MEDI 157 |
| As part of the program to develop novel probes for the estrogen receptor, we have designed target compounds that incorporate an alkylating agent appended through a PEG linker to an 11beta-arylestradiol. Our approach utilizes the independent preparation of the two functional units, an alkynylated Mitomycin C analog and azido substituted-alkoxy arylestradiol, which can be ligated using Click chemistry. The rational design of the bi-functional compounds envisions not only interaction with estrogen receptor ligand binding domain as potent therapeutic anti-estrogens, but also formation of covalent linkages with DNA as alkylating agents to attack hypoxic regions of the tumor. The synthesis routes and preliminary biological results will be presented.
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General Poster Session
7:00 PM-9:00 PM, Sunday, 10 September 2006 Moscone Center -- Hall D, Poster
Sci-Mix
Division of Medicinal Chemistry |
