{"title":"基于苯并咪唑的类似物作为潜在微管蛋白聚合抑制剂的最新进展:综述。","authors":"Rajkumar Reddyrajula, Priya Varshini Kathirvel, Nagula Shankaraiah","doi":"10.1016/j.bmcl.2025.130167","DOIUrl":null,"url":null,"abstract":"<div><div>Microtubules, as dynamic regulators in many cellular processes, remain pivotal targets in cancer chemotherapy. Among the structural motifs explored, the benzimidazole scaffold has emerged as a privileged heterocyclic ring system in the development of potent therapeutic agents, owing to its versatility and pharmacological relevance. This review critically examines the synthesis, anticancer activity, structure-activity relationships (SAR), and tubulin polymerization inhibitory properties of diverse benzimidazole derivatives. In addition, various synthetic strategies and innovative approaches for generating benzimidazole based analogs with enhanced cytotoxic profiles are highlighted. Recent findings underscore the potential of benzimidazole derivatives as promising tubulin polymerization inhibitors, contributing significantly to the discovery of next-generation anticancer agents.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"122 ","pages":"Article 130167"},"PeriodicalIF":2.5000,"publicationDate":"2025-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Recent developments of benzimidazole based analogs as potential tubulin polymerization inhibitors: A critical review\",\"authors\":\"Rajkumar Reddyrajula, Priya Varshini Kathirvel, Nagula Shankaraiah\",\"doi\":\"10.1016/j.bmcl.2025.130167\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Microtubules, as dynamic regulators in many cellular processes, remain pivotal targets in cancer chemotherapy. Among the structural motifs explored, the benzimidazole scaffold has emerged as a privileged heterocyclic ring system in the development of potent therapeutic agents, owing to its versatility and pharmacological relevance. This review critically examines the synthesis, anticancer activity, structure-activity relationships (SAR), and tubulin polymerization inhibitory properties of diverse benzimidazole derivatives. In addition, various synthetic strategies and innovative approaches for generating benzimidazole based analogs with enhanced cytotoxic profiles are highlighted. Recent findings underscore the potential of benzimidazole derivatives as promising tubulin polymerization inhibitors, contributing significantly to the discovery of next-generation anticancer agents.</div></div>\",\"PeriodicalId\":256,\"journal\":{\"name\":\"Bioorganic & Medicinal Chemistry Letters\",\"volume\":\"122 \",\"pages\":\"Article 130167\"},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2025-03-10\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Bioorganic & Medicinal Chemistry Letters\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0960894X25000769\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0960894X25000769","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Recent developments of benzimidazole based analogs as potential tubulin polymerization inhibitors: A critical review
Microtubules, as dynamic regulators in many cellular processes, remain pivotal targets in cancer chemotherapy. Among the structural motifs explored, the benzimidazole scaffold has emerged as a privileged heterocyclic ring system in the development of potent therapeutic agents, owing to its versatility and pharmacological relevance. This review critically examines the synthesis, anticancer activity, structure-activity relationships (SAR), and tubulin polymerization inhibitory properties of diverse benzimidazole derivatives. In addition, various synthetic strategies and innovative approaches for generating benzimidazole based analogs with enhanced cytotoxic profiles are highlighted. Recent findings underscore the potential of benzimidazole derivatives as promising tubulin polymerization inhibitors, contributing significantly to the discovery of next-generation anticancer agents.
期刊介绍:
Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.