Participation of the beta-hydroxyketone part for potent cytotoxicity of callystatin A, a spongean polyketide

Citation
N. Murakami et al., Participation of the beta-hydroxyketone part for potent cytotoxicity of callystatin A, a spongean polyketide, BIO MED CH, 9(1), 2001, pp. 57-67
Citations number
21
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
0968-0896 → ACNP
Volume
9
Issue
1
Year of publication
2001
Pages
57 - 67
Database
ISI
SICI code
0968-0896(200101)9:1<57:POTBPF>2.0.ZU;2-7
Abstract
The participation of the beta -hydroxyketone part of callystatin A in the p otent cytotoxicity was analyzed through the analogue-syntheses and the asse ssment of their biological potencies. The ketonic carbonyl, the 19-hydroxyl , and the three asymmetric methyl groups located in the beta -hydroxyketone part of callystatin A were revealed to contribute to the cytotoxic potency , respectively. Moreover, the alpha,beta -unsaturated delta -lactone portio n was shown to serve as a conclusive functional group for the cytotoxic act ivity. (C) 2000 Elsevier Science Ltd. All rights reserved.