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Four novel dicyelic arene-homospermidine conjugates (6a-d) were synthesized and evaluated for cytotoxicity in L1210,α- difluoromethylomithine (DFMO) treated L1210,melanoma B16,spermidine (SPD) treated B16,and Hela cells.In the DFMO- treated L1210 experiments,6a-d were more sensitive to DFMO than naphthalene-homospermidine (6e),suggesting that 6a-d can utilize the polyamine transporter (PAT) to enter the cells as well as 6e.The diminished cytotoxicity in the SPD/B16 experiments also supported this conclusion.In summary,the homospermidine is an efficacious vector to ferry dicyclic arches into cells via PAT.
Four novel dicyelic arene-homospermidine conjugates (6a-d) were synthesized and evaluated for cytotoxicity in L1210, α-difluoromethylomithine (DFMO) treated L1210, melanoma B16, spermidine (SPD) treated B16, and Hela cells. The DFMO-treated L1210 experiments that 6a-d were more sensitive to DFMO than naphthalene-homospermidine (6e), suggesting that 6a-d can utilize the polyamine transporter (PAT) to enter the cells as well as 6e. diminished cytotoxicity in the SPD / B16 experiments also supported this conclusion. In summary, the homospermidine is an efficacious vector to ferry dicyclic arches into cells via PAT.