(2E,4E,6R)-N-[tert-Butyl(Dimethyl)Silyl]Oxy-7-[4-(Dimethylamino)Phenyl]-4,6-Dimethyl-7-Oxohepta-2,4-Dienamide置于甲醇,Cesium Fluoride体系中,化学反应 3.0H,反应生成 曲古柳菌素a 参考文献:Synthesis Of Hdac Inhibitors: Trichostatin A And Analogues 标题:Synthesis Of Hdac Inhibitors: Trichostatin A And Analogues 摘要:本文涉及组蛋白去乙酰化酶(hdacs)和hdac抑制剂,如三氯乙酸(tsa)及其类似物.实施例提供了合成tsa和tsa类似物的简单方法.这些方法提供了合成tsa和tsa类似物的途径,使得生产hdac抑制剂的成本更低,数量更大,比以往更容易获得.
专利号:US-5993845-A 优先权日:1996-09-04 标题:Anti-fibrotic medicament 发明人:GEERTS ALBERT EMMANUEL CORNEIL; NIKI TOSHIRO 权利人:UNIV BRUXELLES 摘要:Compounds of submicromolar concentrations of a histone deacetylase inhibitor, useful as anti-fibrotic agents. The compounds strongly inhibit three main features of myofibroblastic differentiation of cultured hepatic stellate cells and of skin fibroblasts: (1) synthesis of collagens type I and III, the predominant collagens in fibrosis of liver and other organs; (2) cellular proliferation; and (3) expression of smooth muscle alpha -actin, a marker for activated myofibroblasts. Preferred compounds include trichostatin A or a pharmaceutically acceptable salt thereof, and sodium butyrate.
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合成参考文献
参考文献:10.1245/s10434-010-0956-9 摘要:Iwasaki Y, Sunaga N, Tomizawa Y, Imai H, Iijima H, Yanagitani N, Horiguchi K, Yamada M, Mori M. Epigenetic inactivation of the thyroid hormone receptor beta1 gene at 3p24.2 in lung cancer. Ann Surg Oncol. 2010 Aug;17(8):2222–8. doi: 10.1245/s10434-010-0956-9. 参考文献:10.1007/s11481-010-9192-0 摘要:Suh H, Choi S, Khattar P, Choi N, Lee SC. Histone Deacetylase Inhibitors Suppress the Expression of Inflammatory and Innate Immune Response Genes in Human Microglia and Astrocytes. Journal of Neuroimmune Pharmacology. 2010 Feb 17;5(4):521–32. doi: 10.1007/s11481-010-9192-0. 参考文献:10.1007/s12185-010-0517-9 摘要:Masui S. Pluripotency maintenance mechanism of embryonic stem cells and reprogramming. International Journal of Hematology. 2010 Feb 16;91(3):360–72. doi: 10.1007/s12185-010-0517-9. 参考文献:10.1186/1471-2180-10-49 摘要:Laskowski MC, Smulian AG. Insertional mutagenesis enables cleistothecial formation in a non-mating strain of Histoplasma capsulatum. BMC Microbiol. 2010 Feb 16;10():49.