白杨素Mannich碱衍生物的合成及其抗癌活性

目的设计合成新型白杨素Mannich碱衍生物,并寻求具有抗癌活性的新化合物。方法利用Baker-Venkataraman重排法完成白杨素的全合成,再与甲醛、胺类进行Mannich缩合反应得到目标化合物。采用MTT法,以5-氟尿嘧啶为阳性对照,评价目标化合物对人宫颈癌细胞(Hela)、人肺腺癌细胞(A549)、人胃癌细胞(SGC-901)、人结肠癌细胞(HCT-116)、人白血病细胞(K562)5种肿瘤细胞的抗癌活性。结果与结论合成了10个未见文献报道的新化合物,其结构经1H-NMR、IR和MS确证。体外抗癌活性实验表明,部分化合物显示出较好的抗癌活性。

Synthesis and antitumor activities of mannich base derivatives of chrysin

Objective To design and synthesize new mannich base derivatives of chrysin and evaluate their antitumor activities. Methods Chrysin was total synthesized by Baker-Venkataraman rearrangement. The target compounds were synthesized at C-8 in A-ring via Mannich reaction with chrysin as leading compound. Taking fluorouracil as reference, their antitumor activities were evaluated by MTT method. Results and Conclusions Ten new aminomethylation compounds are synthesized and their structures are confirmed by ¹H-NMR, IR and MS. The results of primary pharmacological tests indicate that some of new compounds have moderate inhibitory effects on Hela(human cervical carcinoma cell line), A549(human lung adenocarcinoma cell line ), SGC-7901 (human gastric cancer cell line), HCT-116(human colon cancer cell line), K562(human leukemia cell line).