Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 1, Pages 683-688Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.10.054
Keywords
Marine cyanobacteria; Natural products; Lipopeptide; Anticancer; Spectroscopy
Categories
Funding
- NIH [CA 52955, NS 053398]
- NIH/NCI [CA100851]
- NATIONAL CANCER INSTITUTE [U19CA052955, U01CA052955, R01CA100851] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE [R01NS053398] Funding Source: NIH RePORTER
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Bioassay-guided fractionation of two cyanobacterial extracts from Papua New Guinea has yielded hoiamide D in both its carboxylic acid and conjugate base forms. Hoiamide D is a polyketide synthase (PKS)/non-ribosomal peptide synthetase (NRPS)-derived natural product that features two consecutive thiazolines and a thiazole, as well as a modified isoleucine residue. Hoiamide D displayed inhibitory activity against p53/MDM2 interaction (EC50 = 4.5 mu M), an attractive target for anticancer drug development. (C) 2011 Elsevier Ltd. All rights reserved.
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