A series of 3-benzofuryl-4-phenyl(allyl)-5-mercapto-1,2,4-triazoles have been synthesized by cyclization of the corresponding substituted thiosemicarbazides of benzofuran-2-carboxylic acid. S-alkylation of 5-mercaptotriazoles with various alkyl-, alkenyl-, and benzyl-substituted benzyl chlorides; chloroacetamides; and chloroacetic-, 2-bromopropionic-, and 2-bromocaproic acids has been studied. The antitumor activity of the synthesized compounds was tested.
The physicochemical properties and antitumor activity of dacarbazine, its analogs, and the new alkylating agent imidazene are reviewed. It is shown that the activity of dacarbazine is superior to most of its analogs. Imidazene exhibits an advantage over dacarbazine with respect to both stability and activity and can be used for the treatment of malignant melanoma and sarcoma of soft tissues and in combined chemotherapy.
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