Induction of apoptosis by aryl-substituted diamines: role of aromatic group substituents and distance between nitrogens.
A series of aromatic substituted diamines was synthesized and characterized for their cytotoxic profiles against human breast and prostate tumor cell lines. Following a structure function analysis of the effects of changes of the benzyl substituents and the distance between amino groups the most potent analogues were analyzed biologically and were shown to induce apoptosis. These compounds do not induce the enzyme SSAT or deplete intracellular polyamine levels, mechanisms demonstrated by other cytotoxic polyamine analogues.
Burns
Mark R
MR
MediQuest Therapeutics, Inc., 4010 Stone Way North, Seattle, WA 98103, USA. markburns@mqti.com
LaTurner
Solveig
S
Ziemer
Josh
J
McVean
Maralee
M
Devens
Bruce
B
Carlson
C Lance
CL
Graminski
Gerard F
GF
Vanderwerf
Scott M
SM
Weeks
Reitha S
RS
Carreon
Jay
J
D017209:Apoptosis / Q000187:drug effects*; D003959:Diamines / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009584:Nitrogen / Q000737:chemistry*; D014407:Tumor Cells, Cultured
D003959:Diamines; D009584:Nitrogen