Aziridine and hydroxy- and chloroethylamine derivatives of colchicine and their biological activity

With the aim of enhancing the cytostatic properties of the initial alkaloid, new aziridine and bis(chloroethyl)amine derivatives of colchicine have been synthesized by the direct interaction of colchicine with chloroethylamine hydrochloride and also via the mono-and diethanolamine derivatives. The structures of the compounds obtained have been studied by spectral methods. An increased radiomodifying and antitumoral activity and a decreased toxicity of the substances synthesized as compared with the initial colchicine has been shown. Results obtained in the National Cancer Institute of the USA from the study of the cytostatic activity of the bis(chloroethyl)amino derivative of 60 tumor lines are presented.