Priya Sakshi, Islam Md Mustahidul, Kasana Shivani, Kurmi Balak Das, Gupta Ghanshyam Das, Patel Preeti
Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, India.
IK Gujral Punjab Technical University, Kapurthala, India.
Future Med Chem. 2025 Feb;17(4):449-465. doi: 10.1080/17568919.2025.2458450. Epub 2025 Jan 31.
The study of chalcone-1,2,3-triazole hybrids for anticancer activity is quite a recent area of focus, primarily because of the increasing demand for developing new drugs to treat cancer. The chalcones and 1,2,3-triazole rings in hybrid compounds has recently emerged as a promising strategy for developing novel anticancer agents. The 1,2,3-triazole ring, known for its stability and hydrogen bonding capabilities, enhances the target binding affinity of these hybrids. Chalcones possess an α,β-unsaturated carbonyl system crucial for their anticancer activity The synergistic effect of these two moieties results in compounds with potent anticancer properties. This review explores the structure-activity relationship studies which revealed that the electronic and lipophilic properties of substituents on the phenyl rings of chalcones significantly influence their anticancer activity. Electron-donating and electron-withdrawing groups can affect cellular uptake and target engagement. Incorporating various substituents into the 1,2,3-triazole ring can improve selectivity and potency against specific cancer cell lines. These hybrids often exert their anticancer effects through apoptosis and cell cycle disruption. Recent research indicates 1,2,3-triazole chalcone hybrids hold therapeutic promise as anticancer agents. Further optimization through SAR studies and in-depth mechanistic investigations could lead to the development of highly potent and selective anticancer agents with minimal toxicity.
查尔酮 - 1,2,3 - 三唑杂化物的抗癌活性研究是一个相当新的重点领域，主要是因为开发治疗癌症新药的需求不断增加。杂化化合物中的查尔酮和1,2,3 - 三唑环最近已成为开发新型抗癌药物的一种有前景的策略。以其稳定性和氢键结合能力而闻名的1,2,3 - 三唑环增强了这些杂化物与靶点的结合亲和力。查尔酮具有对其抗癌活性至关重要的α,β - 不饱和羰基体系。这两个部分的协同作用产生了具有强大抗癌特性的化合物。本综述探讨了构效关系研究，这些研究表明查尔酮苯环上取代基的电子和亲脂性性质显著影响其抗癌活性。供电子基团和吸电子基团会影响细胞摄取和与靶点的结合。在1,2,3 - 三唑环中引入各种取代基可以提高对特定癌细胞系的选择性和效力。这些杂化物通常通过诱导凋亡和破坏细胞周期发挥其抗癌作用。最近的研究表明，1,2,3 - 三唑查尔酮杂化物作为抗癌药物具有治疗前景。通过构效关系研究和深入的机制研究进行进一步优化，可能会开发出毒性最小的高效且选择性的抗癌药物。
