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The compounds were evaluated for in vitro cytotoxic activity against three human cancer cell lines (HCT-116, MCF-7, HepG2) and one normal cell line (WRL-68) at 48 and 72 h. Results indicated moderate to good anticancer potential, with 8a showing the strongest effects on HCT-116 and HepG2, and 8f best on MCF-7. Docking studies supported interactions with possible targets while limited toxicity appeared in normal cells.",{"@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":35,"@type":76,"position":81},"https://docshare.wps.com/document/healthcare/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/design-synthesis-and-cytotoxic-evaluation-of-quinazoline-derivatives-bearing-triazole-acetamides/406723/",{"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/design-synthesis-and-cytotoxic-evaluation-of-quinazoline-derivatives-bearing-triazole-acetamides/406723.png","ImageObject",300,407,{"name":92,"@type":93},"dabgoudw","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-11-06","2026-09-28",true,{"@type":102,"interactionType":103,"userInteractionCount":52},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"What compounds were designed and synthesized in the study?","Question",{"text":112,"@type":113},"A series of quinazoline-based agents bearing triazole-acetamides (8a–l) were designed and synthesized for evaluation.","Answer",{"name":115,"@type":110,"acceptedAnswer":116},"Which cell lines were used to test cytotoxic activity?",{"text":117,"@type":113},"Cytotoxicity was tested against three human cancer cell lines (HCT-116, MCF-7, HepG2) and one normal cell line (WRL-68) at 48 and 72 h.",{"name":119,"@type":110,"acceptedAnswer":120},"Which derivatives showed the strongest anticancer activity?",{"text":121,"@type":113},"8a showed the most potent results against HCT-116 and also the best results against HepG2, while 8f exhibited the best activity against MCF-7 at 48 h.","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},406723,1790912868,{"code":4,"msg":5,"data":131},{"doc_id":128,"user_id":132,"nickname":92,"user_avatar":133,"doc_module":4,"category_id":34,"category_name":35,"doc_title":65,"doc_description":67,"doc_content":134,"file_id":135,"file_url":136,"file_type":137,"file_size":138,"view_count":52,"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,"preview_page_count":4},3985747860484,"https://ap-avatar.wpscdn.com/davatar_276721f389ce27ea32af1340a28f341c","Heliyon 9 (2023) e13528  \nContents lists available at ScienceDirect  \nHeliyon  \njournal [homepage:](homepage: www.cell.com/heliyon)[ www.cell.com/heliyon](homepage: www.cell.com/heliyon)  \n| Research article\u003Cbr>Design, synthesis, and cytotoxic evaluation of quinazoline derivatives bearing triazole-acetamides |  |  | |\n| --- | --- | --- | --- |\n| Keyvan Pedrood a, Fahimeh Taayoshi b, Ali Moazzam a, Aida Iraji c, d, Ali Yavari a, Samira Ansari e, Sayed Mahmoud Sajjadi-Jazi a,\u003Cbr>Mohammad Reza Mohajeri-Tehrani a, Nadia Garmsirif, Vahid Haghpanah a, Meysam Soleymanibadi g, Bagher Larijani a, Haleh Hamedifar e, h, Neda Adibpour b, **,\u003Cbr>*\u003Cbr>Mohammad Mahdavi a,\u003Cbr>a Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran\u003Cbr>b Department of Medicinal Chemistry, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran c Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran\u003Cbr>d Central Research Laboratory, Shiraz University of Medical Sciences, Shiraz, Iran\u003Cbr>e CinnaGen Medical Biotechnology Research Center, Alborz University of Medical Sciences, Karaj, Iran f Department of Biology, Payame Noor University (PNU), P.O.Box 19395-4697, Tehran, Iran\u003Cbr>g Department of Pharmaceutical Biotechnology, School of Pharmacy, Hamadan University of Medical Science Hamadan, Iran h CinnaGen Research and Production Co., Alborz, Iran |  |  |  |\n| A R T I C L E I N F O |  | A B S T R A C T |  |\n| Keywords: Anticancer activity Click chemistry Docking Quinazoline |  | A novel series of quinazoline-based agents bearing triazole-acetamides 8a-l were designed and synthesized. All the obtained compounds were tested for in vitro cytotoxic activities against three human cancer cell lines named HCT-116, MCF-7, and HepG2, as well as a normal cell line WRL-68 after 48 and 72 h. The results implied that quinazoline-oxymethyltriazole compounds exhibited moderate to good anticancer potential. The most potent derivative against HCT-116 was 8a (X = 4-OCH3 and R = H) with IC50 values of 10.72 and 5.33 μM after 48 and 72 h compared with doxorubicin with IC50 values of 1.66 and 1.21 μM, respectively. The same trend was seen in the HepG2 cancerous cell line in which 8a recorded the best results with IC50 values of 17.48 and 7.94 after 48 and 72 h, respectively. The cytotoxic analysis against MCF-7 showed that 8f with IC50 = 21.29 μM (48 h) exhibited the best activity, while compounds 8k (IC 50 = 11.32 μM) and 8a (IC 50 = 12.96 μM), known as the most effective cytotoxic agents after 72 h. Doxorubicin as positive control exhibited IC50 values of 1.15 and 0.82 μM after 48 and 72 h, respectively. Noteworthy, all derivatives showed limited toxicity against the normal cell line. Moreover, docking studies were also presented to understand the interactions between these novel derivatives and possible targets. |  |\n\n* Corresponding author.  \n** Corresponding author.  \nE-mail addresses: [n.adibpor@zums.ac.ir](n.adibpor@zums.ac.ir) (N. Adibpour), [momahdavi@sina.tums.ac.ir](momahdavi@sina.tums.ac.ir) (M. Mahdavi).  \n[https://doi.org/10.1016/j.heliyon.2023.e13528](https://doi.org/10.1016/j.heliyon.2023.e13528)  \nReceived 15 September 2022; Received in revised form 27 January 2023; Accepted 1 February 2023 Available online 4 February 2023  \n2405-8440/© 2023 Published by Elsevier Ltd. This is an open access article under the CC BY-NC-ND license  \n([http://creativecommons.org/licenses/by-nc-nd/4.0/](http://creativecommons.org/licenses/by-nc-nd/4.0/)).  \n1. Introduction  \nCancer is a multifactorial disease known as the uncontrolled growth of abnormal cells in a body that can infiltrate and destroy normal body tissue [1]. Cancer is expected to be one of the leading causes of death, affecting the lives of millions of people around the world. According to a report on the global burden of cancer worldwide, there were 18.1 million new cancer ","cbCaib07OHxSM3vR","https://ap.wps.com/l/cbCaib07OHxSM3vR","pdf",1514086,11,"English","# Introduction\n## Cancer background and hallmarks\n## Quinazoline scaffold and drug relevance\n## Triazoles and click chemistry rationale","[{\"question\":\"What compounds were designed and synthesized in the study?\",\"answer\":\"A series of quinazoline-based agents bearing triazole-acetamides (8a–l) were designed and synthesized for evaluation.\"},{\"question\":\"Which cell lines were used to test cytotoxic activity?\",\"answer\":\"Cytotoxicity was tested against three human cancer cell lines (HCT-116, MCF-7, HepG2) and one normal cell line (WRL-68) at 48 and 72 h.\"},{\"question\":\"Which derivatives showed the strongest anticancer activity?\",\"answer\":\"8a showed the most potent results against HCT-116 and also the best results against HepG2, while 8f exhibited the best activity against MCF-7 at 48 h.\"}]","Design, synthesis, and cytotoxic evaluation of quinazoline derivatives bearing triazole-acetamides | PDF",1790567545,28]