Solid phase organic synthesis of polyamine derivatives and initial biological evaluation of their antitumoral activity.
A series of N1-monosubstituted putrescine and spermine derivatives was synthesised using a solid phase methodology. We evaluated their cytotoxicity, calmodulin antagonism and polyamine uptake inhibition, pharmacological properties shared by some antitumoral agents.
Tomasi
S
S
Pharmacochimie de Molécules de Synthèse et de Produits Naturels, Faculté de Pharmacie, Rennes, France.
Le Roch
M
M
Renault
J
J
Corbel
J C
JC
Uriac
P
P
Carboni
B
B
Moncoq
D
D
Martin
B
B
Delcros
J G
JG
D006631:Amine Oxidase (Copper-Containing); D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002147:Calmodulin / Q000037:antagonists & inhibitors; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D003641:Deamination; D007939:Leukemia L1210 / Q000378:metabolism / Q000473:pathology; D008956:Models, Chemical; D010084:Oxidation-Reduction; D000587:Oxidoreductases Acting on CH-NH Group Donors / Q000378:metabolism; D011700:Putrescine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D013096:Spermine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D002147:Calmodulin; D013096:Spermine; D006631:Amine Oxidase (Copper-Containing); D000587:Oxidoreductases Acting on CH-NH Group Donors; D011700:Putrescine