Synthesis of novel hexestrol and diethylstilbestrol derivatives as potential anticancer and estrogenic agents.
Two novel series of potential anticancer agents derived from hexestrol and diethylstilbestrol have been synthesized. The first includes several alkylating agents containing sulphonic esters and nitrogen mustard functions attached through various chains to only one phenolic group in hexestrol. The second contains the N1-acetyl-N4-substituted thiosemicarbazide moieties attached to one phenolic group hexestrol or to the two phenolic oxygens in diethylstilbestrol. The tests of some of the products for antileukemic activity in P 388 Lymphocytic Leukemia indicated no significant activity over the parent nuclei. The estrogenic activity of some representative examples of the thiosemicarbazides was found to be dependent on the nature of the N4-substituent in the thiosemicarbazide moiety.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D004054:Diethylstilbestrol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D045166:Estradiol Congeners / Q000138:chemical synthesis*; D004971:Estrus / Q000187:drug effects; D005260:Female; D006589:Hexestrol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D011247:Pregnancy; D051381:Rats
D000970:Antineoplastic Agents; D045166:Estradiol Congeners; D006589:Hexestrol; D004054:Diethylstilbestrol