CAJ | 학술논문

目的：以Ex-Rad为先导化合物，设计合成具有蛋白酪氨酸激酶（PTK）抑制活性的芳基苄砜类化合物。方法以2-萘酚等为原料，合成中间体3a～3f，用过氧化氢在冰乙酸中将3a～3f氧化成目标化合物4a、4b、5a～5f。用酶联免疫吸附法（ELISA）测定PTK抑制活性，计算抑制率，筛选出具有抑制PTK活性的化合物。结果合成含砜及亚砜类化合物8个，结构经1H NMR确证。活性初筛发现化合物5c的抑制活性明显强于先导化合物。结论合成方法简单，原料廉价易得。 ELISA法测定发现5c的PTK抑制活性较强。
목적：이Ex-Rad위선도화합물，설계합성구유단백락안산격매（PTK）억제활성적방기변풍류화합물。방법이2-내분등위원료，합성중간체3a～3f，용과양화경재빙을산중장3a～3f양화성목표화합물4a、4b、5a～5f。용매련면역흡부법（ELISA）측정PTK억제활성，계산억제솔，사선출구유억제PTK활성적화합물。결과합성함풍급아풍류화합물8개，결구경1H NMR학증。활성초사발현화합물5c적억제활성명현강우선도화합물。결론합성방법간단，원료렴개역득。 ELISA법측정발현5c적PTK억제활성교강。
Objective To use Ex-Rad as a lead compound to design and synthesize aryl benzyl sulfones derivatives with protein tyrosine kinases(PTK) inhibitory activity. Methods 2-Naphthol was used as a raw material to synthesize intermediates 3a-3f. The target compounds 4a, 4d, and 5a-5f were synthesized by oxidizing 3a-3f in acetic acid with H2O2. Enzyme-linked immunosorbent assay(ELISA) was used and inhibition rate was calculated to screen out the compounds with PTK inhibitory activitity. Results Eight compounds containing a sulfone or sulfoxide group were synthesized and the structures were confirmed by 1H NMR. Preliminary evaluation of the 8 compounds demonstrated that the PTK inhibitory activity of 5c was much stronger than that of the lead compound. Conclusion The synthetic method is simple, and the materials are cheap and readily available. 5c shows strong PTK inhibitory activity by ELISA.