Synthetic studies of cortistatin A analogue from the CD-ring fragment of vitamin D₂

Chem Pharm Bull (Tokyo). 2013;61(10):1024-9. doi: 10.1248/cpb.c13-00375.

Abstract

Syntheses of analogue compounds of cortistatin A (1), an anti-angiogenic steroidal alkaloid from Indonesian marine sponge, were investigated by utilizing the CD-ring fragment of vitamin D₂. The incidental preparation of a new analogue having CD-cis-fused skeleton and its biological evaluation revealed the importance of the CD-trans-fused structure for the potent and selective antiproliferative activity of 1 against human umbilical vein endothelial cells (HUVECs).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Proliferation / drug effects
  • Ergocalciferols / chemistry*
  • Human Umbilical Vein Endothelial Cells
  • Humans
  • Isomerism
  • Molecular Conformation
  • Polycyclic Compounds / chemical synthesis
  • Polycyclic Compounds / chemistry*
  • Polycyclic Compounds / pharmacology
  • Porifera / chemistry
  • Porifera / metabolism

Substances

  • Ergocalciferols
  • Polycyclic Compounds
  • cortistatin A