Synthesis, DNA-binding properties, and antitumor activity of novel distamycin derivatives.

Arcamone, F M; Animati, F; Barbieri, B; Configliacchi, E; D'Alessio, R; Geroni, C; Giuliani, F C; Lazzari, E; Menozzi, M; Mongelli, N

Arcamone, F M; Animati, F; Barbieri, B; Configliacchi, E; D'Alessio, R; Geroni, C; Giuliani, F C; Lazzari, E; Menozzi, M; Mongelli, N.

Afiliación

Arcamone FM; Research and Development, Farmitalia-Carlo Erba, Erbamont Group, Milan, Italy.

J Med Chem ; 32(4): 774-8, 1989 Apr.

Article en En | MEDLINE | ID: mdl-2590277

RESUMEN

A group of potential alkylating agents have been synthesized that are structurally related to the oligopeptide antiviral antibiotic distamycin. All derivatives form complexes with native calf-thymus DNA but compounds 2, 3, and 6 give rise to covalent adducts. Cytostatic activity against both human and murine tumor cell lines in vitro is displayed by the new compounds. Compounds 3 and 4 are active on melphalan-resistant L1210 leukemia in mice.

Asunto(s)

ADN/metabolismo; Distamicinas; Neoplasias/tratamiento farmacológico; Pirroles; Alquilantes; Animales; Fenómenos Químicos; Química; Cromatografía Líquida de Alta Presión; Dicroismo Circular; Distamicinas/síntesis química; Distamicinas/metabolismo; Distamicinas/uso terapéutico; Humanos; Leucemia L1210/tratamiento farmacológico; Leucemia Experimental/tratamiento farmacológico; Ratones; Pirroles/síntesis química; Pirroles/metabolismo; Pirroles/uso terapéutico; Relación Estructura-Actividad; Células Tumorales Cultivadas

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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirroles / ADN / Distamicinas / Neoplasias Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 1989 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos

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