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Despite progress in medicine, treatment still faces hurdles from drug resistance, toxicity of combination regimens, and limited selectivity toward cancer cells. Multitarget directed ligands (MTDLs) address these issues by engaging multiple molecular targets. This review summarizes novel multi-target derivatives of nitrogen-containing heterocycles—imidazole, pyrazole, 1,2,3-triazole, and 1,2,4-triazole—covering literature from 2006 to 2026. It emphasizes inhibitory potency, protein binding interactions, and structure-activity relationship (SAR) insights to support development of new multi-target anticancer agents.",{"@graph":69,"@context":122},[70,84,105],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":40,"@type":76,"position":81},"https://docshare.wps.com/document/research-report/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/diversity-and-multi-target-potential-of-pyrazole-imidazole-or-triazole-derivatives-in-modern-anticancer-therapy/350338/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/diversity-and-multi-target-potential-of-pyrazole-imidazole-or-triazole-derivatives-in-modern-anticancer-therapy/350338.png","ImageObject",300,407,{"name":92,"@type":93},"Cart","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-09-23","2026-09-22",true,{"@type":102,"interactionType":103,"userInteractionCount":14},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"What challenges in cancer therapy does multitarget directed ligands (MTDLs) aim to address?","Question",{"text":112,"@type":113},"They help overcome drug resistance, reduce toxicity issues seen in combination therapy, and improve drug selectivity toward cancer cells.","Answer",{"name":115,"@type":110,"acceptedAnswer":116},"Which nitrogen-containing heterocycles are covered in the review?",{"text":117,"@type":113},"Imidazole, pyrazole, 1,2,3-triazole, and 1,2,4-triazole derivatives are reviewed as multi-targeted candidates.",{"name":119,"@type":110,"acceptedAnswer":120},"What evaluation dimensions does the review focus on for the selected molecules?",{"text":121,"@type":113},"It analyzes inhibitory activity across molecular targets, binding interactions with protein sites, and includes structure-activity relationship (SAR) studies.","https://schema.org",{"og:url":83,"og:type":124,"og:title":65,"og:site_name":95,"og:description":67},"article",{"robots":126,"canonical":83},"index,follow",{"doc_id":128,"site_id":62},350338,1790135672,{"code":4,"msg":5,"data":131},{"doc_id":128,"user_id":132,"nickname":92,"user_avatar":133,"doc_module":4,"category_id":39,"category_name":40,"doc_title":65,"doc_description":67,"doc_content":134,"file_id":135,"file_url":136,"file_type":137,"file_size":138,"view_count":14,"is_deleted":4,"is_public":8,"is_downloadable":8,"audit_status":8,"page_count":139,"language":140,"language_code":63,"site_id":62,"html_lang":63,"table_of_contents":141,"faqs":142,"seo_title":143,"seo_description":67,"update_tm":144,"read_time":145},18829141979164,"https://eur-avatar.wpscdn.com/davatar_6f874abed73319feea01a86fa6f0fab8","Review  \nDiversity and Multi-Target Potential of Pyrazole, Imidazole or Triazole Derivatives in Modern Anticancer Therapy  \nMartyna Mysłek 1,†, Anna Kaczmarek 2,†, Piotr ´Swi ˛atek 2, * and Z˙aneta Czynikowska 1, *  \nAcademic Editors: Oleg M. Demchuk and Monika Wujec  \nReceived: 13 March 2026  \nRevised: 4 May 2026  \nAccepted: 5 May 2026  \nPublished: 7 May 2026  \nCopyright: © 2026 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.  \n1 Department of Basic Chemical Sciences, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211a, 50-556 Wroclaw, Poland; [martyna.myslek@student.umw.edu.pl](martyna.myslek@student.umw.edu.pl)  \n2 Department of Medicinal Chemistry, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211a, 50-556 Wroclaw, Poland; [anna.kaczmarek@umw.edu.pl](anna.kaczmarek@umw.edu.pl)  \n* [Correspondence: piotr.swiatek@umw.edu.pl](Correspondence: piotr.swiatek@umw.edu.pl) (P.´S .); zaneta.czyznikowska@umw.edu.pl (Z˙ .C.);  \nTel.: +48-71-784-03-90 (P.´S .); +48-71-784-03-31 (Z˙ .C.)† These authors contributed equally to this work.  \nAbstract  \nCancers are intricate and multifactorial diseases. Despite progress in medicine, there are still some obstacles in their treatment due to drug resistance, the toxicity of combination therapy and lack of drug selectivity toward cancer cells. The solution to this may be multitarget directed ligands (MTDLs), which have gained more and more popularity over the years. This review presents a comprehensive overview of novel potential multi-targeted derivatives of nitrogen-containing heterocycles, as imidazole, pyrazole, 1,2,3-triazole and 1,2,4-triazole. The review gathers the selected literature from 2006 to 2026 . The analysis focuses on the potency of the inhibitory activity of selected molecules against a variety of molecular targets, as well as on their interactions with protein binding sites. Additionally, the structure-activity relationship (SAR) studies within the collected series are included. The discussion may contribute to the development of new multi-target anticancer agents.  \nKeywords: multi-target directed ligands; anticancer therapy; nitrogen heterocycles; imidazole; pyrazole; triazole  \n1. Introduction  \nCancer remains one of the most significant global health challenges of the 21st century. Statistics from the International Agency for Research on Cancer (IARC) for the year 2022 showed that there were around 20 million new cases of cancer and around 9.7 million deaths. According to the data, on average, one in five people in the world may develop cancer during their lifetime [1] . The observed increase in cancerous cases is consistent with population ageing and socio-economic development, and is indicative of changes in lifestyle and environmental exposure. Despite the valuable progress that has been made in the fields of early diagnosis and targeted therapy, drug resistance and metastasis limit the effectiveness of therapeutic approaches. Therefore, the design of new chemical compounds capable of modulating biological targets through non-traditional interaction patterns has become a major focus of current drug discovery efforts. In recent years, the development of multi-targeted therapies has strengthened optimism in the fight against cancer. Multitarget directed ligands (MTDLs) can modulate several signaling pathways simultaneously. Such an approach has proven effective in treating cancers and complex diseases with multifactorial etiology, including neurodegenerative disorders, cardiovascular diseases, and chronic inflammatory conditions. The therapeutic potency of a multi-target agent is  \nenhanced by synergistic effects associated with the simultaneous inhibition of activation of multiple key enzymes, receptors, or transcription factors. Furthermore, to achieve the desired pharmacological effect, such compounds require ","cbCaipPQNplzv20g","https://ap.wps.com/l/cbCaipPQNplzv20g","pdf",8102112,63,"English","# Abstract\n# 1. Introduction","[{\"question\":\"What challenges in cancer therapy does multitarget directed ligands (MTDLs) aim to address?\",\"answer\":\"They help overcome drug resistance, reduce toxicity issues seen in combination therapy, and improve drug selectivity toward cancer cells.\"},{\"question\":\"Which nitrogen-containing heterocycles are covered in the review?\",\"answer\":\"Imidazole, pyrazole, 1,2,3-triazole, and 1,2,4-triazole derivatives are reviewed as multi-targeted candidates.\"},{\"question\":\"What evaluation dimensions does the review focus on for the selected molecules?\",\"answer\":\"It analyzes inhibitory activity across molecular targets, binding interactions with protein sites, and includes structure-activity relationship (SAR) studies.\"}]","Diversity and Multi-Target Potential of Pyrazole, Imidazole or Triazole Derivatives in Modern Anticancer Therapy | PDF",1790088539,159]