[{"data":1,"prerenderedAt":-1},["ShallowReactive",2],{"doc-seo-628508-105":3,"detail-sidebar-cat-0-en-105":80,"doc-detail-628508-en":130},{"code":4,"msg":5,"data":6},0,"ok",{"site_id":7,"language":8,"slug":9,"title":10,"keywords":11,"description":12,"schema_data":13,"social_meta":73,"head_meta":75,"extra_data":77,"updated_unix":79},105,"en","an-outlook-of-the-structure-activity-relationship-sar-of-naphthalimide-derivatives-as-anticancer-agents","An Outlook of the Structure Activity Relationship (SAR) of Naphthalimide Derivatives as Anticancer Agents","","Drug efficacy against cancer in clinical practice is often constrained by pharmacokinetic limitations, adverse side effects, and the emergence of resistance. Naphthalimide-based anticancer agents have shown strong effectiveness, including high DNA binding affinity and activity across multiple cancer types. Studies on diverse naphthalimide derivatives—heterocyclic fused, substituted, metal-containing, and carboxamide forms—identify cases with superior potency to reference standards such as cisplatin and related agents. The focus is to clarify how substitution patterns modulate the structure-activity relationship and which modifications enhance or diminish activity.",{"@graph":14,"@context":72},[15,34,55],{"@type":16,"itemListElement":17},"BreadcrumbList",[18,23,27,31],{"item":19,"name":20,"@type":21,"position":22},"https://docshare.wps.com","Home","ListItem",1,{"item":24,"name":25,"@type":21,"position":26},"https://docshare.wps.com/document/","Document",2,{"item":28,"name":29,"@type":21,"position":30},"https://docshare.wps.com/document/healthcare/","Healthcare",3,{"item":32,"name":10,"@type":21,"position":33},"https://docshare.wps.com/document/an-outlook-of-the-structure-activity-relationship-sar-of-naphthalimide-derivatives-as-anticancer-agents/628508/",4,{"url":32,"name":10,"@type":35,"image":36,"author":41,"headline":10,"publisher":44,"fileFormat":47,"inLanguage":8,"description":12,"dateModified":48,"datePublished":49,"encodingFormat":47,"isAccessibleForFree":50,"interactionStatistic":51},"DigitalDocument",{"url":37,"@type":38,"width":39,"height":40},"https://docshare.wps.com/thumbnails/an-outlook-of-the-structure-activity-relationship-sar-of-naphthalimide-derivatives-as-anticancer-agents/628508.png","ImageObject",300,407,{"name":42,"@type":43},"Hazel","Person",{"url":19,"name":45,"@type":46},"DocShare","Organization","application/pdf","2026-11-10","2026-10-21",true,{"@type":52,"interactionType":53,"userInteractionCount":33},"InteractionCounter",{"@type":54},"ViewAction",{"@type":56,"mainEntity":57},"FAQPage",[58,64,68],{"name":59,"@type":60,"acceptedAnswer":61},"Why are naphthalimide derivatives considered promising anticancer agents?","Question",{"text":62,"@type":63},"They have demonstrated strong DNA binding affinity and anticancer efficacy across multiple cancer types. Their activity also supports targeting various cancer cell lines.","Answer",{"name":65,"@type":60,"acceptedAnswer":66},"How do structural features influence the structure-activity relationship (SAR) of naphthalimides?",{"text":67,"@type":63},"The document emphasizes that substitution patterns affect biological activity, including cases where derivatives outperform reference norms. Changes to side chains, aromatic systems, and ring substituents are highlighted as key variables.",{"name":69,"@type":60,"acceptedAnswer":70},"What mechanisms beyond DNA intercalation are mentioned for anticancer effects?",{"text":71,"@type":63},"Besides intercalating into DNA, naphthalimide derivatives can generate reactive oxygen species, disrupt mitochondrial and lysosome function, inhibit histone deacetylase, and interfere with DNA/RNA synthesis. They may also activate receptor tyrosine kinases and influence apoptosis-related