China Medical University

Chih-Shiang Chang

Sheng-Chu Kuo

Che-Ming Teng

Shiow-Lin Pan

Kuo-Hsiung Lee

Tian-Shung Wu

Chung-Ming Sun

Li-Jiau Huang

Jai-Sing Yang

Li-Chen Chou

Tzong-Der Way

Jing-Gung Chung

Jang-Chang Lee

Chien-Ting Chen

Ching-Che Huang

Shih-Ming Huang

Jih-Hwa Guh

Kai-Wei Chang

Wei-Ling Chang

Ching-Shih Chen

Hsiang-Wen Lin

Ju-Fang Liu

Po-Chen Chu

The invention provides a novel class of propiolylamide-based irreversible inhibitors of PKM2 compounds of the general formula I, pharmaceutical compositions, and methods of inducing an anti-tumor effect in a subject suffering from tumor comprising administering to the subject a pharmaceutical composition comprising an effective amount of compound of formula I.

Irreversible inhibitors of pyruvate kinase M2 and the use thereof

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(Naform) 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-phenyl-4-quinolones as anticancer agents

2-selenophene-4-quinolones as anticancer agents

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 (Naform) 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.

Hydrophilic derivatives of 2-selenophene-4-quinolones as anticancer agents

Benzimidazole compounds of formula (I): wherein R, R, R, R, R, X, Y, Z, and Zare defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.

Benzimidazole compounds and their use as anticancer agents

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 &#x39b;/, &#x39b;/-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

Hydrophilic derivatives of 2-aryl-4-quinolones as anticancer agents

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Taichung, Taiwan

Chih-Shiang Chang