71198-37-3Relevant academic research and scientific papers
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
One-Pot Evolution of Ageladine A through a Bio-Inspired Cascade towards Selective Modulators of Neuronal Differentiation
Iwata, Takayuki,Otsuka, Satoshi,Tsubokura, Kazuki,Kurbangalieva, Almira,Arai, Daisuke,Fukase, Koichi,Nakao, Yoichi,Tanaka, Katsunori
, p. 14707 - 14716 (2016/10/03)
A bio-inspired cascade reaction has been developed for the construction of the marine natural product ageladine A and a de novo array of its N1-substituted derivatives. This cascade features a 2-aminoimidazole formation that is modeled after an arginine post-translational modification and an aza-electrocyclization. It can be effectively carried out in a one-pot procedure from simple anilines or guanidines, leading to structural analogues of ageladine A that had been otherwise synthetically inaccessible. We found that some compounds out of this structurally novel library show a significant activity in modulating the neural differentiation. Namely, these compounds selectively activate or inhibit the differentiation of neural stem cells to neurons, while being negligible in the differentiation to astrocytes. This study represents a successful case in which the native biofunction of a natural product could be altered by structural modifications.
Heterocyclic compounds useful for kinase inhibition
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Page/Page column 97, (2016/04/02)
Provided herein are compounds useful for kinase inhibition.
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.
