A series of four novel hydrazine-modified diamine conjugates （7a-b, 8a-b） were synthesized and evaluated for cytotoxicity against Melanoma B 16, α-difluoromethylornithine （DFMO）-treated B 16, spermidine （SPD）-treated B 16, Mouse leukemia L 1210 and Hela cell lines. Both the DFMO-B 16 and SPD-B 16 experiments indicated that conjugates 7a-b and 8a-b could recognize the polyamine transporter （PAT） and enter the cells in part or in whole via PAT, although they were not as efficient as the reference, 9- anthracenemethyl homospermidine （1）. 2007 Chao Jie Wang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
Jun Jun ZhouHao HuangSong Qiang XieYu XiaWangJin ZhaoChao Jie Wang
A series of novel antitumor agents-the solanesylpiperazinotriamine derivatives were designed and synthesized, their structures were confirmed by IR,^ 1H-NMR, MS, and element analysis. The preliminary tests showed that at low micromolar concentrations these compounds exhibited obvious toxicity on tumor cells in vitro, and the synergistic effect on clinical antitumor agent indicated that at noncytotoxic concentrations they also evidently enhanced the curative effect of vincristine.
Chao Jie WANGJian Hong WANGYing GANZhi Yong CHENGang Jun DUJin ZHAO
Four novel dicyclic 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 DFMOtreated L 1210 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/B 16 experiments also supported this conclusion. In summary, the homospermidine is an efficacious vector to ferry dicyclic arenes into cells via PAT.
Peng Fei ChengJian Hong WangSong Qiang XieJin ZhaoChao Jie Wang
