School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, Selangor Darul Ehsan, 47500, Malaysia.
School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, Selangor Darul Ehsan, 47500, Malaysia; Curtin Medical School, Curtin Health Innovation Research Institute, Faculty of Health Sciences, Curtin University, GPO Box U1987 Perth, Western, Bentley, 6845, Australia.
Eur J Med Chem. 2024 Oct 5;276:116680. doi: 10.1016/j.ejmech.2024.116680. Epub 2024 Jul 16.
1,3,5-Triazine scaffold has garnered considerable interest due to its wide-ranging pharmacological properties, particularly in the field of cancer research. Breast cancer is the most commonly diagnosed cancer among women. Approximately one in eight women will receive a diagnosis of invasive breast cancer during their lifetime. The five-year survival rate for invasive breast cancer is less than 30 %, indicating a need to develop a more effective therapeutic agent targeting breast cancer. This review discusses bioactive 1,3,5-triazines targeting breast cancer cells by the inhibition of different enzymes, which include PI3K, mTOR, EGFR, VEGFR, FAK, CDK, DHFR, DNA topoisomerase, ubiquitin-conjugating enzyme, carbonic anhydrase, and matrix metalloproteinase. The anticancer agent search in some drug discovery programs is based on compound screening for antiproliferative activity. Often, multiple targets contribute to the anticancer effect of 1,3,5-triazines and this approach allows identification of active molecules prior to identification of their targets.
1,3,5-三嗪支架由于其广泛的药理特性而引起了相当大的关注，特别是在癌症研究领域。乳腺癌是女性中最常见的癌症。大约每 8 名女性中就有 1 人在其一生中被诊断患有浸润性乳腺癌。浸润性乳腺癌的 5 年生存率不到 30%，这表明需要开发针对乳腺癌的更有效的治疗药物。这篇综述讨论了通过抑制不同酶（包括 PI3K、mTOR、EGFR、VEGFR、FAK、CDK、DHFR、DNA 拓扑异构酶、泛素连接酶、碳酸酐酶和基质金属蛋白酶）来靶向乳腺癌细胞的生物活性 1,3,5-三嗪。一些药物发现计划中的抗癌药物搜索是基于化合物筛选抗增殖活性。通常，多种靶标有助于 1,3,5-三嗪的抗癌作用，这种方法允许在鉴定其靶标之前鉴定活性分子。
