MEDI 311 |
| Phenoxazines are known for anti-multidrug resistance (MDR) activities. We hypothesize that by increasing the alkyl side chain length, the derivative's potency as anticancer agent will increase. We are synthesizing and characterizing a series of seven hydrophobic N-substituted phenoxazines with a six carbon alkyl side chain and different amino functionalities. Each synthesis is based on the ability of N-(10-chloroalkyl)phenoxazines to undergo iodide catalyzed nucleophilic substitution reactions with secondary amines such as N,N-diethylamine, N-diethanolamine, pyrrolidine, piperidine, morpholine, thiomorpholine, and (â-hydroxyethyl)piperazine. The products are characterized by UV, IR, 1H and 13C NMR, mass spectral and elemental data. The lipophilicities are to be determined. The purified compounds also are to be evaluated for anticancer activity. In this study, in addition to the synthesis of seven hexylamino phenoxazine derivatives, we plan to determine their IC50 and screen them for inhibition of the phosphorylation of AKT and downstream targets. Acknowledgement: We thank the NIH (AREA grant # 5-20860) for support |
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Poster Session
7:00 PM-9:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster
Division of Medicinal Chemistry |