394248-99-8Relevant academic research and scientific papers
COMPOUNDS AND THEIR USES AS SPLEEN TYROSINE KINASE INHIBITORS
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Paragraph 0113, (2021/12/28)
Provided are compounds of Formula (I) which can be used as Syk inhibitors and potently as therapeutic agents against diseases mediated by Syk.
Discovery of benzo[d]oxazole derivatives as the potent type-I FLT3-ITD inhibitors
Bao, Jiyin,Liu, Haichun,Zhi, Yanle,Yang, Wenqianzi,Zhang, Jiawei,Lu, Tao,Wang, Yue,Lu, Shuai
, (2019/09/30)
Fms-like tyrosine kinase 3 (FLT3) has been considered as a potential drug target for the treatment of acute myeloid leukemia (AML), because of its high and aberrant expression in AML patients, especially the patients with FLT3-ITD mutation. Initiating from a hit compound (IC50: 500 nM against FLT3-ITD), a series of compounds were designed and synthesized based on benzo[d]oxazole-2-amine scaffold to discover new potent FLT3-ITD inhibitors. During the medicinal chemistry works, flexible molecular docking was used to provide design rationale and study the binding modes of the target compounds. Through the mixed SAR exploration based on the enzymatic and cellular activities, compound T24 was identified with potent FLT3-ITD inhibitory (IC50: 0.41 nM) and anti-proliferative (IC50: 0.037 μM against MV4-11 cells) activities. And the binding mode of T24 with “DFG-in” FLT3 was simulated by a 20-ns molecular dynamics run, providing some insights into further medicinal chemistry efforts toward novel FLT3 inhibitors in AML therapy.
Pyrrolopyrimidine compound, pharmaceutical composition containing thereof, and preparation method and applications
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Paragraph 0231-0235, (2019/11/29)
The invention relates to a pyrrolopyrimidine compound represented by formula I, a pharmaceutical composition containing thereof, and a preparation method and applications in preventing or treating Weel protein kinase related diseases.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 0574-0576, (2019/04/25)
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849
Witty, David R.,Bateson, John,Hervieu, Guillaume J.,Al-Barazanji, Kamal,Jeffrey, Phillip,Hamprecht, Dieter,Haynes, Andrea,Johnson, Christopher N.,Muir, Alison I.,O'Hanlon, Peter J.,Stemp, Geoffrey,Stevens, Alex J.,Thewlis, Kevin,Winborn, Kim Y.
, p. 4872 - 4878 (2007/10/03)
A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.
