Design and synthesis of inhibitors of hedgehog signaling based on the alkaloid cyclopamine Academic Article uri icon

Overview

MeSH Major

  • Drug Design
  • Hedgehog Proteins
  • Signal Transduction
  • Veratrum Alkaloids

abstract

  • The synthesis and biological evaluation of structurally simplified, metabolically stable cyclopamine-like Sonic Hedgehog (SHH) signaling inhibitors, i.e., 5, is described in four chemical steps from commercially available steroidal precursors. Biological evaluation of this cyclopamine analogue in two different systems establishes the high potency of 5 as a SHH signaling inhibitor. This approach provides important new lead structures for the development of new cancer chemotherapeutic agents based on the inhibition on SHH signaling.

publication date

  • July 2, 2009

Research

keywords

  • Academic Article

Identity

Language

  • eng

Digital Object Identifier (DOI)

  • 10.1021/ol900974u

PubMed ID

  • 19552464

Additional Document Info

start page

  • 2824

end page

  • 7

volume

  • 11

number

  • 13