Graduate School of Science and Technology, Shizuoka University, Naka-ku, Hamamatsu 432-8561, Japan.
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5943-6. doi: 10.1016/j.bmcl.2010.01.061. Epub 2010 Jan 21.
4-Bromo-3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (3c) was first synthesized from 3,4-dimethyl-1-phenyl-2-phospholene 1-oxide (2c) by a bromo-radical substitution reaction occurred at C-4 position by N-bromosuccinimide and 2,2'-azobisisobutyronitrile. The novel phospha sugar analogue 3c exerted high anti-proliferative effect on U937 cells evaluated by MTT in vitro methods and was much more efficient than that of Gleevec, which is known as a molecule targeting chemotherapeutical agent. The substitution of 2-phospholenes at C-3 and C-4 position with methyl groups as well as 4-bromo substituent suggests a good anti-proliferative effect.
4-溴-3,4-二甲基-1-苯基-2-磷杂环戊烯 1-氧化物（3c）首先由 3,4-二甲基-1-苯基-2-磷杂环戊烯 1-氧化物（2c）通过 N-溴代丁二酰亚胺和 2,2'-偶氮二异丁腈在 C-4 位发生溴自由基取代反应合成。新型磷酰胺糖类似物 3c 通过 MTT 体外方法评估对 U937 细胞表现出高的增殖抑制作用，其效率明显高于已知的靶向化疗药物格列卫。2-磷杂环戊烯在 C-3 和 C-4 位用甲基取代以及 4-溴取代基表明具有良好的增殖抑制作用。
