Preparation and antischistosomal and antitumor activity of hycanthone and some of its congeners. Evidence for the mode of action of hycanthone.
J Med Chem
; 31(1): 254-60, 1988 Jan.
Article
em En
| MEDLINE
| ID: mdl-3336024
ABSTRACT
The synthesis of a series of esters of hycanthone (HC) and 7-hydroxyhycanthone, their antitumor activity, and their antischistosomal effects on HC-sensitive and HC-resistant schistosomes are reported. Binding studies using tritium-labeled HC and hycanthone N-methylcarbamate (HNMC) with calf thymus DNA provided evidence that HNMC but not HC alkylated the DNA. Tritiated HNMC also bound to the DNA of intact HeLa cells exposed to the drug while very little tritiated HC bound to DNA under the same conditions. The mechanism proposed previously to account for the antischistosomal action of HC, namely, drug esterification followed by alkylation of DNA, applies also to the antitumor action of the drug as shown in Scheme I.
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Base de dados:
MEDLINE
Assunto principal:
Schistosoma mansoni
/
Esquistossomicidas
/
Tioxantenos
/
Leucemia Experimental
/
Leucemia P388
/
Hicantone
/
Antineoplásicos
Limite:
Animals
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
1988
Tipo de documento:
Article