4010-81-5Relevant articles and documents
High yielding, base catalyzed C6 regioselective amination and N9 alkylation in purine nucleotide
Dhuda, Gautamkumar,Kapadiya, Khushal,Ladwa, Paresh,Godhaniya, Bhavna,Modha, Jayesh
, p. 2871 - 2874 (2019)
2,6-Dichloropurine is an interesting new nucleoside which gave regioselectively various 2-derivatized or 6-derivatized purines by using a secondary amines. An efficient, simple and regioselective synthesis of C6 morpholine, N9 alkylated purine nucleoside derivatives were attained via chloro-amine coupling reaction between 2,6-dichloropurine with morpholine followed by commercial alkylation method using DMF and K2CO3. Over the traditionally used protocols and procedure, it have been exhibited advance benefits such as admirable yield, simple reaction conditions and modest influence.
DUAL KINASE-BROMODOMAIN INHIBITORS
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Page/Page column 106; 213, (2021/12/12)
Provided herein are compounds of Formula (I) that are dual inhibitors of kinases and bromo-domain proteins. The disclosure also relates to pharmaceutical compositions containing such compounds, methods for using such compounds in the treatment of cancers, particularly, the treatment of multiple myeloma cancers, and to related uses.
PURINES AND METHODS OF THEIR USE
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Page/Page column 65-66, (2021/12/28)
Disclosed are compounds useful in the treatment of neurological disorders. The compounds described herein, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological diseases.
Identification of a potent and selective phosphatidylinositol 3-kinase δ inhibitor for the treatment of non-Hodgkin's lymphoma
Zuo, Wei-Qiong,Hu, Rong,Wang, Wan-Li,Zhu, Yong-Xia,Xu, Ying,Yu, Luo-Ting,Liu, Zhi-Hao,Wang, Ning-Yu
, (2020/10/23)
PI3Kδ has proved to be an effective target for anti-lymphoma drugs. However, the application of current approved PI3Kδ inhibitors has been greatly limited due to their specific immune-mediated toxicity and increased risk of infection, it is necessary to develop more PI3Kδ inhibitors with new scaffold. In this study, SAR study with respect to piperazinone-containing purine derivatives led to the discovery of a potent and selective PI3Kδ inhibitor, 4-(cyclobutanecarbonyl)-1-((2-(2-ethyl-1H-benzo[d]imidazol-1-yl)-9-methyl-6-morpholino-9H-purin-8-yl)methyl)piperazin-2-one (WNY1613). WNY1613 exhibits good antiproliferative activity against a panel of non-Hodgkin's lymphoma (NHL) cell lines by inducing cancer cell apoptosis and inhibiting the phosphorylation of PI3K and MAPK downstream components. In addition, it can also prevent the tumor growth in both SU-DHL-6 and JEKO-1 xenograft models without observable toxicity. WNY1613 thus could be developed as a promising candidate for the treatment of NHL after subsequent extensive pharmacodynamics and pharmacokinetics investigation.