| RRC ID |
10808
|
| Author |
Bazin MA, Le Lamer AC, Delcros JG, Rouaud I, Uriac P, Boustie J, Corbel JC, Tomasi S.
|
| Title |
Synthesis and cytotoxic activities of usnic acid derivatives.
|
| Journal |
Bioorg Med Chem
|
| 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.
|
| Volume |
16(14)
|
| Pages |
6860-6
|
| Published |
2008-7-15
|
| DOI |
10.1016/j.bmc.2008.05.069
|
| PII |
S0968-0896(08)00511-7
|
| PMID |
18558490
|
| MeSH |
Animals
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry*
Apoptosis / drug effects
Benzofurans / chemical synthesis
Benzofurans / chemistry*
Benzofurans / pharmacology*
CHO Cells
Carrier Proteins
Cell Line, Tumor
Cricetinae
Cricetulus
Humans
Mice
Polyamines
Structure-Activity Relationship
|
| IF |
3.073
|
| Times Cited |
53
|
|
WOS Category
|
CHEMISTRY, MEDICINAL
CHEMISTRY, ORGANIC
BIOCHEMISTRY & MOLECULAR BIOLOGY
|
| Resource |
| Human and Animal Cells |
U251(RCB0461) |
