Identification from a combinatorial library of a small molecule that selectively induces apoptosis in cancer cells.
The selective induction of death in cancer cells is a major challenge in modern medicine. In this communication we describe the synthesis of an 88-membered combinatorial library, and the subsequent evaluation of these compounds for their ability to selectively induce apoptosis in cancerous cells. A compound was identified from the library that induces apoptosis in U-937 and HL-60 cell lines. This compound is a remarkably selective pro-apoptotic agent for these cancer cell lines, as it does not induce significant death in noncancerous white blood cells, even at concentrations as high as 1000 muM.
Nesterenko
Vitaliy
V
Department of Chemistry, Roger Adams Laboratory, University of Illinois, Urbana, IL 61801, USA.
Putt
Karson S
KS
Hergenrother
Paul J
PJ
D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001555:Benzene Derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D002234:Carbodiimides / Q000138:chemical synthesis / Q000494:pharmacology; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D020298:U937 Cells
D000588:Amines; D001555:Benzene Derivatives; D002234:Carbodiimides; D002264:Carboxylic Acids