酚类天然产物Buxifoximes A的合成及生物活性

Total synthesis and biological evaluation of phenolic natural product Buxifoximes A

摘要:

利用商品化试剂4-羟基苯甲酰甲醛水合物(3)为起始原料，与甲氧基胺盐酸盐经一步肟化反应，以79%的收率合成了酚类天然产物Buxifoximes A(1). 同时还经已知反应步骤合成了Buxifoximes A的天然类似物2. 初步的抗肿瘤生物活性测试表明，二者对MV4-11细胞表现出了优秀的抑制作用，同时探讨了构效关系.

Abstract:

Compound 4-hydroxyphenylglyoxal hydrate was chosen as starting material, which can react with N-methoxylamine hydrochloride in one step of oximation reaction, affording phenolic natural product buxifoximes A in yield of 79%. Meanwhile, we also synthesized compound 2, a natural analogue of Buxifoximes A, according to a known procedure. Furthermore, the inhibitory effect of compound and compound 2 on cancer cell proliferation was evaluated and found to possess potent inhibitory activity against MV4-11. Meanwhile, preliminary structure–activity relationships for these two compounds are discussed.