4431-64-5Relevant articles and documents
Discovery of CDK5 Inhibitors through Structure-Guided Approach
Khair, Nishat Z.,Lenjisa, Jimma L.,Tadesse, Solomon,Kumarasiri, Malika,Basnet, Sunita K. C.,Mekonnen, Laychiluh B.,Li, Manjun,Diab, Sarah,Sykes, Matthew J.,Albrecht, Hugo,Milne, Robert,Wang, Shudong
supporting information, p. 786 - 791 (2019/05/17)
Specific abrogation of cyclin-dependent kinase 5 (CDK5) activity has been validated as a viable approach for the development of anticancer agents. However, no selective CDK5 inhibitor has been reported to date. Herein, a structure-based in silico screenin
Benzene guanidine containing strong electron withdrawing group and preparation method of salt thereof
-
Paragraph 0028; 0029, (2017/07/19)
The invention discloses a benzene guanidine containing strong electron withdrawing group and preparation method of salt thereof. The benzene guanidine and the salt compound of the benzene guanidine can be applied as the accelerator of rubber, medicine int
Synthesis, structure-activity relationship and biological evaluation of 2,4,5-trisubstituted pyrimidine CDK inhibitors as potential anti-tumour agents
Shao, Hao,Shi, Shenhua,Foley, David W.,Lam, Frankie,Abbas, Abdullah Y.,Liu, Xiangrui,Huang, Shiliang,Jiang, Xiangrui,Baharin, Nadiah,Fischer, Peter M.,Wang, Shudong
, p. 447 - 455 (2013/11/19)
A series of 2,4,5-trisubstituted pyrimidines have been synthesised and characterised, which exhibited potent CDK inhibition and anti-proliferative activities. The structure-activity relationship is analysed and a rational for CDK9 selectivity is discussed
Identification of pyrimidine derivatives as hSMG-1 inhibitors
Gopalsamy, Ariamala,Shi, Mengxiao,Bennett, Eric M.,Bard, Joel,Zhang, Wei-Guo,Yu, Ker
, p. 6636 - 6641,6 (2012/12/12)
hSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. From our screening efforts, we have identified pyrimidine derivatives as hSMG-1 kinase inhibitors. We report structure-based optimization of this pan-kinase scaffold to improve its biochemical profile and overall kinome selectivity, including mTOR and CDK, to generate the first reported selective hSMG-1 tool compound.
PYRIMIDINES, TRIAZINES AND THEIR USE AS PHARMACEUTICAL AGENTS
-
Page/Page column 38, (2009/10/22)
A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X1 and X2 are one or two
