Fluorescent inhibitors of thymidylate synthetase.
J Pharm Sci
; 66(3): 434-6, 1977 Mar.
Article
en En
| MEDLINE
| ID: mdl-403277
ABSTRACT
Two fluorescent derivatives of 2'-deoxy-5-fluorouridine 5'-p-aminophenyl phosphate were prepared by treatment of this compound with fluorescein isothiocyanate in dimethyl sulfoxide or 5-(dimethylamino)naphthalene sulfonyl chloride in pyridine. The products of the reactions were isolated by diethylaminoethylcellulose chromatography and were shown to be homogeneous by polyacrylamide electrophoresis and TLC. Confirmation of the structure was provided by elemental analysis, absorption and fluorescence spectra, PMR measurements, and liberation of nucleotide upon hydrolysis with snake venom phosphodiesterase. The fluorescent derivatives are good competitive inhibitors (Ki approximately10(-6) M) of thymidylate synthetase from a methotrexate-resistant strain of Lactobacillus casei.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Timidilato Sintasa
/
Nucleótidos de Uracilo
/
Fluorodesoxiuridilato
/
Metiltransferasas
Idioma:
En
Revista:
J Pharm Sci
Año:
1977
Tipo del documento:
Article