1. Academic Validation
  2. Induction of apoptosis by aryl-substituted diamines: role of aromatic group substituents and distance between nitrogens

Induction of apoptosis by aryl-substituted diamines: role of aromatic group substituents and distance between nitrogens

  • Bioorg Med Chem Lett. 2002 May 6;12(9):1263-7. doi: 10.1016/s0960-894x(02)00156-7.
Mark R Burns 1 Solveig LaTurner Josh Ziemer Maralee McVean Bruce Devens C Lance Carlson Gerard F Graminski Scott M Vanderwerf Reitha S Weeks Jay Carreon
Affiliations

Affiliation

  • 1 MediQuest Therapeutics, Inc., 4010 Stone Way North, Seattle, WA 98103, USA. [email protected]
Abstract

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.

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