Synthesis and antitumor activity of selenophosphocholine analogues containing tegafur / 药学学报
Zhong-Lin ZANG; Shao-Qiong LIU; Xiong CHEN; Yan-Jie LI; Bing ZHOU; Xin-Hua XU.
Acta Pharmaceutica Sinica
; (12): 1184-1187, 2006.
Artículo
en Zh
| WPRIM | ID: wpr-281963
<p><b>AIM</b>To synthesize the selenophosphocholine analogues containing tegafur and test their antitumor activities.</p><p><b>METHODS</b>The cyclic glyceroselenophospholopid conjugate of tegafur was synthesized by the reaction of hexaethylphosphorous triamide with N1-(2-furanidyl)-N3-(hydroxyalkyl)-5-fluyorouracil and 1-O-hexadecyl glycerol as well as selenium in one-pot. Cyclic glyceroselenophospholopid conjugate of tegafur reacted with triethylamine to give title compounds.</p><p><b>RESULTS</b>Six new compounds have been synthesized. Their structures were confirmed by 1H NMR, 13P NMR and elemental analysis. Antitumor activity of the title compounds against PGA1 was tested.</p><p><b>CONCLUSION</b>The reaction of triethylamine with cyclic glyceroselenophospholopid conjugate of tegafur very readily occurred, which was finished within 2 h at room temperature. The opening-ring products of trans isomers showed antimutor activity against human uriaryl bladder cancer cell more effective than that of the tegafur.</p>
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