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 Chemjournal_title
Bioorganic & medicinal chemistryauthors
Bazin MA,Le Lamer AC,Delcros JG,Rouaud I,Uriac P,Boustie J,Corbel JC,Tomasi Sdoi
10.1016/j.bmc.2008.05.069subject
Has Abstractpub_date
2008-07-15 00:00:00pages
6860-6issue
14eissn
0968-0896issn
1464-3391pii
S0968-0896(08)00511-7journal_volume
16pub_type
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