pathways.","https://schema.org",{"og:url":32,"og:type":74,"og:title":10,"og:site_name":45,"og:description":12},"article",{"robots":76,"canonical":32},"index,follow",{"doc_id":78,"site_id":7},628508,1792835107,{"code":4,"msg":81,"data":82},"success",[83,87,91,95,100,105,109,114,119,122,126],{"id":22,"doc_module":4,"doc_module_name":25,"category_name":84,"show_sort_weight":85,"slug":86},"Story & Novel",90,"story-novel",{"id":26,"doc_module":4,"doc_module_name":25,"category_name":88,"show_sort_weight":89,"slug":90},"Literature",80,"literature",{"id":33,"doc_module":4,"doc_module_name":25,"category_name":92,"show_sort_weight":93,"slug":94},"Exam",70,"exam",{"id":96,"doc_module":4,"doc_module_name":25,"category_name":97,"show_sort_weight":98,"slug":99},5,"Comic",60,"comic",{"id":101,"doc_module":4,"doc_module_name":25,"category_name":102,"show_sort_weight":103,"slug":104},6,"Technology",50,"technology",{"id":106,"doc_module":4,"doc_module_name":25,"category_name":29,"show_sort_weight":107,"slug":108},7,40,"healthcare",{"id":110,"doc_module":4,"doc_module_name":25,"category_name":111,"show_sort_weight":112,"slug":113},8,"Research & Report",30,"research-report",{"id":115,"doc_module":4,"doc_module_name":25,"category_name":116,"show_sort_weight":117,"slug":118},9,"Religion & Spirituality",20,"religion-spirituality",{"id":117,"doc_module":4,"doc_module_name":25,"category_name":120,"show_sort_weight":117,"slug":121},"World Cup","world-cup",{"id":123,"doc_module":4,"doc_module_name":25,"category_name":124,"show_sort_weight":123,"slug":125},10,"Lifestyle","lifestyle",{"id":127,"doc_module":4,"doc_module_name":25,"category_name":128,"show_sort_weight":96,"slug":129},19,"General","general",{"code":4,"msg":81,"data":131},{"doc_id":78,"user_id":132,"nickname":42,"user_avatar":133,"doc_module":4,"category_id":106,"category_name":29,"doc_title":10,"doc_description":12,"doc_content":134,"file_id":135,"file_url":136,"file_type":137,"file_size":138,"view_count":33,"is_deleted":4,"is_public":22,"is_downloadable":22,"audit_status":22,"page_count":139,"language":140,"language_code":8,"site_id":7,"html_lang":8,"table_of_contents":141,"faqs":142,"seo_title":143,"seo_description":12,"update_tm":144,"read_time":145,"preview_page_count":4},137441390410,"https://ap-avatar.wpscdn.com/avatar/2000252f4ab5702993?_k=1776741390130283984","Send Orders for Reprints [to reprints@benthamscience.net](to reprints@benthamscience.net)  \nAnti-Cancer Agents in Medicinal Chemistry, XXXX, XX, 0-0 1  \nREVIEW ARTICLE  \nAn Outlook of the Structure Activity Relationship (SAR) of Naphthalimide Derivatives as Anticancer Agents  \nAeyaz Ahmad Bhat 1,*  \n1Department of Chemistry, School of Physical Sciences, Lovely Professional University, Phagwara, 144411, India  \nA R T I C L E H I S T O R Y  \nReceived: August 09, 2023  \nRevised: September 19, 2023  \nAccepted: October 13, 2023  \nDOI:  \n10. 2174/0118715206274007231107094411  \nAbstract: The efficacy of drugs against cancer in clinical settings may be limited due to pharmacokinetic issues, side effects and the emergence of drug resistance. However, a class of anticancer drugs known as naphthalimides have proven to be very effective. These derivatives have demonstrated to be effective in treating different types of cancers and exhibit strong DNA binding affinity. The anticancer properties of the naphthalimide derivatives allow them to target a number of cancer cell lines. Researchers have investigated the anticancer activity of numerous naphthalimide derivatives, such as heterocyclic fused, non-fused substituted, metal-substituted and carboxamide derivatives. Surprisingly, some derivatives demonstrate greater activity than the reference norms, such as cisplatin, amonafide, mitonafide and others and are selective against many cell lines. The primary objective of this research is to comprehend the effects of various substitution patterns on the structure-activity relationship (SAR) of these derivatives and the instances in which they enhance or reduce this biological activity.  \nKeywords: Anticancer, apoptosis, naphthalimide, 1,8 naphthalimide derivatives, structure activity relationship (SAR), synthesis.  \n1. A BRIEF INTRODUCTION TO NAPHTHALIMIDES  \nA class of polycyclic imides known as 1Hbenzo[de]isoquinoline-1,3-(2H)-diones includes naphthalimides. These compounds have valuable physicochemical and biological characteristics and their derivatives also share these characteristics. Numerous biological activities, including analgesic, antibacterial, antiviral and anticancer effects are displayed by naphthalimides and their derivatives [1] . In fact, naphthalimides' potent anticancer action is greatly influenced by their capacity to intercalate into DNA. Naphthalimides can interfere with DNA's natural structure and function when they intercalate between the base pairs [2] . However, there are additional mechanisms by which naphthalimides and their derivatives can exert their anticancer properties. Some of these include the production of reactive oxygen species (ROS), the disruption of mitochondrial and lysosome function, the inhibition of histone deacetylase, the interruption of DNA and RNA synthesis and the activation of receptor tyrosine kinases [3-5] . Naphthalimides are a class of organic substances that have sparked interest in cancer research due to their anticancer properties. Naphthalimides are known to intercalate between DNA base pairs, altering DNA structure and impeding activities such as DNA replication and transcription. This trait has the potential to limit cancer cell proliferation and ultimately cause cell death. In preclinical studies, several naphthalimide compounds demonstrated considerable anticancer efficacy. Researchers have been striving to improve the structure of naphthalimides in order to increase their selectivity for cancer cells while reducing harm to healthy cells. This selectivity is critical for lowering side effects and improving cancer treatment safety [6] . They have been demonstrated to be beneficial against a wide range of cancers, including lung, breast, ovarian and colon cancer. The naphthalimide family consists of the three well-known compounds mitonafide, pinafide, and amonafide. Mitonafide, also  \n*Address correspondence to this author at the Department of Chemistry, School of Physical Sciences, ","cbCaiquvBUxfe1Tb","https://ap.wps.com/l/cbCaiquvBUxfe1Tb","pdf",4874375,21,"English","# A brief introduction to naphthalimides\n## DNA intercalation and mechanisms\n## Reported anticancer activities and derivative classes","[{\"question\":\"Why are naphthalimide derivatives considered promising anticancer agents?\",\"answer\":\"They have demonstrated strong DNA binding affinity and anticancer efficacy across multiple cancer types. Their activity also supports targeting various cancer cell lines.\"},{\"question\":\"How do structural features influence the structure-activity relationship (SAR) of naphthalimides?\",\"answer\":\"The document emphasizes that substitution patterns affect biological activity, including cases where derivatives outperform reference norms. Changes to side chains, aromatic systems, and ring substituents are highlighted as key variables.\"},{\"question\":\"What mechanisms beyond DNA intercalation are mentioned for anticancer effects?\",\"answer\":\"Besides intercalating into DNA, naphthalimide derivatives can generate reactive oxygen species, disrupt mitochondrial and lysosome function, inhibit histone deacetylase, and interfere with DNA/RNA synthesis. They may also activate receptor tyrosine kinases and influence apoptosis-related pathways.\"}]","An Outlook of the Structure Activity Relationship (SAR) of Naphthalimide Derivatives as Anticancer Agents | PDF",1792616839,53]