Description:
| Courtesy of Hecht,
Maloney |
Executive Summary
The invention involves a practical
synthesis of the Rsk2 inhibitor and potential antitumor agent SL0101-1 and
analogues.
Background
Recent studies have
demonstrated the role of Rsk in cell survival signaling and promoting cell
survival by regulating the expression and activation of pro-survival proteins
such as CREB. This combination of promoting cell survival and prevention of
apoptosis causes excessive cell survival, leading to diseases such as cancer and
autoimmune disorders. It has been found that Rsk2 is over-expressed in more than
50 percent of human breast cancers, validating the Rsk family as a potential
target for drug design. SL0101 is a known inhibitor of Rsk2 and a valuable
research reagent to the biomedical community.
Invention
Description
The present application discloses an efficient synthetic
route to SL0101 derivatives — several naturally-derived inhibitors of Rsk2 — and
provides a synthetic method for structural analogues.
Applications
The synthetic methods can be used to
produce SL0101 for sale to researchers.
Further
Information
David Maloney and Sidney Hecht, Organic
Letters, 7, 6, 1097 (2005).
