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Your search keyword '"Teng-Kuang Yeh"' showing total 15 results
Start Over Author "Teng-Kuang Yeh" Publisher american chemical society
15 results on '"Teng-Kuang Yeh"'

3. Bromomethylthioindole Inspired Carbazole Hybrids as Promising Class of Anti-MRSA Agents

Author

I-Wen Huang, Ching-Fang Yeh, De-Jiun Tsai, Chen-Tso Tseng, Yi-Yu Ke, Amit A. Sadani, Kak-Shan Shia, Chun-Ping Chang, Chia-Yi Cheng, Teng-Kuang Yeh, Chien-Huang Wu, Yu-Wei Liu, Guann-Yi Yu, Jinq-Chyi Lee, Yi-Ping Kuo, Jen-Shin Song, Tsai-Ling Lauderdale, Yi-Wun Jhang, and Lun K. Tsou

Subjects
0301 basic medicine, 030106 microbiology, Biology, medicine.disease_cause, Biochemistry, Enterococcus faecalis, Microbiology, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, Drug Discovery, medicine, 030212 general & internal medicine, Indole test, Strain (chemistry), Carbazole, Organic Chemistry, biochemical phenomena, metabolism, and nutrition, bacterial infections and mycoses, biology.organism_classification, Methicillin-resistant Staphylococcus aureus, In vitro, chemistry, Staphylococcus aureus, Vancomycin, medicine.drug
Abstract

Series of N-substituted carbazole analogues bearing an indole ring were synthesized as anti-methicillin-resistant Staphylococcus aureus (MRSA) agents from a molecular hybridization approach. The representative compound 19 showed an MIC = 1 μg/mL against a panel of MRSA clinical isolates as it possessed comparable in vitro activities to that of vancomycin. Moreover, compound 19 also exhibited MIC = 1 μg/mL activities against a recent identified Z172 MRSA strain (vancomycin-intermediate and daptomycin-nonsusceptible phenotype) and the vancomycin-resistant Enterococcus faecalis (VRE) strain. In a mouse model with lethal infection of MRSA (4N216), a 75% survival rate was observed after a single dose of compound 19 was intravenously administered at 20 mg/kg. In light of their equipotent activities against different MRSA isolates and VRE strain, the data underscore the importance of designed hybrid series for the development of new N-substituted carbazoles as potential anti-MRSA agents.

Published
2016

6. Design, Synthesis, and Evaluation of Thiazolidine-2,4-dione Derivatives as a Novel Class of Glutaminase Inhibitors.

Author

Teng-Kuang Yeh, Ching-Chuan Kuo, Yue-Zhi Lee, Yi-Yu Ke, Kuang-Feng Chu, Hsing-Yu Hsu, Hsin-Yu Chang, Yu-Wei Liu, Jen-Shin Song, Cheng-Wei Yang, Li-Mei Lin, Manwu Sun, Szu-Huei Wu, Po-Chu Kuo, Chuan Shih, Chiung-Tong Chen, Lun Kelvin Tsou, and Shiow-Ju Lee

Subjects
*GLUTAMINASES, *KIDNEYS, *THIAZOLIDINEDIONES, *HIGH throughput screening (Drug development), *CANCER cells, *LABORATORY mice
Abstract

Humans have two glutaminase genes, GLS (GLS1) and GLS2, each of which has two alternative transcripts: the kidney isoform (KGA) and glutaminase C (GAC) for GLS, and the liver isoform (LGA) and glutaminase B (GAB) for GLS2. Initial hit compound (Z)-5-((1-(4-bromophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)methylene)thiazolidine-2,4-dione (2), a thiazolidine-2,4-dione, was obtained from a high throughput screening of 40 000 compounds against KGA. Subsequently, a series of thiazolidine-2,4-dione derivatives was synthesized. Most of these were found to inhibit KGA and GAC with comparable activities, were less potent inhibitors of GAB, and were moderately selective for GLS1 over GLS2. The relationships between chemical structure, activity, and selectivity were investigated. The lead compounds obtained were found to (1) offer in vitro cellular activities for inhibiting cell growth, clonogenicity, and cellular glutamate production, (2) exhibit high concentrations of exposure in plasma by a pharmacokinetic study, and (3) reduce the tumor size of xenografted human pancreatic AsPC-1 carcinoma cells in mice. [ABSTRACT FROM AUTHOR]

Published
2017
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8. Phenyl Benzenesulfonylhydrazides Exhibit Selective Indoleamine 2,3-Dioxygenase Inhibition with Potent in Vivo Pharmacodynamic Activity and Antitumor Efficacy.

