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 language | English |
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Pages (from-to) | 673-677 |
Number of pages | 5 |
Journal | ACS Medicinal Chemistry Letters |
Volume | 3 |
Issue number | 8 |
DOIs | |
Publication status | Published - 2012 Aug 9 |
Keywords
- Cortistatin A
- analogue synthesis
- antiangiogenesis
- marine sponge
- structure-activity relationship
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry