Studies directed toward the elucidation of the pharmacophore of steroid-based sonic hedgehog signaling inhibitors Academic Article uri icon

Overview

MeSH Major

  • Hedgehog Proteins
  • Signal Transduction
  • Steroids

abstract

  • Previous work from our laboratory has established that the readily available steroid-based analog 2 of cyclopamine 1 is, like 1, a highly potent inhibitor of Hedgehog signaling. The first structure-activity relationship studies on 2, i.e., the synthesis and biological evaluation of both the C-17 epi analog 4 and the C-3 deoxy analog 11, both of which are more potent than cyclopamine 1, are described. The implications of these results for the emerging pharmacophore of these Sonic Hedgehog signaling inhibitors are discussed.

publication date

  • October 7, 2011

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC3184309

Digital Object Identifier (DOI)

  • 10.1021/ol202020c

PubMed ID

  • 21905689

Additional Document Info

start page

  • 5140

end page

  • 3

volume

  • 13

number

  • 19