113136-80-4Relevant academic research and scientific papers
NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS
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Page/Page column 127; 128, (2020/10/09)
The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis
Huang, Zhi,Zhao,Qin, Zhongxiang,Li, Yongtao,Wang, Tianqi,Zhou, Wei,Zheng, Jianyu,Yang, Shengyong,Shi, Yi,Fan, Yan,Xiang, Rong
, (2019/08/07)
Based on the significantly synergistic effects of CDK4 and VEGFR2 inhibitors on growth of cancer cells, a series of novel multi-kinase inhibitors targeting CDK4 and VEGFR2 were designed, synthesized and evaluated, among which Roxyl-ZV-5J exhibited potent and balanced activities against both CDK4 and VEGFR2 with half-maximal inhibitory concentration at the nanomolar level. It effectively induced breast and cervical cancer cell cycle arrest and cell apoptosis. Roxyl-ZV-5J also inhibited the proliferation, tube formation and VEGFR2 downstream signaling pathways of HUVECs. Oral administration of Roxyl-ZV-5J led to significant tumor regression and anti-angiogenesis without obvious toxicity in SiHa xenograft mouse model. In addition, this compound showed good pharmacokinetics. This study confirmed a new tool for dual CDK-VEGFR2 pathways inhibition achieved with a single molecule, which provided valuable leads for further structural optimization and anti-angiogenesis and anti-tumor mechanism study.
Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate
Li, Yongtao,Guo, Qingxiang,Zhang, Chao,Huang, Zhi,Wang, Tianqi,Wang, Xin,Wang, Xiang,Xu, Guangwei,Liu, Yanhua,Yang, Shengyong,Fan, Yan,Xiang, Rong
supporting information, p. 3231 - 3237 (2017/07/07)
A series of novel hybrid structure derivatives, containing both LEE011 and Cabozantinib pharmacophore, were designed, synthesized and evaluated. Surprisingly, a compound 4d was discovered that highly exhibited effective and selective activity of CDK9 inhi
Discovery of anilinopyrimidines as dual inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and cellular activity
Zhan, Zhengsheng,Ai, Jing,Liu, Qiufeng,Ji, Yinchun,Chen, Tiantian,Xu, Yechun,Geng, Meiyu,Duan, Wenhu
, p. 673 - 678 (2014/07/07)
Both c-Met and VEGFR-2 are important targets for cancer therapies. Here we report a series of potent dual c-Met and VEGFR-2 inhibitors bearing an anilinopyrimidine scaffold. Two novel synthetic protocols were employed for rapid analoguing of the designed
