| Abstract
| - Apoptosis, or programmed cell death, is a cellular mechanism used to regulate cell number andeliminate damaged or mutated cells. Concomitant with the initiation of the apoptotic cell signal,chemotherapeutic agents also induce anti-apoptotic factors, such as NF-κB, which compromise the overallefficacy of chemotherapeutic anticancer treatment. Here we describe an adjuvant therapy in which a smallmolecule is used to sensitize cancer cells toward apoptosis induced by chemotherapeutics. Our resultsindicate that the imidazoline 1d modulates the pro-survival NF-κB pathway and selectively sensitizes cancercells toward DNA damaging agents, thus enhancing the overall efficacy of the treatment. Pretreatment ofcancer cells with the noncytotoxic imidazoline 1d (10 nM) resulted in a significant increase in apoptosisand anticancer efficacy of the clinically significant DNA damaging agents camptothecin and cisplatin.Noncancerous cells remained unaffected during this regimen.
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