MEDI 78 |
| Nuclear receptors (NRs) regulate the expression of responsive genes and thereby affect diverse processes, including cell growth, development, and metabolism. Numerous field of medicines, including cancer, reproductive biology, and metabolic syndrome are target to NRs. Some natural ligands of NRs have steroidal (or secosteroidal) structure. For example, most of so far known vitamin D receptor (VDR) ligands contain secosteroidal structure, those are unstable to heat and light. Only a few vitamin D agonists, including a bis-phenol derivative LG190178, are known as non-secosteroidal derivatives. Based on these bis-phenol skeletons, we prepared several diphenylmethane derivatives containing nitrogen atom(s). Interestingly, some of these compounds showed specific binding affinity toward not VDR but androgen receptor (AR) selectively, and elicited androgen-antagonistic activity. It means that diphenylmethane skeleton may be a steroid skeleton substitute, which has many advantages over a steroid skeleton. In this presentation, the structure-activity relationships toward VDR and AR will be discussed. |
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General Poster Session
7:00 PM-9:00 PM, Sunday, 10 September 2006 Moscone Center -- Hall D, Poster
Division of Medicinal Chemistry |