876126-60-2Relevant articles and documents
Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors
Hu, Rong,Liu, Zhi-Hao,Shi, Yao-Jie,Wang, Ning-Yu,Wang, Wan-Li,Xiao, Kun-Jie,Xu, Ying,Yu, Luo-Ting,Zhu, Yong-Xia,Zuo, Wei-Qiong
, (2020/02/26)
Protein kinase inhibitors and epigenetic regulatory molecules are two main kinds of anticancer drugs developed in recent years. Both kinds of drugs harbor their own advantages and disadvantages in the treatment of cancer, and the development of small mole
POTENT DUAL BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
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Page/Page column 128-129, (2016/04/26)
Disclosed herein are compounds that are inhibitors of BRD4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BRD4 are also disclosed. In certain aspects, disclosed are compounds of Formula I-IV.
Synthesis and biological evaluation of 2,4-diaminopyrimidines as selective Aurora A kinase inhibitors
Qin, Wen-Wen,Sang, Chun-Yan,Zhang, Lin-Lin,Wei, Wei,Tian, Heng-Zhi,Liu, Huan-Xiang,Chen, Shi-Wu,Hui, Ling
, p. 174 - 184 (2015/03/31)
The Aurora kinases are a family of serine/threonine kinases that interact with components of the mitotic apparatus and serve as potential therapeutic targets in oncology. Here we synthesized 15 2,4-diaminopyrimidines and evaluated their biological activities, including antiproliferation, inhibition against Aurora kinases and cell cycle effects. These compounds generally exhibited more potent cytotoxicity against tumor cell lines compared with the VX-680 control, especially compound 11c, which showed the highest cytotoxicities, with IC50 values of 0.5-4.0 1/4M. Compound 11c had more than 35-fold more selectivity for Aurora A over Aurora B, and molecular docking analysis indicated that compound 11c form better interaction with Aurora A both from the perspective of structure and energy. Furthermore, compound 11c induced G2/M cell cycle arrest in HeLa cells. This series of compounds has the potential for further development as selective Aurora A inhibitors for anticancer activity.