Creation of readily accessible and orally active analogue of cortistatin A

Naoyuki Kotoku, Yuji Sumii, Takeshi Hayashi, Satoru Tamura, Takashi Kawachi, Sho Shiomura, Masayoshi Arai, Motomasa Kobayashi

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)

Abstract

Syntheses of structurally simplified analogues of cortistatin A (1), a novel antiangiogenic steroidal alkaloid from Indonesian marine sponge, and their biological activities were investigated. The analogues were designed by considering the 3-D structure of 1. Compound 30, in which the isoquinoline moiety was appended to the planar tetracyclic core structure, showed potent antiproliferative activity against human umbilical vein endothelial cells (HUVECs) together with high selectivity and also showed in vivo antiangiogenic activity and significant antitumor effect by oral administration.

Original languageEnglish
Pages (from-to)673-677
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume3
Issue number8
DOIs
Publication statusPublished - 2012 Aug 9

Keywords

  • Cortistatin A
  • analogue synthesis
  • antiangiogenesis
  • marine sponge
  • structure-activity relationship

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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