199865-36-6Relevant academic research and scientific papers
Synthesis of aminopyrimidylindoles structurally related to meridianins
Rossignol, Emilie,Youssef, Ali,Moreau, Pascale,Prudhomme, Michelle,Anizon, Fabrice
, p. 10169 - 10176 (2007)
The synthesis of new meridianin derivatives substituted at the C-5′ position of the 2-aminopyrimidine ring by various aryl groups and substituted or not by a methyl group on the indole nitrogen is described. The 2-aminopyrimidine ring was obtained via a B
Discovery of N-(4-(3-isopropyl-2-methyl-2 H-indazol-5-yl)pyrimidin-2-yl)-4-(4-methylpiperazin-1-yl)quinazolin-7-amine as a Novel, Potent, and Oral Cyclin-Dependent Kinase Inhibitor against Haematological Malignancies
Huang, Jianhang,Wang, Xinren,Dong, Ruinan,Liu, Xiaoyue,Li, Hongmei,Zhang, Tianyi,Xu, Junyu,Liu, Chenhe,Zhang, Yanmin,Hou, Shaohua,Tang, Weifang,Lu, Tao,Chen, Yadong
, p. 12548 - 12571 (2021/09/11)
Hematologic malignancies (HM) start in blood forming tissue or in the cells of the immune system. Cyclin-dependent kinases (CDKs) regulate cell cycle progression, and some of them control cellular transcription. CDK inhibition can trigger apoptosis and could be particularly useful in hematological malignancies. Herein, we describe our efforts toward the discovery of a novel series of quinazoline derivatives as CDK inhibitors. Intensive structural modifications lead to the identification of compound 37d as the most active inhibitors of CDKs 1, 2, 4, 8 and 9 with balancing potency and selectivity against CDKs. Further biological studies revealed that compound 37d can arrest the cell cycle and induce apoptosis via activating PARP and caspase 3. More importantly, compound 37d showed good antitumor efficacy in multiple HM mice xenograft models with no obvious toxicity. These results indicated that CDK 1, 2, 4, 8, and 9 inhibitors could be potentially used to treat certain hematologic malignancies.
4-(1-methylindole-3-yl) pyrimidine derivative and application thereof
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Paragraph 0134-0136, (2021/10/30)
A series of 4-(1-methylindole-3-yl) pyrimidine derivatives are prepared through reasonable design by taking 4-indolyl-2-arylaminopyrimidine as a skeleton, an in-vitro anti-inflammatory activity test result shows that most of the compounds have relatively high inhibition capability on inflammatory cytokines IL-6 and IL-8, and an experimental result shows that most of the compounds have different degrees of inhibition effects on IL-6 and IL-8 induced by LPS, and the inhibition effects are basically superior to that of 4-indolyl-2-aminopyrimidine. The invention provides a certain research basis for further obtaining anti-ALI micromolecules with high anti-inflammatory activity and high bioavailability.
Preparation method for osimertinib mesylate
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Paragraph 0013; 0014, (2018/04/28)
The invention discloses a preparation method for osimertinib mesylate. The chemical name of osimertinib mesylate is N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide mesylate (AZD9291), and the chemical formula is C28H33N7O2.CH4O3S. The process of the preparation technique of the preparation method is simple, materials areeasy to obtain, and the preparation method is cost-efficient and environment-friendly, can help realize industrialization, can promote the economic and technological development of osimertinib activeingredients, reduces production cost, and is suitable for mass production.
Consecutive three-component synthesis of ynones by decarbonylative sonogashira coupling
Merkul, Eugen,Oeser, Thomas,Mueller, Thomas J.J.
supporting information; experimental part, p. 5006 - 5011 (2009/12/07)
A study was conducted to demonstrate consecutive three-component synthesis of ynones by decarbonylative Sonogashira coupling. Sonogashira coupling started from electron-rich heterocycles and oxalyl chloride as a source of the CO building block via interme
Towards the syntheses of N-H and N-alkylated derivatives of meridianins
Simon, Ga?lle,Couthon-Gourves, Hélène,Haelters, Jean-Pierre,Corbel, Bernard,Kervarec, Nelly,Michaud, Fran?ois,Meijer, Laurent
, p. 793 - 801 (2008/03/29)
(Chemical Equation Presented) Novel N-H and N-alkylated derivatives of meridianins have been synthesized as potential antitumor agents by a two-step conversion of N-tosyl-3-acetylindoles or N-alkyl-3-acetylindoles to the corresponding enaminones using DMF-DMA, with or without added pyrrolidine. Further cyclization with guanidine gave the corresponding 2-aminopyrimidines. The structures of the compounds, thus obtained, were proved by 1H and 13C NMR spectroscopy, NOE experiments and X-ray analysis.
ARYL PYRIMIDINE DERIVATIVES
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Page/Page column 32, (2010/10/20)
The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT2B-antagonists. The invention is also directed to formulations and methods for t
