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目的:合成哌啶酮类法尼基转移酶抑制药,并且评价其抗肿瘤活性。方法:在其他基团保持最佳的基础上,哌啶酮环的1-位氮原子上用咪唑基、羧基和取代氨基等不同的基团取代得到目标化合物,用MTT法检测它们抑制人Raji细胞的IC_(50)值,比较它们对肿瘤细胞的抑制活性。结果:合成出了9个哌啶酮类新化合物,抗肿瘤生物活性实验结果表明9个目标化合物都有抑瘤活性。结论:用不同的基团取代哌啶-2-酮衍生物1位N后活性有一定的改变,能够与锌离子结合的基团活性较高,表明该位置上基团可能是与酶分子中的锌离子作用。
OBJECTIVE: To synthesize piperidinoid farnesyl transferase inhibitors and to evaluate their anti-tumor activity. Methods: The target compounds were obtained by substituting different groups such as imidazolyl group, carboxyl group and substituted amino group on the nitrogen atom of 1-position of piperidone ring on the basis of keeping the best of other groups. Their inhibitory effects on human Raji The IC50 values of the cells were compared for their inhibitory activity on tumor cells. Results: Nine new piperidinones were synthesized. The antitumor activity showed that all 9 target compounds had antitumor activity. CONCLUSION: The activity of the piperidine-2-one derivatives substituted by different groups is changed slightly after 1-position N, and the group capable of binding with zinc ion has a higher activity, indicating that the group at this position may be related to the enzyme molecule Zinc ion effect.