Tang Lin, Chen Tingting, Yang Hongpeng, Wen Xiaoxue, Sun Yunbo, Liu Shuchen, Peng Tao, Zhang Shouguo, Wang Lin
Beijing Institute of Radiation Medicine Beijing 100850 P. R. China
Faculty of Environment & Life, Beijing University of Technology Beijing 100124 P. R. China.
RSC Adv. 2021 Nov 22;11(59):37462-37471. doi: 10.1039/d1ra05226h. eCollection 2021 Nov 17.
In this work, a series of novel benzyl naphthyl sulfoxides/sulfones derived from Rigosertib were designed and synthesized as potential antitumor agents. The cytotoxicity against four human cancer cell lines (HeLa, MCF-7, HepG2 and SCC-15) and two normal human cell lines (HUVEC and 293T) indicated that some of the sulfones and sulfoxides possessed potent antineoplastic activity that reached nanomolar levels and relatively low toxicity to normal cells. Among them, (2-methoxy-5-((naphthalen-2-ylsulfonyl)methyl)phenyl)glycine (15b) was found to be a promising antitumor drug candidate that could significantly inhibit tumor cell migration and induce tumor cell apoptosis the p53-Bcl-2-Bax signaling pathway at nanomolar concentrations.
在本研究中，设计并合成了一系列源自瑞戈非尼的新型苄基萘基亚砜/砜类化合物作为潜在的抗肿瘤药物。对四种人类癌细胞系（HeLa、MCF-7、HepG2和SCC-15）和两种正常人类细胞系（HUVEC和293T）的细胞毒性表明，一些砜类和亚砜类化合物具有强大的抗肿瘤活性，达到纳摩尔水平，且对正常细胞毒性相对较低。其中，（2-甲氧基-5-（（萘-2-基磺酰基）甲基）苯基）甘氨酸（15b）被发现是一种有前景的抗肿瘤药物候选物，它能在纳摩尔浓度下显著抑制肿瘤细胞迁移并通过p53-Bcl-2-Bax信号通路诱导肿瘤细胞凋亡。
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