摘要
以色氨酸甲酯盐酸盐、三氟乙酸和三苯基膦为原料,在四氯化碳溶剂中用一锅法在β-咔啉母核中引入三氟甲基,并通过酯的氨解反应合成一系列新型含氟β-咔啉类衍生物,其结构经IR、MS1、H-NMR和13C-NMR确证。初步体外活性实验表明,所合成的化合物具有一定的抗肿瘤活性和对单胺氧化酶的抑制活性。
Using tryptophan methyl ester hydrochloride, trifluoroacetic acid and triphenylphosphine as starting materials, trifluoromethyl group was introduced to the β-carbolines in tetrachloromethane solvent by one-pot method and then a series of fluorinated β-carboline compounds never reported in the literature were synthesized by the aminolysis of intermediate ester. Their structures were all characterized by IR, MS, ^1H- NMR and ^13C-NMR. Their anti-tumor activities were tested by MTT method and their inhibition activity on monoamine oxidase were also tested. The pharmacological tests of fluorinated β-carbolines in vitro showed that they exhibited inhibition activity on tumour cell and monoamine oxidase in some extent.
出处
《中国药物化学杂志》
CAS
CSCD
2007年第2期111-113,共3页
Chinese Journal of Medicinal Chemistry
基金
浙江省自然科学基金项目(Y405113)
关键词
含氟β-咔啉类衍生物
一锅法
氨解反应
抗肿瘤活性
单胺氧化酶抑制活性
fluorinated β-carboline derivatives
one-pot method
aminolysis reaction
antitumor activity
monoamine oxidase inhibitory activity
