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-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
专利号:US-5569786-A 优先权日:1987-01-06 标 题 :Isolation, structural elucidation and synthesis of novel antineoplastic substances denominated 'combretastatins' 发明人:PETTIT GEORGE R; SINGH SHEO B 权利人:UNIV ARIZONA 摘要:New antineoplastic substances have been isolated, structurally elucidated and synthesized having a general structural formula of: (I) or H or OCH3; or R1R2 is -OCH2O-; R3 is H or OH; and R4 is OH or OCH3. These substances have been denominated 'combretastatin A-1, -A-2, -A-3, -B-1, -B-2, -B-3 and -B-4'. preparation containing the substances and methods of treating a host inflicted with a neoplastic growth with the preparation is described.
[参考文献]: Forester Sc, Et Al. Gut Metabolites Of Anthocyanins, Gallic Acid, 3-O-Methylgallic Acid, And 2,4,6-Trihydroxybenzaldehyde, Inhibit Cell Proliferation Of Caco-2 Cells. J Agric Food Chem. 2010 May 12;58(9):5320-7. [参考文献]: Forester Sc, The Anthocyanin Metabolites Gallic Acid, 3-O-Methylgallic Acid, And 2,4,6-Trihydroxybenzaldehyde Decrease Human Colon Cancer Cell Viability By Regulating Pro-Oncogenic Signals. Mol Carcinog. 2014 Jun;53(6):432-9.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198