Junaid Ahmad, Lim Felicia Phei Lin, Tiekink Edward R T, Dolzhenko Anton V
School of Pharmacy, Monash University Malaysia Jalan Lagoon Selatan Bandar Sunway Selangor Darul Ehsan 47500 Malaysia
Research Centre for Crystalline Materials, School of Science and Technology, Sunway University 5 Jalan Universiti Bandar Sunway Selangor Darul Ehsan 47500 Malaysia.
RSC Adv. 2020 Jul 6;10(43):25517-25528. doi: 10.1039/d0ra04970k. eCollection 2020 Jul 3.
New 6, -diaryl-1,3,5-triazine-2,4-diamines were designed using the 3D-QSAR model developed earlier. These compounds were prepared and their antiproliferative activity was evaluated against three breast cancer cell lines (MDA-MB231, SKBR-3 and MCF-7) and non-cancerous MCF-10A epithelial breast cells. The synthesized compounds demonstrated selective antiproliferative activity against triple negative MDA-MB231 breast cancer cells. The most active compound in the series inhibited MDA-MB231 breast cancer cell growth with a GI value of 1 nM. None of the tested compounds significantly affected the growth of the normal breast cells. The time-dependent cytotoxic effect, observed when cytotoxicity was assessed at different time intervals after the treatment, and morphological features, observed in the fluorescence microscopy and live cell imaging experiments, suggested apoptosis as the main pathway for the antiproliferative activity of these compounds against MDA-MB231 cells.
利用先前开发的3D-QSAR模型设计了新型6, -二芳基-1,3,5-三嗪-2,4-二胺。制备了这些化合物，并评估了它们对三种乳腺癌细胞系（MDA-MB231、SKBR-3和MCF-7）以及非癌性MCF-10A乳腺上皮细胞的抗增殖活性。合成的化合物对三阴性MDA-MB231乳腺癌细胞表现出选择性抗增殖活性。该系列中最具活性的化合物抑制MDA-MB231乳腺癌细胞生长的GI值为1 nM。所测试的化合物均未显著影响正常乳腺细胞的生长。在处理后的不同时间间隔评估细胞毒性时观察到的时间依赖性细胞毒性效应，以及在荧光显微镜和活细胞成像实验中观察到的形态学特征，表明凋亡是这些化合物对MDA-MB231细胞抗增殖活性的主要途径。
