Halogenated triptolide derivatives as immunomodulators and anticancer agents

摘要

Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, CR¹R² is selected from CHOH, C-O, CHF, CF₂ and C(CF₃)OH; CR⁶ and CR¹³ are selected from CH, COH and CF; CR⁷R⁸, CR⁹R¹⁰ and CR¹¹R¹² are selected from CH₂, CHOH, C-O, CHF and CF₂; and CR³R⁴R⁵ is selected from CH₃, CH₂OH, C-O, COOH, CH₂F, CHF₂ and CF₃; such that: at least one of R¹-R¹³ comprises fluorine; no more than two of CR³R⁴R⁵, CR⁶, CR⁷R⁸, CR⁹R¹⁰, CR¹¹R¹², and CR¹³ comprises fluorine or oxygen; and, when CR¹R² is CHOH, CR³R⁴R⁵ is not CH₂F.