%0 Journal Article
%A Shilabin, Abbas Gholipour
%A Kasanah, Noer
%A Wedge, David E.
%A Hamann, Mark T.
%D 2007
%T Lysosome and HER3 (ErbB3) Selective Anticancer Agent Kahalalide F: Semisynthetic
Modifications and Antifungal Lead-Exploration Studies
%U https://acs.figshare.com/articles/journal_contribution/Lysosome_and_HER3_ErbB3_Selective_Anticancer_Agent_Kahalalide_F_Semisynthetic_Modifications_and_Antifungal_Lead_Exploration_Studies/2986690
%R 10.1021/jm061288r.s001
%2 https://acs.figshare.com/ndownloader/files/4687369
%K cancer cell lines
%K antifungal activity
%K analogue
%K HER
%K II
%K phase
%K NCI 60 cell panel
%X Kahalalide F (1) shows remarkable antitumor activity against different carcinomas and has recently completed
phase I clinical trials and is being evaluated in phase II clinical studies. The antifungal activity of this
molecule has not been thoroughly investigated. In this report, we focused on acetylation and oxidation of
the secondary alcohol of threonine, as well as reductive alkylation of the primary amine of ornithine, and
each product was evaluated for improvements in antifungal activity. 1 and analogues do not exhibit
antimalarial, antileishmania, or antibacterial activity; however, the antifungal activity against different strains
of fungi was particularly significant. This series of compounds was highly active against Fusarium spp.,
which represents an opportunistic infection in humans and plants. The in vitro cytotoxicity for the new
analogues of 1 was evaluated in the NCI 60 cell panel. Analogue 5 exhibited enhanced potency in several
human cancer cell lines relative to 1.
%I ACS Publications