405224-23-9Relevant articles and documents
Pyrazolopyridine hydroxamic acid compound as well as preparation method and application thereof
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, (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.
Discovery of novel CDK inhibitors via scaffold hopping from CAN508
Jing, Liandong,Tang, Yanbo,Xiao, Zhiyan
, p. 1386 - 1391 (2018/03/21)
Cyclin-dependent kinases (CDKs) are promising drug targets for various human diseases, especially for cancers. Scaffold hopping strategy was applied on CAN508, a known selective CDK9 inhibitor, and a series of pyrazolo[3,4-b]pyridine compounds were synthe
Design and synthesis of novel substituted naphthyridines as potential c-Met kinase inhibitors based on MK-2461
Wu, Jing-Fang,Liu, Ming-Ming,Huang, Shao-Xu,Wang, Yang
supporting information, p. 3251 - 3255 (2015/07/08)
Abstract Two series of novel 1,5-naphthyridine and 1,6-naphthyridine derivatives were designed and synthesized based on the c-Met kinase inhibitor MK-2461 under the guidance of scaffold hopping strategy. All were tested on c-Met kinase and in vitro anti-tumor activities against Hela and A549 cell lines. The results indicated that 1,6-naphthyridine was a more promising c-Met inhibitory structure core compared with 1,5-naphthyridine. Among them, 26b and 26c showed the best enzymic and cytotoxic activities. The western blot experiments implied that the cytotoxic activity of 26c might be partially through suppressing the phosphorylation of c-Met kinase.
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYSNTHESIS FOR BACTERIAL INFECTIONS
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, (2014/09/16)
The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial FabI and can be used for the treatment of Staphylococcal infections.
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.
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYNTHESIS FOR BACTERIAL INFECTIONS
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, (2013/04/10)
The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial Fab I and can be used for the treatment of Staphylococcal infections.
A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway
Huart, Anne-Sophie,Saxty, Barbara,Merritt, Andy,Nekulova, Marta,Lewis, Stephen,Huang, Yide,Vojtesek, Borivoj,Kettleborough, Catherine,Hupp, Ted R.
, p. 5578 - 5585 (2013/10/01)
Reactivation of the wild-type p53 pathway is one key goal aimed at developing targeted therapeutics in the cancer research field. Although most p53 protein kinases form 'p53-activating' signals, there are few kinases whose action can contribute to the inhibition of p53, as Casein kinase 1 (CK1) and Checkpoint kinase 1 (CHK1). Here we report on a pyrazolo-pyridine analogue showing activity against both CK1 and CHK1 kinases that lead to p53 pathway stabilisation, thus having pharmacological similarities to the p53-activator Nutlin-3. These data demonstrate the emerging potential utility of multivalent kinase inhibitors.
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5
Zhang, Peng,Zou, Mu-Fa,Rodriguez, Alice L.,Jeffrey Conn,Newman, Amy Hauck
experimental part, p. 3026 - 3035 (2010/07/06)
The metabotropic glutamate receptor subtype 5 (mGluR5) has been implicated in numerous neuropsychiatric disorders including addiction. We have discovered that the rigid diaryl alkyne template, derived from the potent and selective noncompetitive mGluR5 antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP), can serve to guide the design of novel quinoline analogues and pharmacophore optimization has resulted in potent mGluR5 noncompetitive antagonists (EC50 range 60-100 nM) in the quinoline series.
Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors
Shi, Jianyou,Xu, Guobin,Zhu, Wei,Ye, Haoyu,Yang, Shengyong,Luo, Youfu,Han, Jing,Yang, Jincheng,Li, Rui,Wei, Yuquan,Chen, Lijuan
supporting information; experimental part, p. 4273 - 4278 (2010/09/04)
Two series of 3-aminopyrazole compounds including 24 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and 16 pyrazolo[3,4-b]pyridines were synthesized and evaluated against HCT116, A549, and A2780 tumor cell lines. Among them, three compounds were found to have the ideal anti-proliferative activities in vitro. Docking experiments showed that the novel pyrazolo[3,4-b]pyridines share the similar interaction mode with Aurora-A kinase as PHA739358.
2-Amino-5-aryl-pyridines as selective CB2 agonists: Synthesis and investigation of structure-activity relationships
Gleave, Robert J.,Beswick, Paul J.,Brown, Andrew J.,Giblin, Gerard M.P.,Haslam, Carl P.,Livermore, David,Moses, Andrew,Nicholson, Neville H.,Page, Lee W.,Slingsby, Brian,Swarbrick, Martin E.
scheme or table, p. 6578 - 6581 (2010/06/12)
2-Amino-5-aryl-pyridines, exemplified by compound 1, had been identified as a synthetically tractable series of CB2 agonists from a high-throughput screen of the GlaxoSmithKline compound collection. Described herein are the results of an investigation of the structure-activity relationships (SAR) which led to the identification a number of potent and selective agonists.