CAS: 56420-45-2; (8S,10S)-10-(((2R,4S,5R,6S)-4-Amino-5-Hydroxy-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)-6,8,11-Trihydroxy-8-(2-Hydroxyacetyl)-1-Methoxy-7,8,9,10-Tetrahydrotetracene-5,12-Dione

上下游产品

doxorubicin3'-N-(N'',N''-dimethylformamidinyl)-4'-epidoxorubicin N,N-dimethyl-4′-epi-doxorubicin N3'-acetyl-4'-epidoxorubicin

(8S,10S)-10-((2R,4S,5R,6S)-4-Amino-5-Hydroxy-6-Methyl-Tetrahydro-Pyran-2-Yloxy)-8-(1,2-Dihydroxy-Ethyl)-6,8,11-Trihydroxy-1-Methoxy-7,8,9,10-Tetrahydro-Naphthacene-5,12-Dione置于sodium Tetrahydroborate体系中,化学反应生成 表阿霉素
参考文献:Impairment Of Myocardial Contractility By Anticancer Anthracyclines: Role Of Secondary Alcohol Metabolites And Evidence Of Reduced Toxicity By A Novel Disaccharide Analogue
标题:Impairment Of Myocardial Contractility By Anticancer Anthracyclines: Role Of Secondary Alcohol Metabolites And Evidence Of Reduced Toxicity By A Novel Disaccharide Analogue
摘要:蒽环类抗癌药物多柔比星(dox)会导致心肌毒性.其侧链羰基通过酶促还原作用转化为次级醇代谢物,而该代谢物被认为与心脏毒性相关.因此,我们监测了暴露于dox或两种反应生成较少次级醇代谢物的类似物(表柔比星epi和新型二糖基蒽环类化合物men 10755)的雄性大鼠右心室条的负性变时作用(定义为对舒张后收缩的抑制作用). 30μm Epi的摄取率高于dox,但由于其对羰基还原具有抗性,导致形成相同数量的醇代谢物.men 10755表现出摄取受损,因此形成了最低水平的醇代谢物.相应地,Dox和epi抑制了舒张后收缩约40-50%,而men 10755抑制了约6%. 100μm Epi表现出与dox相等的摄取率,但形成了约50%的醇代谢物减少.100μm Men 10755仍然表现出最低摄取率,并形成了较epi约60%的醇代谢物减少.在这些条件下,Dox对舒张后收缩的抑制作用为88%.epi和men 10755的抑制作用分别为dox的约18%(p<0.05)和约80%(p<0.001). 30-100μm Dox,Epi或men 10755的负性变时作用与细胞中醇代谢物的水平(r=0.88,P<0.0001)和羰基蒽环类药物的水平(r=0.79,P<0.0001)相关.然而,多重比较显示,醇代谢物在抑制收缩性方面的效果比羰基蒽环类药物高出约20-40倍.因此,通过化学手段(如侧链缬氨酸酯化)增加men 10755的摄取和转化为醇代谢物(而不是保留为羰基形式),可以增强其负性变时作用. 这些结果表明,次级醇代谢物是心脏毒性的关键介导因素.减少摄取并限制向醇代谢物转化的形成,可能会使men 10755比dox和epi更具心脏耐受性. 英国药理学杂志 (2001) 134,1271-1278; Doi:10.1038/sj.Bjp.0704369
DOI:10.1038/sj.Bjp.0704369

专利信息

专利号:US-2024294462-A1
优先权日:2023-02-15
标题:Method for the Synthesis of Ionizable Lipids Using a Doubly Alkylated Intermediate
发明人：SAADATI FARIBA; TRAN HUY; CIUFOLINI MARCO; ATMURI N D PRASAD
权利人:NANOVATION THERAPEUTICS INC
摘要:Provided herein is a method for the preparation of ionizable, cationic amino lipids using a doubly alkylated nucleophilic intermediate to produce a ketone. The ketone, or a corresponding alcohol, is subjected to one or more synthesis steps to add an ionizable moiety thereto. The method can be advantageously employed for the synthesis of unsymmetrical analogues of the above lipids that would be considerably more difficult to make by alternative strategies. The method can also be used to prepare symmetrical ionizable, cationic amino lipids with fewer steps and/or with the use of fewer hazardous chemicals than known synthesis methods.

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:WO-2004011474-A1
优先权日:2002-07-31
标题:Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-6653468-B1
优先权日:2002-07-31
标 题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-2010137421-A1
优先权日:2006-11-08
标题 :Small molecule therapeutics, synthesis of analogues and derivatives and methods of use
发明人：THEODORAKIS EMMANUEL; BATOVA AYSE
权利人:THEODORAKIS EMMANUEL; BATOVA AYSE
摘要:Provided herein are compounds that are inducers of apoptosis activators of caspases and pharmaceutically acceptable derivatives thereof. Also provided are methods of synthesis of the compounds and methods for treatment of diseases in which there is uncontrolled cell growth and spread of abnormal cells, such as cancers, by administering the compounds.