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Métodos Terapéuticos y Terapias MTCI
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Int J Cancer ; 68(3): 356-63, 1996 Nov 04.
Artículo en Inglés | MEDLINE | ID: mdl-8903478


Formulation difficulties prevented the otherwise promising clinical development of the anti-tumour agent trimelamol (TM; tris-[hydroxymethyl]trimethylmelamine]). A synthetic analogue programme resulted in the identification of CB 7646 (bis N-[hydroxymethyl]trimethylmelamine) as a compound with improved stability and favourable formulation characteristics. The in vitro and in vivo activity of CB 7646 was shown to be very similar to that of TM. In addition, curative activities were shown in the PXN/65 human ovarian cancer xenograft and the MX-1 and T-61 human breast cancer xenograft models. The effectiveness of the N-(hydroxymethyl)melamines against platinum-refractory disease was noted in the phase I clinical trial of TM. In line with this finding, the present study confirmed the effective activity of both TM and CB 7646 against various forms of platinum resistance in in vitro models. Curative activity for TM and CB 7646 was seen in the HX110P human ovarian cancer xenograft with acquired carboplatin resistance. Animal studies indicated less neurotoxicity for CB 7646 than for TM. The pharmacokinetic profile of CB 7646 indicated a decreased plasma elimination, indicative of slower in vivo degradation than for TM. CB 7646, therefore, represents a promising candidate for clinical development, designed to supersede TM.

Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Triazinas/síntesis química , Triazinas/farmacología , Animales , Antineoplásicos/química , Química Farmacéutica , Cisplatino/farmacología , Cisplatino/toxicidad , Evaluación Preclínica de Medicamentos , Ensayos de Selección de Medicamentos Antitumorales , Estabilidad de Medicamentos , Femenino , Humanos , Masculino , Ratones , Ratones Endogámicos BALB C , Trasplante de Neoplasias , Enfermedades del Sistema Nervioso/inducido químicamente , Neoplasias Ováricas/tratamiento farmacológico , Plasmacitoma/tratamiento farmacológico , Ratas , Ratas Wistar , Soluciones , Trasplante Heterólogo , Triazinas/química , Células Tumorales Cultivadas/efectos de los fármacos , Agua/química
Planta Med ; 56(2): 187-9, 1990 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-2353066


A novel diterpene, (5R, 8R, 9S, 10R)-12-oxo-ent-3,13(16)-clerodien-15-oic acid, has been obtained from the leaves of Premna schimperi (Verbenaceae) using an anti-microbial bioassay-guided isolation procedure. The diterpene was identified on the basis of spectroscopic data and is active against the Gram-positive bacteria Staphylococcus aureus and Bacillus subtilis in the concentration range 20-25 micrograms ml-1.

Antibacterianos/aislamiento & purificación , Diterpenos/farmacología , Plantas Medicinales/análisis , Diterpenos/aislamiento & purificación