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 College of Pharmacy discussed the PhD dissertation entitled \u201c<strong>Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New 2-Mercaptobenzimidazole Derivatives<\/strong>\u201d by the student <strong>Shahbaa Shafeeq Rzoqi<\/strong> and the supervisor, Assistant Professor Dr. <strong>Mohammed Hassan Mohammed<\/strong>, at the Pharmaceutical Chemistry Department. The study aimed to conduct a molecular docking study and synthesize a new series of benzimidazole derivatives as possible alpha estrogen receptor inhibitors (by extracting their IC<sub>50 <\/sub>values) according to the SAR requirements. The study included the design of several 2-mercaptobenzimidazole derivatives that were directly prepared through S-alkylation with four different para-substituted 1-bromomethyl benzenes, followed by N-alkylation and ester hydrolysis, and o-alkylation with 1-(2-chloroethyl) piperidine, methylpiperazine, and morpholine moieties with potential cytotoxic activities against breast cancer. Prior to the synthesis of the target compounds, docking studies were conducted, which showed good docking scores compared to the standard raloxifene against estrogen receptor alpha (ER\u03b1). The results showed that the in-vitro cytotoxicity assay (MTT assay) demonstrated that compounds F1, F2, and F4 possess excellent cytotoxic effects (IC50: 30.61 \u00b1 3.28\u00b5M, IC50: 13.43 \u00b1 2.34\u00b5M, IC50: 24.78 \u00b1 1.02\u00b5M, respectively) towards breast cancer cell lines compared to standard raloxifene with IC50: 26.73 \u00b1 11.84\u00b5M. The study recommended to complete kinetic studies of compounds (F1, F2, F4, and F5) with further in vitro cytotoxic activity research on different cancer cell lines and in vivo studies.<\/span><\/p>\n<p>[\/vc_column_text][\/vc_column][\/vc_row][vc_row][vc_column]<div id=\"cz_49389\" class=\"cz_grid_p cz_49389\"><div class=\"cz_grid cz_grid_1 clr cz_grid_c3 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=\"Picture1\"><a class=\"cz_grid_link \" href=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture1-4.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\/2024\/11\/Picture1-4-600x600.jpg\" class=\"attachment-codevz_600_600\" alt=\"\" title=\"Picture1\" srcset=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture1-4-600x600.jpg 600w, https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture1-4-150x150.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=\"Picture2\"><a class=\"cz_grid_link \" href=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture2-4.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\/2024\/11\/Picture2-4-600x600.jpg\" class=\"attachment-codevz_600_600\" alt=\"\" title=\"Picture2\" srcset=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture2-4-600x600.jpg 600w, https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture2-4-150x150.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=\"Picture3\"><a class=\"cz_grid_link \" href=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture3-2.jpg\" data-xtra-lightbox><img loading=\"lazy\" decoding=\"async\" width=\"444\" height=\"503\" src=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture3-2.jpg\" class=\"attachment-codevz_600_600\" alt=\"\" title=\"Picture3\" srcset=\"https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture3-2.jpg 444w, https:\/\/en.copharm.uobaghdad.edu.iq\/wp-content\/uploads\/sites\/80\/2024\/11\/Picture3-2-265x300.jpg 265w\" sizes=\"auto, (max-width: 444px) 100vw, 444px\" \/><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 College of Pharmacy discussed the PhD dissertation entitled \u201cDesign, Synthesis, and Preliminary Cytotoxicity Evaluation of New 2-Mercaptobenzimidazole Derivatives\u201d &#8230; <a class=\"cz_readmore\" href=\"https:\/\/en.copharm.uobaghdad.edu.iq\/?p=8021\"><i class=\"fa czico-132-arrows-8\" aria-hidden=\"true\"><\/i><span>more<\/span><\/a><\/p>\n","protected":false},"author":9,"featured_media":8022,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"_lmt_disableupdate":"no","_lmt_disable":"","footnotes":""},"categories":[3,7,5],"tags":[],"class_list":["post-8021","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-latest-news","category-dissuasion","category-last-news"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v25.8 - 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