含α-氨基酸的新型有机锗化合物的合成与生物活性研究

Syntheses of Novel Organogermanium Compounds Containing α-Amino Acid and Studies on the Antitumor Activity

设计合成了两个系列20个含α-氨基酸的新型有机锗化合物,对化合物进行了波谱表征,用X射线衍射测定了化合物Ph3GeCH(Ph)CH2CONHCH(CH2COOC2H5)COOC2H5的晶体结构.抗肿瘤实验结果表明,这两个系列的化合物有一定的抗KB,HCT-8和Bel-7402活性.

In order to search new organogermanium antitumor drugs with an activity and low toxicity, 20 new organogermanium compounds were designed and synthesized by attaching α-amino acid to organogermanium moieties. Their structures were confirmed by IR, 1H NMR and elemental analysis. The crystal structure of Ph3GeCH（Ph） CH2CONHCH （ CH2COOC2H5 ） COOC2H5 were determined by X-ray diffraction. Three human neoplastic cell lines（KB, HCT-8 and Bel-7402） were used to screen these compounds. The results indicate that some compounds at 5 μmol/L show a weak in vitro antitumor activity.