RESUMEN
This work deals with the synthesis of a new nitrogen mustard derivative based on thymine. To introduce the bis(2-chloroethyl)amine group to position 4 of the pyrimidine base, many strategies were explored and the desired compound was finally obtained, thanks to a synthetic pathway in five steps.
Asunto(s)
Antineoplásicos Alquilantes/síntesis química , Mecloretamina/síntesis química , Timina/química , Alquilación , Antineoplásicos Alquilantes/química , Etanolaminas/química , Mecloretamina/química , Estructura MolecularRESUMEN
The synthesis and biological activity of a novel DNA cross-linking antitumor agent is presented. The new alkylating agent significantly inhibited cell proliferation, migration and invasion as tested in vitro on the A431 vulvar epidermal carcinoma cell line.
Asunto(s)
Compuestos de Mostaza Nitrogenada/síntesis química , Compuestos de Mostaza Nitrogenada/farmacología , Timina/análogos & derivados , Antineoplásicos Alquilantes/síntesis química , Antineoplásicos Alquilantes/química , Antineoplásicos Alquilantes/farmacología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Quimiotaxis/efectos de los fármacos , Humanos , Metaloproteinasa 2 de la Matriz , Inhibidores de la Metaloproteinasa de la Matriz , Invasividad Neoplásica/prevención & control , Compuestos de Mostaza Nitrogenada/química , Timina/química , Timina/farmacologíaRESUMEN
The synthesis and biological activity of chloroethyl pyrimidine nucleosides is presented. One of these new nucleosides analogues significantly inhibited cell proliferation, migration and invasion as tested in vitro on the A431 vulvar epidermal carcinoma cell line.