Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China.
Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China.
Eur J Med Chem. 2015;96:269-80. doi: 10.1016/j.ejmech.2015.04.027. Epub 2015 Apr 13.
Therapeutics of metastatic or triple-negative breast cancer are still challenging in clinical. Herein we demonstrated the design and optimization of a series of hybrid of 2,4-diaminopyrimidine and arylthiazole derivatives for their anti-proliferative properties against two breast cancer cell lines (MCF-7 as human breast cancer and MDA-MB-231 as triple-negative breast cancer). More importantly, some of those compounds with potent antiproliferative activities also indicated excellent inhibitory activities against MDA-MB-231 cell migration. These results suggested that the new series of hybridation of aryl-thiazoles and aminopyrimidines could be identified and developed as novel highly potential anticancer agents against the triple-negative breast cancer as well as metastatic one in the future.
转移性或三阴性乳腺癌的治疗仍然具有临床挑战性。在此，我们展示了一系列 2,4-二氨基嘧啶和芳基噻唑衍生物的设计和优化，以评估其对两种乳腺癌细胞系（MCF-7 作为人乳腺癌和 MDA-MB-231 作为三阴性乳腺癌）的抗增殖特性。更重要的是，一些具有强效增殖抑制活性的化合物对 MDA-MB-231 细胞迁移也表现出优异的抑制活性。这些结果表明，芳基噻唑和氨基嘧啶的新系列杂交物可以被鉴定和开发为新型高潜力的抗癌药物，用于未来的三阴性乳腺癌以及转移性乳腺癌。
