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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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Shilabin AG,Hamann MT

doi

10.1016/j.bmc.2011.06.050

subject

Has Abstract

pub_date

2011-11-15 00:00:00

pages

6628-32

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(11)00490-1

journal_volume

19

pub_type

杂志文章

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