CAS: 2730-71-4; Thiocolchicine

上下游产品

Thiocolchicine 209810-39-9
(7S)-7-氨基-1,2,3-三甲氧基-10-甲硫基-6,7-二氢-5H-苯并[g]庚搭烯-9-酮 Deacetylthiocolchicine 2731-16-0
7-Amino-1,2,3-Trimethoxy-10-Methylsulfanyl-6,7-Dihydro-5H-Benzo[a]-Heptalen-9-One 2731-16-0
秋水仙碱 Colchicine 64-86-8
N-(1,2,3,10-四甲氧基-9-氧代-5,6,7,9-四氢苯并[a]庚搭烯-7-基)乙酰胺 N-(5,6,7,9-Tetrahydro-1,2,3,10-Tetramethoxy-9-Oxobenzo[a]Heptalen-7-yl) Acetamide 54192-66-4
(1S,4R)-4,7,7-Trimethyl-3-Oxo-2-Oxa-Bicyclo[2.2.1]Heptane-1-Carboxylic Acid ((S)-1,2,3-Trimethoxy-10-Methylsulfanyl-9-Oxo-5,6,7,9-Tetrahydro-Benzo[a]Heptalen-7-yl)-Amide 203584-67-2

📜秋水仙碱置于甲硫醇,对甲苯磺酸体系中,用80%的收率获得硫代秋水仙碱
参考文献:Photochemical Isomerization Of Colchicine And Thiocolchicine
标题:Photochemical Isomerization Of Colchicine And Thiocolchicine
摘要:The Photochemical Reactivity Of Colchicine And Thiocolchicine Is Described. Although The Irradiation Of Colchicine Gave A Well-Known Transposition Reaction To Beta-And Gamma-Lumicolchicines,Thiocolchicine Did Not React. Femtosecond Transient Spectroscopy Of Colchicine Showed A Strong Band With Maximum At 510 Nm Appearing At Tau = 0. It Disappeared Within Few Hundred Femtoseconds,Leaving A Broad Structureless Band With A Maximum Around 470 Urn. A Second Band Is Observed Around 410 Nm. The Analysis In Time Showed That The 510-Nm Component Appeared Instantaneously And Decayed Following A Biexponential Low With Time Constants Of 300 +/-100 Fs And 40 Ps. The Kinetics At 420 Nm Has A Measurable Rise Lime Of 300 +/-150 Fs. Quantum Mechanical Calculations On Colchicine Showed That This Absorption Is Due To A S-1--> S-11 Transition. In Thiocolchicine,The Instantaneous Formation Of A Structure With Maxima Out Of The Investigated Spectral Region Was Observed. A Strong Absorption Around 650 Nm Indicated The Presence Of A Band With A Maximum At Longer Wavelengths (> 700 Nm) And A Peak Around 380 Nm,Which Partially Coincides With The Ground-State Absorption And Therefore Strongly Affected Absorption Around 650 Nm And Its Rapid (Similar To500 Fs) Decay By Its Bleaching. The Instantaneous Formation Of An Absorption Was Observed. At Shorter Wavelengths (400 Nm),The T Decay Was Fitted With A Biexponential Curve With The First Time Constant Of About 80 Ps. The Second Part Of,The Decay Had A Very Long Tail Up To 500 Ps. Transient Spectroscopy And Configuration Interaction Calculations Are In Agreement With A Mechanism Involving A Disrotatory Cyclization Of Colchicine In Its First Excited Singlet State. The Lack Of Reactivity Observed In Thiocolchicine Was Explained By Considering The Presence Of Efficient Isc To The Triplet State.
Doi:10.1021/jp035507L

专利信息

专利号:US-2025090698-A1
优先权日:2018-11-27
标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases
发明人：CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT
权利人:INDIAN INSTITUTE OF TECH INDORE
摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.

专利号:US-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

专利号:US-8207221-B2
优先权日:2004-01-30
标 题:Crystalline polymorphs of a CXC-chemokine receptor ligand
发明人：HU MENGWEI; YU YOUNONG; DWYER MICHAEL P; TAVERAS ARTHUR G; KIM-MEADE AGNES; YIN JIANGUO; FU XIAOYONG; MCALLISTER TIMOTHY L; ZHANG SHUYI; KLOPFER KEVIN
权利人:HU MENGWEI; YU YOUNONG; DWYER MICHAEL P; TAVERAS ARTHUR G; KIM-MEADE AGNES; YIN JIANGUO; FU XIAOYONG; MCALLISTER TIMOTHY L; ZHANG SHUYI; KLOPFER KEVIN; SCHERING CORP
摘要:The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: n n n n n n n n n n These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.

专利号:US-8461298-B2
优先权日:2004-11-01
标 题:Compositions and methods for modification of biomolecules
发明人：BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL
权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA
摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

专利号:US-9260371-B2
优先权日:2004-11-01
标题:Compositions and methods for modification of biomolecules
发明人：BERTOZZI CAROLYN RUTH; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; SLETTEN ELLEN MAY
权利人:UNIV CALIFORNIA
摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

专利号:US-6943194-B1
优先权日:1998-01-09
标题:Synthesis of phenstatin and prodrugs thereof
发明人：PETTIT GEORGE R; TOKI BRIAN
权利人:UNIV ARIZONA STATE
摘要:A newly discovered antineoplastic compound denominated “phenstatinâ€? is herein described as are synthetic methods for producing phenstatin and the active prodrug thereof. Phenstatin was converted to the sodium phosphate prodrug (3d) by a dibenzylphosphite phosphorylation and subsequent hydrogenolysis sequence 3b→3c→3d. Phenstatin (3b) was found to be a potent inhibitor of tubulin polymerization and the binding of colchicine to tubulin comparable to combretastatin A-4 (1b).