Author

Shu-Yu Lin, Teng-Kuang Yeh, Ching-Chuan Kuo, Jen-Shin Song, Ming-Fu Cheng, Fang-Yu Liao, Min-Wu Chao, Han-Li Huang, Yi-Lin Chen, Chun-Yu Yang, Mine-Hsine Wu, Chia-Ling Hsieh, Wenchi Hsiao, Yi-Hui Peng, Jian-Sung Wu, Li-Mei Lin, Manwu Sun, Yu-Sheng Chao, Chuan Shih, and Su-Ying Wu

Subjects
*HYDRAZIDES, *INDOLEAMINE 2,3-dioxygenase, *ANTINEOPLASTIC agents, *ENZYME inhibitors, *BENZENESULFONIC acid, *PHARMACODYNAMICS, *DRUG efficacy
Abstract

Tryptophan metabolism has been recognized as an important mechanism in immune tolerance. Indoleamine 2,3-dioxygenase plays a key role in local tryptophan metabolism via the kynurenine pathway and has emerged as a therapeutic target for cancer immunotherapy. Our prior study identified phenyl benzenesulfonyl hydrazide 2 as a potent in vitro (though not in vivo) inhibitor of indoleamine 2,3-dioxygenase. Further lead optimization to improve in vitro potencies and pharmacokinetic profiles resulted in N'-(4-bromophenyl)-2-oxo-2,3-dihydro-1H-indole-5-sulfonyl hydrazide 40, which demonstrated 59% oral bioavailability and 73% of tumor growth delay without apparent body weight loss in the murine CT26 syngeneic model, after oral administration of 400 mg/kg. Accordingly, 40, is proposed as a potential drug lead worthy of advanced preclinical evaluation. [ABSTRACT FROM AUTHOR]

Published
2016
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10. Discovery of Novel N-β-d-Xylosylindole Derivatives as Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitors for the Management of Hyperglycemia in Diabetes.

Author

Chun-Hsu Yao, Jen-Shin Song, Chiung-Tong Chen, Teng-Kuang Yeh, Ming-Shiu Hung, Chih-Chun Chang, Yu-Wei Liu, Mao-Chia Yuan, Chieh-Jui Hsieh, Chung-Yu Huang, Min-Hsien Wang, Ching-Hui Chiu, Tsung-Chih Hsieh, Szu-Huei Wu, Wen-Chi Hsiao, Kuang-Feng Chu, Chi-Hui Tsai, Yu-Sheng Chao, and Jinq-Chyi Lee

Published
2011
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11. Design and Synthesis of Tetrahydropyridothieno[2,3-d]pyrimidine Scaffold Based Epidermal Growth Factor Receptor (EGFR) Kinase Inhibitors: The Role of Side Chain Chirality and Michael Acceptor Group for Maximal Potency.

Author

Chia-Hsien Wu, Mohane Selvaraj Coumar, Chang-Ying Chu, Wen-Hsing Lin, Yi-Rong Chen, Chiung-Tong Chen, Hui-Yi Shiao, Shaik Rafi, Sing-Yi Wang, Hui Hsu, Chun-Hwa Chen, Chun-Yu Chang, Teng-Yuan Chang, Tzu-Wen Lien, Ming-Yu Fang, Kai-Chia Yeh, Ching-Ping Chen, Teng-Kuang Yeh, Su-Huei Hsieh, and John T.-A. Hsu

Published
2010
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12. Substituted 4-Carboxymethylpyroglutamic Acid Diamides as Potent and Selective Inhibitors of Fibroblast Activation Protein.

Author

Ting-Yueh Tsai, Teng-Kuang Yeh, Xin Chen, Tsu Hsu, Yu-Chen Jao, Chih-Hsiang Huang, Jen-Shin Song, Yu-Chen Huang, Chia-Hui Chien, Jing-Huai Chiu, Shih-Chieh Yen, Hung-Kuan Tang, Yu-Sheng Chao, and Weir-Torn Jiaang

Subjects
*ENZYME inhibitors, *ORGANIC compounds, *PROTEOLYTIC enzymes, *PEPTIDASE, *ANTINEOPLASTIC agents, *DRUG development
Abstract

Fibroblast activation protein (FAP) belongs to the prolyl peptidase family. FAP inhibition is expected to become a new antitumor target. Most known FAP inhibitors often resemble the dipeptide cleavage products, with a boroproline at the P1 site; however, these inhibitors also inhibit DPP-IV, DPP-II, DPP8, and DPP9. Potent and selective FAP inhibitor is needed in evaluating that FAP as a therapeutic target. Therefore, it is important to develop selective FAP inhibitors for the use of target validation. To achieve this, optimization of the nonselective DPP-IV inhibitor 8led to the discovery of a new class of substituted 4-carboxymethylpyroglutamic acid diamides as FAP inhibitors. SAR studies resulted in a number of FAP inhibitors having IC50of 100 μM). Compounds 18a, 18b, and 19are the only known potent and selective FAP inhibitors, which prompts us to further study the physiological role of FAP. [ABSTRACT FROM AUTHOR]

Published
2010
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14. Discovery of 2-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an Active Metabolite. A Novel, Potent and Selective Cannabinoid-1 Receptor Inverse Agonist with High...

Author

Chien-Huang Wu, Ming-Shiu Hung, Jen-Shin Song, Teng-Kuang Yeh, Ming-Chen Chou, Cheng-Ming Chu, Jiing-Jyh Jan, Min-Tsang Hsieh, Shi-Liang Tseng, Chun-Ping Chang, Wan-Ping Hsieh, Yinchiu Lin, Yen-Nan Yeh, Wan-Ling Chung, Chun-Wei Kuo, Chin-Yu Lin, Horng-Shing Shy, Yu-Sheng Chao, and Kak-Shan Shia

Published
2009
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