在 Human Protease Plasmin体系中,用 Various Solvent(S) 用作溶剂,化学反应生成盐酸多柔比星 参考文献:可激活的抗癌前药中的延长的多个电子级联和环化间隔系统,可增强药物释放. 标题:可激活的抗癌前药中的延长的多个电子级联和环化间隔系统,可增强药物释放. 摘要:描述和设计了几种新颖的用于前药的自消除间隔基系统.这些细长的间隔物系统可以结合在可裂解的指定分子和母体药物之间.合成了含萘和联苯的间隔基,但没有消除.据报道,抗癌药阿霉素和紫杉醇的前药含有两个或三个电子级联间隔基.发现hobt的一种新型催化应用,用于使碳酸4-硝基苯基酯与苯胺衍生物反应,通过氨基甲酸酯键连接1,6-消除间隔基,从而合成n-芳基氨基甲酸酯.另外,合成了含有双间隔基的紫杉醇前药,其包含1,6-消除间隔基和经由2'-氨基甲酸酯键连接至紫杉醇的双胺连接基.与含有常规间隔物系统的前药相比,在特定的三肽指定剂与母体药物阿霉素或紫杉醇之间掺入了新型间隔物系统的前药被证明可以显着更快地被纤溶酶激活.预期本文报道的普遍适用的新型间隔物系统将有助于改进的酶活化前药的未来开发. Doi:10.1021/jo0158884
专利信息
专利号:US-4413120-A 优先权日:1981-04-06 标题:Process for producing acosamine, daunosamine, 1-thioacosamine and related compounds 发明人:WHISTLER ROY L 权利人:PURDUE RESEARCH FOUNDATION 摘要:A process for synthesizing acosamine, daunosamine and 1-thioacosamines from L-rhamnal is disclosed that can generally be characterized by Michael addition of an alkoxide or thioalkoxide to the enone formed by allylic oxidation of L-rhamnal to directly generate the 2-deoxy functionality, and stereospecific reduction of the oxime to the arabino compound which establishes configuration at C-3 and generates a compound which requires only epirmerization at C-4 to yield the desired product. The synthesis of anthracycline antibiotics incorporating these sugars or their derivatives by glycosidation of the glycone is also disclosed.
专利号:US-7659244-B2 优先权日:2003-11-03 标题:Rapamycin peptides conjugates: synthesis and uses thereof 发明人:SHARMA SANJAY K; WOO THOMAS; NAICKER SELVARAJ 权利人:QUEST PHARMATECH INC 摘要:The present invention relates to new rapamycin derivatives for the inhibition of cell proliferation. The compounds can advantageously target two proteins in dividing cells and interfere with cell cycle. There is thus provided derivatives of rapamycin in which the 42 position of rapamycin is linked to an amino acid or a peptide through a carbamate ester linkage. These rapamycin derivatives can be synthesized by reacting 42-O-(4-Nitrophenoxycarbonyl) rapamycin and an amino acid or a free amino peptide under basic conditions. These rapamycin derivatives can be used to inhibit the cell cycle and are therefore useful for treating cell proliferation disorders.
专利号:CN-102146108-B 优先权日:2011-01-14 标题 :Synthesis of 3′-azidoeprubicin with anticancer activity
专利号:EP-1384710-B1 优先权日:1995-11-27 标题 :Synthesis of heterocyclic compounds containing five- or six-membered rings
专利号:JP-4778405-B2 优先权日:1995-11-27 标题 :Method for the synthesis of target cytotoxic anthracycline analogues
专利号:ES-2310222-T3 优先权日:1995-11-27 标 题 :SYNTHESIS OF HETEROCICLIC COMPOUNDS CONTAINING FIVE RINGS OR SIX MEMBERS.
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