The diorganotin（Ⅳ） complexes of N-（3,5-dibromosalicylidene）-α-amino acid, R2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（where R=H, Me, i-Pr, Bz; R＇=n-Bu, Cy）, were synthesized by the reactions of diorganotin dichlorides...The diorganotin（Ⅳ） complexes of N-（3,5-dibromosalicylidene）-α-amino acid, R2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（where R=H, Me, i-Pr, Bz; R＇=n-Bu, Cy）, were synthesized by the reactions of diorganotin dichlorides with in situ formed potassium salt of N-（3,5-dibromosalicylidene）-α-amino acid and characterized by elemental analysis, IR and NMR （^1H, ^13C and ^119Sn） spectra. The crystal structures of n-Bu2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（R=i-Pr, Bz） and Cy2Sn（2-O-3,5-Br2C6H2CH=NCHRCOO）（R=Me, Bz） were determined by X-ray single crystal diffraction and showed that the tin atoms are in a distorted trigonal bipyramidal geometry to form five- and six-membered chelate rings with the tridentate ligand. Bioassay results indicated that the compounds possess better in vitro antitumour activity against three human tumour cell lines, HeLa, CoLo205 and MCF-7, than cis-platin and moderate anti-bacterial activity against two bacteria, E. coli and S. aureus.展开更多
With phosphoric formic acid (PFA) and its analog,phosphonoacetic acid (PAA),as the lead compounds,α-amino phosphonates were introduced into PFA and PAA.The derivatives oi N-( alkoxycarbonyl-aikoxyphosphonyl)-α-arnin...With phosphoric formic acid (PFA) and its analog,phosphonoacetic acid (PAA),as the lead compounds,α-amino phosphonates were introduced into PFA and PAA.The derivatives oi N-( alkoxycarbonyl-aikoxyphosphonyl)-α-arnino phosphonates (Ⅰ) and N-(alkoxycarbonyl-methyt-alkoxyphosphonyl)-α-amino phosphonates (Ⅱ) with the N-terminal of amino phosphonates bonding to phosphorus atom of PFA and PAA were synthesized via the reaction of the corresponding phosphonyl chloride with a-amino phosphonates in the presence of a base.The 31P NMK spectra of Ⅰ and Ⅱwere determined.It is found that the coupling constants 3Jpp with R3 being alkyl group were lower than those with R3 being (substituted) phenyl,and this result was discussed.The preliminary bioassay showed that some of the compounds Ⅰ and Ⅱhave better activities against tobacco mosaic virus (TMV).The inhibitory was higher than that of DHT (2,4-dioxyhexahydro-1,3,5-triazine).In addition,some of the compounds showed the activity against cancer cells.展开更多
In recent years, considerable efforts have been expended to the development ofenantioselective synthesis of α-amino acids and the use of α-amino acids as chiralbuilding blocks for the synthesis of complex molecules....In recent years, considerable efforts have been expended to the development ofenantioselective synthesis of α-amino acids and the use of α-amino acids as chiralbuilding blocks for the synthesis of complex molecules. Numerous unnatural aminoacids which are often the characteristic units of biologically active peptides, have alsobeen discovered. Herein we describe a convenient and general access to natural andunnatural α-amino acids which are based on the use of the chiral building blocks,(S)-1a-e and (R)-1a-e from kinetic resolution of α-furfuryl amines (Scheme 1).展开更多
STUDIES of radiation chemistry on methionine (Met) were very active in previous years because of its actions of radioprotection to biological systems by quenching·OH radicals. On the other hand, people have paid ...STUDIES of radiation chemistry on methionine (Met) were very active in previous years because of its actions of radioprotection to biological systems by quenching·OH radicals. On the other hand, people have paid more and more attention to the researches on the phosphorylation of the biological polymolecules. It is wall known that phosphate ester is regarded as the deposi-展开更多
基金Project supported by the Natural Science Foundation of Shandong Province （No. Z2002F01）, the State Key Laboratory of Crystal Materials （No. 2005B 103） and the Scientific Research Foundation of Qufu Normal University.
文摘The diorganotin（Ⅳ） complexes of N-（3,5-dibromosalicylidene）-α-amino acid, R2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（where R=H, Me, i-Pr, Bz; R＇=n-Bu, Cy）, were synthesized by the reactions of diorganotin dichlorides with in situ formed potassium salt of N-（3,5-dibromosalicylidene）-α-amino acid and characterized by elemental analysis, IR and NMR （^1H, ^13C and ^119Sn） spectra. The crystal structures of n-Bu2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（R=i-Pr, Bz） and Cy2Sn（2-O-3,5-Br2C6H2CH=NCHRCOO）（R=Me, Bz） were determined by X-ray single crystal diffraction and showed that the tin atoms are in a distorted trigonal bipyramidal geometry to form five- and six-membered chelate rings with the tridentate ligand. Bioassay results indicated that the compounds possess better in vitro antitumour activity against three human tumour cell lines, HeLa, CoLo205 and MCF-7, than cis-platin and moderate anti-bacterial activity against two bacteria, E. coli and S. aureus.
基金Project supported by the National Natural Science Foundation of China
文摘With phosphoric formic acid (PFA) and its analog,phosphonoacetic acid (PAA),as the lead compounds,α-amino phosphonates were introduced into PFA and PAA.The derivatives oi N-( alkoxycarbonyl-aikoxyphosphonyl)-α-arnino phosphonates (Ⅰ) and N-(alkoxycarbonyl-methyt-alkoxyphosphonyl)-α-amino phosphonates (Ⅱ) with the N-terminal of amino phosphonates bonding to phosphorus atom of PFA and PAA were synthesized via the reaction of the corresponding phosphonyl chloride with a-amino phosphonates in the presence of a base.The 31P NMK spectra of Ⅰ and Ⅱwere determined.It is found that the coupling constants 3Jpp with R3 being alkyl group were lower than those with R3 being (substituted) phenyl,and this result was discussed.The preliminary bioassay showed that some of the compounds Ⅰ and Ⅱhave better activities against tobacco mosaic virus (TMV).The inhibitory was higher than that of DHT (2,4-dioxyhexahydro-1,3,5-triazine).In addition,some of the compounds showed the activity against cancer cells.
基金Project supported by the National Natural Science Foundation of China.
文摘In recent years, considerable efforts have been expended to the development ofenantioselective synthesis of α-amino acids and the use of α-amino acids as chiralbuilding blocks for the synthesis of complex molecules. Numerous unnatural aminoacids which are often the characteristic units of biologically active peptides, have alsobeen discovered. Herein we describe a convenient and general access to natural andunnatural α-amino acids which are based on the use of the chiral building blocks,(S)-1a-e and (R)-1a-e from kinetic resolution of α-furfuryl amines (Scheme 1).
文摘STUDIES of radiation chemistry on methionine (Met) were very active in previous years because of its actions of radioprotection to biological systems by quenching·OH radicals. On the other hand, people have paid more and more attention to the researches on the phosphorylation of the biological polymolecules. It is wall known that phosphate ester is regarded as the deposi-
