China Medical University

Yung Shin Pharmaceutical Ind. Co., Ltd.

Tairx, Inc.

Li-Chen Chou

Sheng-Chu Kuo

Jai-Sing Yang

Li-Jiau Huang

Kuo-Hsiung Lee

Che-Ming Teng

Shiow-Lin Pan

Tian-Shung Wu

Tzong-Der Way

Jing-Gung Chung

Chung-Ming Sun

Chih-Shiang Chang

Shih-Ming Huang

Ching-Che Huang

Chien-Ting Chen

Jang-Chang Lee

Yang-Chang Wu

Mann-Jen Hour

Tai-Lin Chen

Hong-Zin Lee

Po-Wu Gean

Fang-Yu Lee

Jih-Hwa Guh

Chi-Hung Huang

Hui-Yi Lin

Mei-Hua Hsu

Meng-Tung Tsai

Shi-Hong Zhuang

Mei-Chi Fang

Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof:  

2-aryl-4-quinazolinones and their pharmaceutical compositions

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

A compound of Formula I is disclosed as follows: 

Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives

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

The present invention synthesizes a series of selenolo[3,2-c]pyrazole and selenolo[2,3-c]pyrazole derivatives, and discovers their anticancer activity.

Selenolopyrazole derivatives and use thereof as anticancer agents

A fused pyrazolyl compound of the following formula: wherein A, Ar, Ar, R, R, R, and R, are as defined herein. Also disclosed is a pharmaceutical composition containing an effective amount of the above-described fused pyrazolyl compound.

Fused pyrazolyl compound

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Taichung, Taiwan

Li-Chen Chou