Combinatorial Synthesis for the Expedited Discovery of Novel Selective Antiestrogens for Breast Cancer Prevention and Therapy
Abstract
We have conceived of an approach to prepare by combinatorial methods, libraries of novel ligands for the estrogen receptor, that might be useful in the treatment or prevention of breast cancer, by the creation of simple amide or five-membered ring heterocyclic core structures that display peripheral substituents (phenols, aliphatic groups, etc.) commonly found in non-steroidal estrogens. We have made good progress on the preparation of novel estrogen of the diphenyl carboxamide class, the diphenylsulfonamide class, the phenyl benzylcarboxamide and sulfonamide classes, and the pyrazole, oxazole, thiazole, and imidazole classes. Members of same class have high affinity for the estrogen receptor. Future efforts will be directed at perfecting the solid phase synthesis of the pyrazole class, which appear to be the most promising, and expanding the size of the libraries that can b% prepared.
Document Details
- Document Type
- Technical Report
- Publication Date
- Sep 01, 1998
- Accession Number
- ADB244889
Entities
People
- John Katzenellenbogen
Organizations
- University of Illinois Urbana–Champaign