[{"data":1,"prerenderedAt":-1},["ShallowReactive",2],{"doc-detail-31895":3,"doc-seo-31895":27},{"code":4,"msg":5,"data":6},0,"success",{"doc_id":7,"user_id":8,"nickname":9,"user_avatar":10,"doc_module":4,"category_id":11,"category_name":12,"doc_title":13,"doc_description":14,"file_id":15,"file_url":16,"file_type":17,"file_size":18,"view_count":4,"is_deleted":4,"is_public":19,"is_downloadable":19,"audit_status":19,"page_count":20,"language":21,"language_code":22,"table_of_contents":23,"faqs":24,"seo_title":13,"seo_description":14,"update_tm":25,"read_time":26},31895,1099513958607,"Jiven","https://ap-avatar.wpscdn.com/avatar/100002390cf8733938c?x-image-process=image/resize,m_fixed,w_180,h_180&k=1778829742770036399",8,"Research & Report","Thioxoimidazolidinone Derivatives as EGFR Inhibitors for Cancer Therapy","Cancer remains a leading cause of death, and EGFR dysregulation—through overexpression or mutation—drives uncontrolled growth and therapy failure. Existing EGFR inhibitors can be limited by mutation-driven resistance, toxicity, and reduced efficacy. Imidazole derivatives are highlighted as ATP-site binders that suppress EGFR signaling and can show nanomolar-range potency. Building on structure–activity rationale, thioxoimidazolidinone derivatives bearing thioacetamide were designed via ligand-based drug design and evaluated for cytotoxic and EGFR-inhibiting activity.","cbCaid2At22QOR2g","https://ap.wps.com/l/cbCaid2At22QOR2g","pdf",3644854,1,13,"English","en","# Introduction\n## Rationale for designing the target compounds and the aim of work","[{\"question\":\"Why is EGFR considered a promising target for cancer therapy?\",\"answer\":\"EGFR is a key surface protein that regulates signaling controlling cell division, survival, adhesion, and migration. Overexpression and mutation of EGFR are linked to cancer development and progression.\"},{\"question\":\"What challenges limit the effectiveness of FDA-approved EGFR inhibitors?\",\"answer\":\"Emerging EGFR mutations can reduce therapeutic effectiveness, increasing toxicity and leading to drug resistance.\"},{\"question\":\"What design strategy and structural features guide the target compounds in this study?\",\"answer\":\"A ligand-based drug design rationale is used based on EGFR inhibitor interactions: a hinge-region heterocycle contacting Met793, a hydrophobic group occupying the hydrophobic groove, a hydrophilic linker forming hydrogen bonds, and a hydrophobic tail fitting the binding pocket. Thioxoimidazolidinone derivatives with a thioacetamide moiety were synthesized and tested for cytotoxic and EGFR-inhibiting properties.\"}]",1780434044,33,{"code":4,"msg":28,"data":29},"ok",{"site_id":30,"language":22,"slug":31,"title":13,"keywords":32,"description":14,"schema_data":33,"social_meta":84,"head_meta":86,"extra_data":88,"updated_unix":25},105,"thioxoimidazolidinone-derivatives-as-egfr-inhibitors-for-cancer-therapy","",{"@graph":34,"@context":83},[35,52,66],{"@type":36,"itemListElement":37},"BreadcrumbList",[38,42,46,49],{"item":39,"name":40,"@type":41,"position":19},"https://docshare.wps.com","Home","ListItem",{"item":43,"name":44,"@type":41,"position":45},"https://docshare.wps.com/document/","Document",2,{"item":47,"name":12,"@type":41,"position":48},"https://docshare.wps.com/document/research-report/",3,{"item":50,"name":13,"@type":41,"position":51},"https://docshare.wps.com/document/thioxoimidazolidinone-derivatives-as-egfr-inhibitors-for-cancer-therapy/31895/",4,{"url":50,"name":13,"@type":53,"author":54,"headline":13,"publisher":56,"fileFormat":59,"description":14,"dateModified":60,"datePublished":60,"encodingFormat":59,"isAccessibleForFree":61,"interactionStatistic":62},"DigitalDocument",{"name":9,"@type":55},"Person",{"url":39,"name":57,"@type":58},"DocShare","Organization","application/pdf","2026-06-02",true,{"@type":63,"interactionType":64,"userInteractionCount":4},"InteractionCounter",{"@type":65},"ViewAction",{"@type":67,"mainEntity":68},"FAQPage",[69,75,79],{"name":70,"@type":71,"acceptedAnswer":72},"Why is EGFR considered a promising target for cancer therapy?","Question",{"text":73,"@type":74},"EGFR is a key surface protein that regulates signaling controlling cell division, survival, adhesion, and migration. Overexpression and mutation of EGFR are linked to cancer development and progression.","Answer",{"name":76,"@type":71,"acceptedAnswer":77},"What challenges limit the effectiveness of FDA-approved EGFR inhibitors?",{"text":78,"@type":74},"Emerging EGFR mutations can reduce therapeutic effectiveness, increasing toxicity and leading to drug resistance.",{"name":80,"@type":71,"acceptedAnswer":81},"What design strategy and structural features guide the target compounds in this study?",{"text":82,"@type":74},"A ligand-based drug design rationale is used based on EGFR inhibitor interactions: a hinge-region heterocycle contacting Met793, a hydrophobic group occupying the hydrophobic groove, a hydrophilic linker forming hydrogen bonds, and a hydrophobic tail fitting the binding pocket. Thioxoimidazolidinone derivatives with a thioacetamide moiety were synthesized and tested for cytotoxic and EGFR-inhibiting properties.","https://schema.org",{"og:url":50,"og:type":85,"og:title":13,"og:site_name":57,"og:description":14},"article",{"robots":87,"canonical":50},"index,follow",{"doc_id":7,"site_id":30}]