65356-50-5Relevant academic research and scientific papers
Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition
Ren, Shen-Zhen,Wang, Zhong-Chang,Zhu, Xiao-Hua,Zhu, Dan,Li, Zhang,Shen, Fa-Qian,Duan, Yong-Tao,Cao, Han,Zhao, Jing,Zhu, Hai-Liang
, p. 4264 - 4275 (2018/07/21)
The overexpress of COX-2 was clearly associated with carcinogenesis and COX-2 as a possible target has long been exploited for cancer therapy. In this work, we described the design and synthesis of a series of diarylpyrazole derivatives integrating with c
Design, synthesis and evaluation of benzenesulfonamide-substituted 1,5-diarylpyrazoles containing phenylacetohydrazide derivatives as COX-1/COX-2 agents against solid tumors
Lu, Xiao-Yuan,Wang, Zhong-Chang,Wei, Ting,Yan, Xiao-Qiang,Wang, Peng-Fei,Zhu, Hai-Liang
, p. 22917 - 22935 (2016/03/15)
Novel benzenesulfonamide-substituted 1,5-diarylpyrazoles containing phenylacetohydrazide derivatives have been designed, synthesized and evaluated for their biological activities as selective COX-2 inhibitors with anticancer potential. In vitro the bioass
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction
Zhuang, Chunlin,Miao, Zhenyuan,Zhu, Lingjian,Dong, Guoqiang,Guo, Zizhao,Wang, Shengzheng,Zhang, Yongqiang,Wu, Yuelin,Yao, Jianzhong,Sheng, Chunquan,Zhang, Wannian
, p. 9630 - 9642 (2013/01/16)
The p53-MDM2 interaction has been proved to be a valuable target to develop effective antitumor agents. Novel p53-MDM2 inhibitors bearing pyrrolidone scaffolds were successfully identified by structure-based design. The nanomolar inhibitor 5 possessed good p53-MDM2 inhibitory activity (Ki = 780 nM) due to its hydrophobic and hydrogen bonding interactions with MDM2. Further hit optimization led to the discovery of a number of highly potent pyrrolidone derivatives with improved p53-MDM2 inhibitory activity and in vitro antiproliferative potency. Compounds 41 (Ki = 260.0 nM) and 60a (Ki = 150.0 nM) showed good and selective activity against tumor cells with deleted p53. In addition, these two compounds also effectively inhibited the tumor growth in the A549 xenograft model. Interestingly, compound 41 was proved to be a potent MDM2/MDMX dual inhibitor. The novel pyrrolidone p53-MDM2 inhibitors represent promising lead structures for the development of novel antitumor agents.
