95907-03-2Relevant articles and documents
Pyrazolopyridine hydroxamic acid compound as well as preparation method and application thereof
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Paragraph 0030; 0034-0036, (2021/09/01)
The invention relates to the technical field of chemical synthesis, in particular to a pyrazolopyridine hydroxamic acid compound as well as a preparation method and application thereof. The pyrazolopyridine hydroxamic acid compound comprises a compound as shown in a formula (1), an isomer thereof, and a hydrate thereof or a pharmaceutically acceptable salt thereof, wherein n is an integer, and R is any one of a substituted or unsubstituted aromatic ring group and a substituted alkyl group. The compound can well inhibit cancer cell proliferation, and then has an excellent treatment effect on tumors.
A high-yielding method for the preparation of isoxazolopyridin-3-amine derivatives
Yu, Wensheng,Bulger, Paul G.,Maloney, Kevin M.
, p. 4941 - 4946 (2016/10/12)
A highly efficient and green method has been developed for the rapid preparation of highly functionalized isoxazolopyridin-3-amine derivatives in excellent yields. This process has a broad substrate scope, is operationally simple, and generally requires no chromatographic purification. In addition, the process is scalable and significantly greener than current alternatives with a PMI of 18 and water as the reaction solvent.
Discovery of dual death-associated protein related apoptosis inducing protein kinase 1 and 2 inhibitors by a scaffold hopping approach
Gao, Ling-Jie,Kovackova, Sona,?ála, Michal,Ramadori, Anna Teresa,De Jonghe, Steven,Herdewijn, Piet
, p. 7624 - 7643 (2015/01/08)
DRAK2 emerged as a promising drug target for the treatment of autoimmune diseases and to prevent graft rejection after organ transplantation. Screening of a compound library in a DRAK2 binding assay led to the identification of an isothiazolo[5,4-b]pyridine derivative as a novel ligand for DRAK2, displaying a Kdvalue of 1.6 μM. Subsequent medicinal chemistry work led to the discovery of a thieno[2,3-b]pyridine derivative with strong DRAK2 binding affinity (Kd= 9 nM). Moreover, this compound also behaves as a functional inhibitor of DRAK2 enzymatic activity, displaying an IC50value of 0.82 μM, although lacking selectivity, when tested against DRAK1. This paper describes for the first time functionally active dual DRAK1 and DRAK2 inhibitors that can be used as starting point for the synthesis of chemical tool compounds to study DRAK1 and DRAK2 biology, or they can be considered as hit compounds for hit-to-lead optimization campaigns in drug discovery programs.