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公开(公告)号：US09029394B2
公开(公告)日：2015-05-12
申请号：US13892545
申请日：2013-05-13
发明人： Sheng-Chu Kuo , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
IPC分类号： C07D215/233 , C07F9/6561 , C07D421/04 , C07F9/60 , C07D491/056
CPC分类号： C07F9/6561 , C07D215/233 , C07D421/04 , C07D491/056 , C07F9/60
摘要： 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.
摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠 盐。 初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。 还合成了2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和N，N-二烷基氨基烷基衍生物。 这些新型中间体显示出显着的抗癌活性。
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公开(公告)号：US20130252999A1
公开(公告)日：2013-09-26
申请号：US13892545
申请日：2013-05-13
发明人： Sheng-Chu KUO , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
IPC分类号： C07D215/233 , C07D491/056
CPC分类号： C07F9/6561 , C07D215/233 , C07D421/04 , C07D491/056 , C07F9/60
摘要： 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.
摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠 盐。 初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。 还合成了2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和N，N-二烷基氨基烷基衍生物。 这些新型中间体显示出显着的抗癌活性。
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3.发明授权Hydrophilic derivatives of 2-selenophene-4-quinolones as anticancer agents 有权2-硒吩-4-喹诺酮的亲水性衍生物作为抗癌剂公开(公告)号：US09023867B2
公开(公告)日：2015-05-05
申请号：US13892576
申请日：2013-05-13
发明人： Sheng-Chu Kuo , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
IPC分类号： C07D421/04 , C07F9/6561 , C07F9/60 , C07D215/233 , C07D491/056
CPC分类号： C07F9/6561 , C07D215/233 , C07D421/04 , C07D491/056 , C07F9/60
摘要： 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.
摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠 盐。 初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。 还合成了2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和N，N-二烷基氨基烷基衍生物。 这些新型中间体显示出显着的抗癌活性。
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公开(公告)号：US09023866B2
公开(公告)日：2015-05-05
申请号：US13892522
申请日：2013-05-13
发明人： Sheng-Chu Kuo , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
IPC分类号： C07D421/04 , C07F9/6561 , C07F9/60 , C07D215/233 , C07D491/056
CPC分类号： C07F9/6561 , C07D215/233 , C07D421/04 , C07D491/056 , C07F9/60
摘要： 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.
摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠 盐。 初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。 还合成了2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和N，N-二烷基氨基烷基衍生物。 这些新型中间体显示出显着的抗癌活性。
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公开(公告)号：US20130253006A1
公开(公告)日：2013-09-26
申请号：US13892522
申请日：2013-05-13
发明人： Sheng-Chu KUO , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
IPC分类号： C07D421/04
CPC分类号： C07F9/6561 , C07D215/233 , C07D421/04 , C07D491/056 , C07F9/60
摘要： 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.
摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠 盐。 初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。 还合成了2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和N，N-二烷基氨基烷基衍生物。 这些新型中间体显示出显着的抗癌活性。
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