📜L-苯丙氨酸乙酯盐酸盐置于4-二甲氨基吡啶,Lithium Hydroxide Monohydrate,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺体系中,用 四氢呋喃,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 3.0H,反应生成4-(1-芘基)丁酰-Phe-Oh
参考文献:Delivery Of Floxuridine Derivatives To Cancer Cells By Water-Soluble Organometallic Cages
标题:Delivery Of Floxuridine Derivatives To Cancer Cells By Water-Soluble Organometallic Cages
摘要:The Self-Assembly Of 2,4,6-Tris(Pyridin-4-yl)-1,3,5-Triazine (Tpt) Triangular Panels With P-Cymene (Ppr(I)C(6)H(4)Me) Ruthenium Building Blocks And 2,5-Dioxydo-1,4-Benzoquinonato (Dobq) Or 5,8-Dioxydo-1,4-Naphthoquinonato (Donq) Bridges,In The Presence Of A Pyrenyl-Nucleoside Derivatives (Pyrener),. Affords The Triangular Prismatic Host Guest Compounds [(Pyrene-R)Cru6(Ppr(I)C(6)H(4)Me)(6)(Tpt)(2)(Dobq)(3)](6+) ([(Pyrene-R)C1](6+)) And [(Pyrene-R)Cru6(Ppr(I)C(6)H(4)Me)(6)(Tpt)(2)(Donq)(3)](6+) ([(Pyrene-R)C2](6+)),Respectively. The Inclusion Of Six Monosubstituted Pyrenyl-Nucleosides (Pyrene-R1 = 5'-(1-Pyrenyl Butanoate)-2'-Deoxyuridine,Pyrene-R2 = 5-Fluoro-5'-(1-Pyrenyl Butanoate)-2'-Deoxyuridine,Pyrene-R3 = 5'-{n-[1-Oxo-4-(1-Pyrenyl)Butyl]Glycyl}-2'-Deoxyuridine,Pyrene-R4 = 5-Fluoro-5'-{n[1-Oxo-4-(1-Pyrenyl)Butyl]-Glycyl}2'-Deoxyuridine,Pyrene-R5 = 5-Fluoro-5'-{n-[1-Oxo-4-(1-Pyrenyl)Butyl]-Phenylalanyl}-2'-Deoxyvuridine,Pyrene-R6 = 5-Fluoro-5'-{n-[1-Oxo-4-(1-Pyrenyl)Butyl]-Phenylalanyl}-2'-Deoxyuridine) Has Been Accomplished. The Carceplex Nature Of [(Pyrene-R)C1](6+) With The Pyrenyl Moiety Firmly Encapsulated In The Hydrophobic Cavity Of The Cage With The Nucleoside Groups Pointing Outward Was Confirmed By NMR Spectroscopy And Electrospray Ionization Mass Spectrometry (Esi-Ms),While The Host-Guest Nature Of [(Pyrene-R)C2](6+) Was Studied In Solution By NMR Techniques. In Contrast To The Floxuridine Compounds Used In The Clinic,The Host-Guest Complexes Are Highly Water-Soluble. Consequently,The Cytotoxicities Of These Water-Soluble Compounds Have Been Established Using Human Ovarian A2780 And A2780Cisr Cancer Cells. All The Host Guest Systems Are More Cytotoxic Than The Empty Cages Alone [1][cf3So3](6) (Ic50 = 23 Mu M) And [2][cf3So3](6) (Ic50 = 10 Mu M),The Most Active Compound [pyrene-R4C1][cf3So3](6) Being 2 Orders Of Magnitude More Cytotoxic (Ic50 = 0.3 Mu M) On These Human Ovarian Cancer Cell Lines (A2780 And A2780Cisr).
Doi:10.1021/bc200472N