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Creation of readily accessible and orally active analogue of cortistatin a.

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.

SUBMITTER: Kotoku N

PROVIDER: S-EPMC4025756 | biostudies-literature | 2012 Aug

REPOSITORIES: biostudies-literature

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Creation of readily accessible and orally active analogue of cortistatin a.

Kotoku Naoyuki N Sumii Yuji Y Hayashi Takeshi T Tamura Satoru S Kawachi Takashi T Shiomura Sho S Arai Masayoshi M Kobayashi Motomasa M

ACS medicinal chemistry letters 20120710 8

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 sh ...[more]

PMID: 24900528

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