Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs.
Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs.
复制标题
新型1,6-二芳基吡啶-2(1H)-酮类似物的合成和生物学评价。
DOI：
10.1016/j.ejmech.2013.04.008
复制
发表时间：
2013
影响因子：
6.7
通讯作者：
Wei Lu
中科院分区：
文献类型：
--
作者：
Taijie Chen;Yu Luo;Youhong Hu;Bo Yang;Wei Lu
通过Chan-Lam和Suzuki连续偶联，设计并合成了一系列1,6-二芳基吡啶-2(1H)- 1类似物。这些新化合物对两种肿瘤细胞系（SKOV-3和HepG2）的抗增殖活性进行了评估。化合物1b、1c、1e和1f的体外细胞毒性与紫杉醇相当，但其体内抗肿瘤活性低于紫杉醇。此外，细胞周期实验表明，这些1,6-二芳基吡啶-2(1H)- 1化合物诱导HepG2细胞株的细胞周期阻滞在G1/M期。
A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan–Lam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.