Synthesis of potential anticancer agents- I: Synthesis of substituted thiophenes

Abstract

In view of the anticancer activity of thiophene-2,5-dicar□ylic acid, a series of derivatives of this acid were prepared. Starting from 2,5-dichloromethylthiophene, thiophene-2,5-dialdehyde, thiophene-2,5-dimethylenyl-thiouronium dichloride, 2,5-dimercaptomethylthiophene were prepared. 3,4-Dihydroxylthiophene, a thiophene isoster of catechol, was prepared by decar□ylation of 2,5-dicar□y-3,4-dihydroxythiophene. Of the compounds reported, the above dithiouronium salt proved highly active against Yoshida sarcoma in rats.