Abstract: Using 7-deoxycholic acid(1) as a starting material, 3,12-dioxy-7-deoxycholic acid(2) was obtained by oxidation with Jones reagent. Then the N,N-bis(2-chloroethyl)-3,12-dioxy-7-deoxycholic amide(4) was synthesized by the reaction of compound 2 with bis(2-chloroethyl)amine. Furthermore, N,N-bis(2-chloroethyl)-12-oxy-3-hydroximino-7-deoxycholic amide(5) and N,N-bis(2-chloroethyl)-12-oxy-3-thiosemicarbazone-7-deoxycholic amide(6) were prepared by the functional group transformation of 3-carbonyl on compound 4. The antiproliferative activities of compounds against HeLa cells were assayed and the result showed that the compounds displayed distinct cytotoxicity.

Key words: deoxycholic acid, substituted-oxy-N,N-bis(chloroethyl)-deoxycholic amides, synthesis, antitumor activity