Alkylation of γ-(4-nitrobenzyl)pyridine by four N-diazoacetyl derivatives of amino acids. Lack of fine correlation with the unscheduled DNA synthesis induced in mouse cells “In vitro”

1977 ◽  
Vol 9 (7) ◽  
pp. 621-631 ◽  
Author(s):  
S. Parodi ◽  
M. Picca ◽  
C. Bolognesi ◽  
M. Cavanna ◽  
P. Carlo ◽  
...  
Keyword(s):  
Amino Acids ◽  
Dna Synthesis ◽  
Unscheduled Dna Synthesis ◽  
Mouse Cells ◽  
Derivatives Of

Use of in Vivo/In Vitro Unscheduled Dna Synthesis for Identification of Organ-Specific Carcinogens

1987 ◽  
Vol 17 (3) ◽  
pp. 245-277 ◽  
Author(s):  
Chie Furihata ◽  
Taijiro Matsushima ◽  
Byron E. Butterworth
Keyword(s):  
Dna Synthesis ◽  
Unscheduled Dna Synthesis ◽  
Organ Specific

Phosphoramidate Derivatives of AZT as Inhibitors of HIV: Studies on the Carboxyl Terminus

1993 ◽  
Vol 4 (2) ◽  
pp. 97-101 ◽  
Author(s):  
C. McGuigan ◽  
R. N. Pathirana ◽  
S. S.-M. Choi ◽  
D. Kinchington ◽  
T. J. O'Connor
Keyword(s):  
Amino Acids ◽  
Biological Activity ◽  
Carboxyl Terminus ◽  
Amino Ester ◽  
Carboxy Terminus ◽  
Free Nucleotides ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Ester Lead

Novel phosphoramidate derivatives of the anti-HIV nucleoside analogue AZT have been prepared by phosphorochloridate chemistry. These materials carry carboxy-protected, amino acids, and are designed to act as membrane-soluble prodrugs of the bio-active free nucleotides. In vitro evaluation revealed the compounds to have a pronounced, selective antiviral activity. In particular, variation in the carboxy terminus region is studied. For alkyl phosphates small changes in the structure of the amino ester lead to marked changes in biological activity. However, for analogous aryl phosphates there is little dependence on the structure of the ester. This suggests a different mechanism of action for these two categories of phosphate prodrug.

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