- CDI-mediated monoacylation of symmetrical diamines and selective acylation of primary amines of unsymmetrical diamines
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A highly efficient and green protocol for monoacylation of symmetrical diamines and chemoselective acylation of primary amines of unsymmetrical diamines has been developed.
- Verma, Sanjeev K.,Ghorpade, Ramarao,Pratap, Ajay,Kaushik
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- Synthesis of Dithiolethiones and Identification of Potential Neuroprotective Agents via Activation of Nrf2-Driven Antioxidant Enzymes
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Oxidative stress is implicated in the pathogenesis of a wide variety of neurodegenerative disorders, and accordingly, dietary supplement of exogenous antioxidants or/and upregulation of the endogenous antioxidant defense system are promising for therapeutic intervention or chemoprevention of neurodegenerative diseases. Nrf2, a master regulator of the cellular antioxidant machinery, cardinally participates in the transcription of cytoprotective genes against oxidative/electrophilic stresses. Herein, we report the synthesis of 59 structurally diverse dithiolethiones and evaluation of their neuroprotection against 6-hydroxydopamine-or H2O2-induced oxidative damages in PC12 cells, a neuron-like rat pheochromocytoma cell line. Initial screening identified compounds 10 and 11 having low cytotoxicity but conferring remarkable protection on PC12 cells from oxidative-mediated damages. Further studies demonstrated that both compounds upregulated a battery of antioxidant genes as well as corresponding genes' products. Significantly, silence of Nrf2 expression abolishes cytoprotection of 10 and 11, indicating targeting Nrf2 activation is pivotal for their cellular functions. Taken together, the two lead compounds discovered here with potent neuroprotective functions against oxidative stress via Nrf2 activation merit further development as therapeutic or chemopreventive candidates for neurodegenerative disorders.
- Bai, Feifei,Fang, Jianguo,Song, Zi-Long,Zhang, Baoxin
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p. 2214 - 2231
(2020/03/06)
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- A N, 6 diphenyl pyrimidine -4 - amine Bcr - Abl inhibitor and its preparation method and application (by machine translation)
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The invention discloses a N, 6 diphenyl pyrimidine - 4 - amine Bcr - Abl inhibitor and its preparation method and application, the structural formula of the inhibitor for the wherein R is a single substituent or double-substituent, substituent is alkyl or halogen; R1 As a single substituent or double-substituent, substituent is alkyl or halogen. The series of inhibitors in vitro ABL1 kinase restraining effects, and can inhibit the proliferation of tumor cells, can be used for anti-tumor pharmaceutical preparation, in particular CML (chronic granulocytic leukemia) drug. The invention provides N, 6 diphenyl pyrimidine - 4 - amine Bcr - Abl inhibitor preparation method, raw materials are apt, mild reaction conditions, the reaction process is simple in operation, reagent used and cheap. (by machine translation)
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Paragraph 0041; 0049-0050; 0066
(2017/04/28)
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