Synthesis of Estrone Heterodimers and Evaluation of Their In Vitro Antiproliferative Activity.

ABSTRACT: Directed structural modifications of natural products offer excellent opportunities to develop selectively acting drug candidates. Natural product hybrids represent a particular compound group. The components of hybrids constructed from different molecular entities may result in synergic action with diminished side effects. Steroidal homo- or heterodimers deserve special attention owing to their potentially high anticancer effect. Inspired by our recently described antiproliferative core-modified estrone derivatives, here, we combined them into heterodimers via Cu(I)-catalyzed azide-alkyne cycloaddition reactions. The two trans-16-azido-3-(O-benzyl)-17-hydroxy-13α-estrone derivatives were reacted with 3-O-propargyl-D-secoestrone alcohol or oxime. The antiproliferative

SUBMITTER: Bozsity N 

PROVIDER: S-EPMC11050183 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature