Synthesis and cytotoxic activities of usnic acid derivatives.

Abstract:

:Nine usnic acid-amine conjugates were evaluated on murine and human cancer cell lines. The polyamine derivatives showed significant cytotoxicity in L1210 cells. Their activities appeared to be independent of the polyamine transport system (PTS). Indeed, their activities were similar in chinese hamster ovary (CHO) and in the PTS deficient CHO-MG cells. In addition, alpha-difluoromethylornithine, an ornithine decarboxylase inhibitor known to indirectly enhance the activity of the PTS and consequently increase the cytotoxicity of cytotoxic drugs entering cells via the PTS, had no effect on the activity of the polyamine derivatives. The more active derivative (1,8-diaminooctane derivative) displayed similar activities on all cancer cell lines studied and induced apoptosis.

journal_name

Bioorg Med Chem

authors

Bazin MA,Le Lamer AC,Delcros JG,Rouaud I,Uriac P,Boustie J,Corbel JC,Tomasi S

doi

10.1016/j.bmc.2008.05.069

subject

Has Abstract

pub_date

2008-07-15 00:00:00

pages

6860-6

issue

14

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)00511-7

journal_volume

16

pub_type

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