Abstract
Exploitation of the polyamine backbone as a vector for intracellular transport of various pharmacophores has focused largely on fixing the cargo molecule to one of the nitrogens in the linear chain. This communication describes the assembly of a model aminopolyamine analogue, 6-amino-N(1),N(12)-diethylspermine, and its biological properties. This amino polyamine presents an additional site of attachment for cargo molecules, reduces cell growth, and achieves cellular concentrations that are higher than those of N(1),N(12)-diethylspermine.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Acetyltransferases / metabolism
-
Adenosylmethionine Decarboxylase / metabolism
-
Animals
-
Antineoplastic Agents / chemical synthesis*
-
Antineoplastic Agents / pharmacokinetics
-
Antineoplastic Agents / pharmacology
-
Biological Transport
-
Cell Line, Tumor
-
Cell Proliferation / drug effects
-
Ornithine Decarboxylase / metabolism
-
Spermine / analogs & derivatives*
-
Spermine / chemical synthesis*
-
Spermine / pharmacokinetics
-
Spermine / pharmacology
-
Stereoisomerism
-
Structure-Activity Relationship
Substances
-
Antineoplastic Agents
-
Spermine
-
Acetyltransferases
-
diamine N-acetyltransferase
-
Ornithine Decarboxylase
-
Adenosylmethionine Decarboxylase