Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 22, Pages 6628-6632Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.06.050
Keywords
Kahalalide F; Anti-cancer; Anti-infective; Structure-activity relationship; Marine natural products
Funding
- 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]
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available
Share Paper
