title: In vitro and in vivo evaluation of select kahalalide F analogs with antitumor and antifungal activities.
abstract: 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.
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, The University of Mississippi, University, MS 38677, United States.
authors.forename: Abbas Gholipour
authors.initials: AG
authors.lastname: Shilabin
authors.forename: Mark T
authors.initials: MT
authors.lastname: Hamann
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D047630:Depsipeptides / Q000737:chemistry* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D000970:Antineoplastic Agents; D047630:Depsipeptides; C097897:kahalalide F