期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 22, 页码 6628-6632出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.06.050
关键词
Kahalalide F; Anti-cancer; Anti-infective; Structure-activity relationship; Marine natural products
资金
- national institute of health of the United States of America [R01AI36596]
- NIH, NIAID, division of aids [AI27094]
- USDA agricultural research service [58-6408-2-009]
Kahalalide F (KF) and the regioisomer isoKF are novel anticancer drugs of marine origin and currently under clinical investigation. Here we report the synthesis of two new KF analogs with significant in vitro and in vivo antifungal and antitumor activities. The primary amine hydrogen of ornithine in KF has been replaced with 4-fluoro-3-methylbenzyl and morpholin-4-yl-benzyl via reductive N-alkylation. The TGI of these analogs using the NCI-60 cell line screening revealed promising results when compared to paclitaxel. The result of in vivo hollow fiber and animal toxicity assays are presented. (C) 2011 Elsevier Ltd. All rights reserved.
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