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本文叙述了二十三个磷酰胺和磷酰胺酯化合物的合成,以研究其抗肿瘤活性。合成的化合物部分经过了动物筛选。化合物II、III、VII、VIII和XXII对小鼠肉瘤180有明显抑制作用。化合物1对多种动物肿瘤具有显著活性,并已推荐临床试用。
This article describes the synthesis of twenty-three phosphoramidites and phosphoramidite compounds to study their anti-tumor activity. Part of the synthesized compound was subjected to animal screening. Compounds II, III, VII, VIII and XXII have a significant inhibitory effect on mouse sarcoma 180. Compound 1 has significant activity on a variety of animal tumors and has been recommended for clinical trials.