申请人:China Medical University
公开号:US20130244983A1
公开(公告)日:2013-09-19
2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na
+
form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.
2-芳基-4-喹啉酮通过与四苄基焦磷酸盐反应转化为二苄基磷酸盐,然后经过氢化反应,用氢取代二苄基基团,接着与Amberlite IR-120(Na+形式)反应形成二钠盐。初步筛选结果表明,这些磷酸盐具有显著的抗癌活性。另外,还合成了一种新的中间体2-硒吡咯烷-4-喹啉酮和2-苯基-4-喹啉酮的N,N-二烷基氨基烷衍生物。这些新的中间体表现出显著的抗癌活性。