2,5-二羟基苯甲醛,5-氨基水杨酸,水杨醛 反应生成薰草菌素 参考文献:A Versatile Solid Phase Synthesis Of Lavendustin A And Certain Biologically Active Analogs 标题:A Versatile Solid Phase Synthesis Of Lavendustin A And Certain Biologically Active Analogs 摘要:Reaction Of Aminomethylated Polystyrene Resin (8) With Succinic Anhydride,Followed By Esterification Of The Free Carboxylic Acid Of The Product 9 With 2,5-Dihydroxybenzaldehyde (4) Afforded The Resin-Linked Aldehyde Intermediate 10. The Key Intermediate 10 Was Converted Into The Protein-Tyrosine Kinase Inhibitor Lavendustin A And Certain Analogs Through Reductive Amination And Reductive Alkylation Steps,Followed By Cleavage From The Resin. This Method Enables The Preparation Of A Wide Variety Of Lavendustin A Analogs Using Combinatorial Chemistry And Parallel Synthesis Techniques. Doi:10.1021/jo961719L
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-12180228-B2 优先权日:2019-06-05 标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof 发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.
专利号:US-11759496-B2 优先权日:2016-05-10 标题:Compounds and pharmaceutical use thereof in the treatment of cancer 发明人:SUSIN SANTOS A; KAROYAN PHILIPPE; MERLE-BERAL HÉLÈNE 权利人:KAROYAN PHILIPPE 摘要:The present invention relates to a compound or a pharmaceutical salt thereof comprising a hexapeptide sequence of formula (I), its method of synthesis and its use in anticancer therapy. The invention also relates to a pharmaceutical composition for use in the treatment of cancer comprising at least one soluble peptide according to the invention or at least one acid nucleic according to the invention or at least one expression vector according to the invention, or at least one host cell according to the invention and a pharmaceutically acceptable carrier.
专利号:US-2009227575-A1 优先权日:2008-03-04 标 题 :7H-PYRROLO[2,3-H]QUINAZOLINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESIS 发明人:VENKATESAN ARANAPAKAM MUDUMBAI; CHEN ZECHENG; DOS SANTOS OSVALDO; BROOIJMANS NATASJA; GOPALSAMY ARIAMALA 权利人:WYETH CORP 摘要:A 7H-pyrrolo[2,3-h]quinazoline compound of the formula I n n n n n n n n n n wherein Ar, R 1 , R 2 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , and n are as defined in the specification, and methods for making same.
专利号:WO-2011059609-A9 优先权日:2009-10-13 标 题 :Dendrimer compositions and methods of synthesis
专利号:WO-2011028334-A2 优先权日:2009-08-26 标题:Synthesis and isolation of dendrimer systems
1: Nam DH, Lee KY, Moon CS, Lee YS. Synthesis and anticancer activity of chromone-based analogs of lavendustin A. Eur J Med Chem. 2010 Sep;45(9):4288-92. doi: 10.1016/j.ejmech.2010.06.030. doi: 10.1016/j.bmc.2008.07.039. 17: Meizel S, Turner KO. Chloride efflux during the progesterone-initiated human sperm acrosome reaction is inhibited by lavendustin A, a tyrosine kinase inhibitor. J Androl. 1996 Jul-Aug;17(4):327-30.
合成参考文献
参考文献:10.1007/s004240050909 摘要:Obayashi K, Horie M, Washizuka T, Nishimoto T, Sasayama S. On the mechanism of genistein-induced activation of protein kinase A-dependent Cl - conductance in cardiac myocytes. Pflgers Archiv European Journal of Physiology. 1999 Jul 19;438(3):269–77. doi: 10.1007/s004240050909. 参考文献:10.1023/b:plan.0000028792.72343.ee 摘要:Day RB, Tanabe S, Koshioka M, Mitsui T, Itoh H, Ueguchi-Tanaka M, Matsuoka M, Kaku H, Shibuya N, Minami E. Two rice GRAS family genes responsive to N -acetylchitooligosaccharide elicitor are induced by phytoactive gibberellins: evidence for cross-talk between elicitor and gibberellin signaling in rice cells. Plant Mol Biol. 2004 Jan;54(2):261–72. doi: 10.1023/b:plan.0000028792.72343.ee. 参考文献:10.1016/j.ejmech.2006.04.008 摘要:Lee KY, Nam DH, Moon CS, Seo SH, Lee JY, Lee YS. Synthesis and anticancer activity of lavendustin A derivatives containing arylethenylchromone substituents. European Journal of Medicinal Chemistry. 2006 Aug;41(8):991–6. doi: 10.1016/j.ejmech.2006.04.008. 参考文献:10.1002/jcp.1041520325 摘要:Lin Y, Chrest FJ, Gabrielson EW. Reversible G1 arrest of a human lung epithelial cell line by staurosporine. J Cell Physiol. 1992 Sep;152(3):646–53. doi: 10.1002/jcp.1041520325. 参考文献:10.1002/stem.5530120104 摘要:Burke TR. Protein-tyrosine kinases: potential targets for anticancer drug development. Stem Cells. 1994 Jan;12(1):1–6. doi: 10.1002/stem.5530120104.