Ontology highlight
ABSTRACT:
SUBMITTER: Hanson RN
PROVIDER: S-EPMC3519291 | biostudies-literature | 2012 Nov
REPOSITORIES: biostudies-literature
Hanson Robert N RN Hua Edward E Labaree David D Hochberg Richard B RB Proffitt Kyle K Essigmann John M JM Croy Robert G RG
Organic & biomolecular chemistry 20120925 42
A convergent synthesis of a novel estrogen receptor-targeted drug hybrid was developed based on structures of the potent anti-proliferative mitomycin C and the steroidal anti-estrogen RU 39411. The steroidal antiestrogen was prepared with an azido-triethylene glycoloxy linker while the mitomycin C derivative (porfirimycin) incorporated a complementary 7-N-terminal alkyne. The two components were ligated using the Huisgen [3 + 2] cycloaddition ("click") reaction. Preliminary biological assays dem ...[more]