China Medical University

National Science Council

Yung Shin Pharmaceutical Ind. Co., Ltd.

Yung Shin Pharm. Ind. Co., Ltd.

Tairx, Inc.

Li-Jiau Huang

Sheng-Chu Kuo

Che-Ming Teng

Kuo-Hsiung Lee

Jai-Sing Yang

Li-Chen Chou

Tian-Shung Wu

Tzong-Der Way

Shiow-Lin Pan

Jing-Gung Chung

Chung-Ming Sun

Chih-Shiang Chang

Jang-Chang Lee

Chien-Ting Chen

Ching-Che Huang

Shih-Ming Huang

Fang-Yu Lee

Hui-Yi Lin

Mei-Hua Hsu

Jih-Hwa Guh

Chun-Jen Chen

Chi-Hung Huang

Mann-Jen Hour

Min-Tsang Hsieh

Hsin-Yi Hung

Ling-Chu Chang

Chin-Yu Liu

Ya-Ling Fang

Ya-Yun Lai

Hua-Sin Chen

Mei-Ling Shih

Mei-Chi Fang

Shi-Hong Zhuang

Meng-Tung Tsai

Huei-Wen Chen

Yung-Yi Cheng

Min-tsang Hsieh

Hui-yi Lin

Huei-Wan Chen

The present invention provides a series of derivatives of stilbenoid which are useful as new inhibitory agents against head and neck squamous cell carcinoma (HNSCC) and hepatoma.

Stilbenoid compound as inhibitor for squamous carcinoma and hepatoma and uses 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

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

Novel compounds of 2-(substituted arylmethyl)-3-(substituted phenyl)-2H-indazoles and 1-(substituted arylmethyl)-3-(substituted phenyl)-1H-indazoles are synthesized, and useful as anti-angiogenic agents.

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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

Substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives and their salts were synthesized. The results of preliminary screening revealed that these compounds are potent in killing solid tumor cancers.

Substituted 2-phenyl-4-quinolone-3-carboxylic acid compounds and their use as antitumor agents

Two series of 6,7,2&prime;,3&prime;,4&prime;,5&prime;-substituted 2-phenyl-4-quinazolinones and 6,2&prime;,3&prime;,4&prime;,5&prime;-substituted 2,3-dihydro-2-phenyl-4-quinazolinones are synthesized and evaluated for cytotoxicity against a panel of human tumor cell lines, such as epidermoid carcinoma of the nasopharynx (KB), lung carcinoma (A-549), ileocecal carcinoma (HCT-8), breast cancer (MCF-7), melanoma (SKMEL-2), ovarian cancer (1A9), glioblastoma (U-87-MG), bone (HOS), P-gp-expressing epidermoid carcinoma of the nasopharynx (KB-VIN), and prostate cancer (PC3) cell lines, and some of the compounds are found potent. The present invention also synthesizes 2-phenyl-4-alkoxy-quinazoline compounds, wherein some of the compounds exhibit antiplatelet activity.

2-phenyl-4-quinazolinone compounds, 2-phenyl-4-alkoxy-quinazoline compounds and their pharmaceutical compositions

The present invention provides a novel series of 2,3,4,5-substituted furo[2,3-c]pyrazole compounds. These compounds are found potent in inhibiting thrombocyte aggregation and antiallergy effect.

2,3,4,5-substituted furo[2,3-c]pyrazole derivatives

Growing community of inventors

Taichung, Taiwan

Li-Jiau Huang