β-锗代-α-氨基酸衍生物的合成及抗肿瘤活性

自六十年代初期发现羧乙基锗倍半氧化物(Ge—132)广泛的生物活性以来,已有许多相应的有机锗化合物被发现,在抗肿瘤活性方面,因有毒性较低、抗瘤谱广等一系列优点而引起人们广泛的兴趣,但由于活性较低影响了应用及发展,据文献报道,有机锗倍半氧

Synthesis and antitumor activity of beta-germanyl-alpha-amino acid derivatives]

Some beta-germanyl-alpha-amino acid derivatives were prepared from the reaction of HGeCl3 with substituted oxazolines. The compositions of the above compounds were studied using IR, element analysis and so on. Experimental results were as follows: for 1-substituted-2-amino-2-carboxyethylgermanium susquioxide (such as IIIb), the po LD50 for mice was found to be above 10 g/kg. When given ip, a maximum inhibition of 50% of the growth of S180 was obtained for IIIb, whereas an inhibition of 42% was achieved for 5-Fu under the same experimental condition.