📜Sodium (S)-2-(4-(4-((((3Z,6Z)-6-Benzylidene-3-((5-(Tert-Butyl)-1H-Imidazol-4-yl)Methylene)-5-Oxo-3,4,5,6-Tetrahydropyrazin-2-yl)Oxy)Methoxy)-4-Oxobutyl)-1H-1,2,3-Triazol-1-yl)Pentanedioate置于esterase Enzyme体系中,化学反应生成 (3Z,6Z)-3-[(5-叔丁基-1H-咪唑-4-基)亚甲基]-6-(苯亚甲基)-2,5-哌嗪二酮 参考文献: Plinabulin Prodrug Analogs And Therapeutic Uses Thereof[fr] Analogues De Promédicaments à Base De Plinabuline Et Utilisations Thérapeutiques Associées 标题: Plinabulin Prodrug Analogs And Therapeutic Uses Thereof[fr] Analogues De Promédicaments à Base De Plinabuline Et Utilisations Thérapeutiques Associées 摘要:公开了式(i)和(i')的化合物,以及制备这些化合物的方法.还公开了用于治疗包括癌症和与血管增殖相关的非癌症疾病的组合物和方法.(式(i)和(i'))
专利号:US-7935704-B2 优先权日:2003-08-01 标 题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 发明人:PALLADINO MICHAEL A; LLOYD GEORGE KENNETH; HAYASHI YOSHIO; NICHOLSON BENJAMIN 权利人:NEREUS PHARMACEUTICALS INC 摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ″, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.
专利号:US-7956058-B2 优先权日:2002-08-02 标 题:Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof 发明人:HAYASHI YOSHIO; PALLADINO JR MICHAEL A; GRODBERG JENNIFER 权利人:NEREUS PHARMACEUTICALS INC 摘要:Compounds represented by the following structure (I) are disclosed: n nas are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ′, R 1 ′, R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.
专利号:US-10434098-B2 优先权日:2015-06-02 标 题 :Deuterated dehydrophenylahistin compounds and preparation method thereof and use thereof in preparation of anti-tumor drugs 发明人:LI WENBAO; SUN TIANWEN; WANG SHIXIAO; ZHAO JIANCHUN; CAI BING; GUAN HUASHI 权利人:MARINE BIOMEDICAL RES INST QINGDAO CO LTD 摘要:Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehydrophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound.
专利号:US-2005197344-A1 优先权日:2003-08-01 标题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
专利号:US-2006223823-A1 优先权日:2002-08-02 标 题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
专利号:US-2006217553-A1 优先权日:2002-08-02 标 题 :Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
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合成参考文献
参考文献:10.2174/138945011798829366 摘要:Spear MA, LoRusso P, Mita A, Mita M. Vascular disrupting agents (VDA) in oncology: advancing towards new therapeutic paradigms in the clinic. Curr Drug Targets. 2011 Dec;12(14):2009–15. doi: 10.2174/138945011798829366.