Citation: Peng Fei Cheng, Jian Hong Wang, Song Qiang Xie, Jin Zhao, Chao Jie Wang. The synthesis and bioevaluation of the dicyclic arene-homospermidine conjugates[J]. Chinese Chemical Letters, ;2007, 18(8): 923-925. doi: 10.1016/j.cclet.2007.05.053 shu

The synthesis and bioevaluation of the dicyclic arene-homospermidine conjugates

a Institute of Natural Products & Medicinal Chemistry, College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475001, China;
b Pharmaceutical College, Henan University, Kaifeng 475001, China

Received Date: 13 November 2006

Fund Project: This work is supported by National Natural Science Foundation of China (No. 20472016), and Henan Natural Science Foundations (Nos. 072102330028 and 512001300).

Four novel dicyclic arene-homospermidine conjugates (6a-d) were synthesized and evaluated for cytotoxicity in L1210, α-difluoromethylornithine (DFMO) treated L1210, melanoma B 16, spermidine (SPD) treated B 16, 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/B 16 experiments also supported this conclusion. In summary, the homospermidine is an efficacious vector to ferry dicyclic arenes into cells via PAT.
- Polyamine conjugate,
- Synthesis,
- Bioevalution
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