Full Text Journal Articles by
Author Guangxiu Dai

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Immunological characterization of HM5023507, an orally active PI3Kδ/γ inhibitor.

Yu Cai, Jun Yu, Ping Ren, Jianlin He, Zhipeng Wu, Kun Xiao, Hong Jia, Jian Wang, Yang Sai, Guangxiu Dai, Xiong Li, Weiguo Su, Karen Ngo, Glenda Castro, Paul D Acton, Wai-Ping Fung-Leung, James P Edwards, Jennifer Venable, Tadimeti S Rao,

Phosphoinositide 3-kinases, delta (PI3Kδ) and gamma (PI3Kγ) are enriched in immune cells and regulate the development and function of innate and adaptive immunity. Dual PI3Kδγ inhibitors are considered high value targets for their potential to treat a variety of immune-mediated diseases, but their discovery has been challenging. Here we describe ... Read more >>

Pharmacol Res Perspect (Pharmacology research & perspectives)
[2020, 8(1):e00559]

Cited: 0 times

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Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.

Hong Jia, Guangxiu Dai, Weiguo Su, Kun Xiao, Jianyang Weng, Zhulin Zhang, Qing Wang, Tianhai Yuan, Fuying Shi, Zheng Zhang, Wei Chen, Yang Sai, Jian Wang, Xiong Li, Yu Cai, Jun Yu, Ping Ren, Jennifer Venable, Tadimeti Rao, James P Edwards, Scott D Bembenek,

An electronic density model was developed and used to identify a novel pyrrolotriazinone replacement for a quinazolinone, a commonly used moiety to impart selectivity in inhibitors for PI3Kγ and PI3Kδ. Guided by molecular docking, this new specificity piece was then linked to the hinge-binding region of the inhibitor using a ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2019, 62(10):4936-4948]

Cited: 1 time

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Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer.

Hong Jia, Guangxiu Dai, Jianyang Weng, Zhulin Zhang, Qing Wang, Feng Zhou, Longxian Jiao, Yumin Cui, Yongxin Ren, Shiming Fan, Jinghong Zhou, Weiguo Qing, Yi Gu, Jian Wang, Yang Sai, Weiguo Su,

HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2014, 57(18):7577-7589]

Cited: 14 times

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Bifunctional inhibition of HIV-1 reverse transcriptase: a first step in designing a bifunctional triphosphate.

Dongyuan Piao, Aravind Basavapathruni, Pinar Iyidogan, Guangxiu Dai, Wolfgang Hinz, Adrian S Ray, Eisuke Murakami, Joy Y Feng, Fei You, Ginger E Dutschman, David J Austin, Kathlyn A Parker, Karen S Anderson,

The onset of resistance to approved anti-AIDS drugs by HIV necessitates the search for novel inhibitors of HIV-1 reverse transcriptase (RT). Developing single molecular agents concurrently occupying the nucleoside and nonnucleoside binding sites in RT is an intriguing idea but the proof of concept has so far been elusive. As ... Read more >>

Bioorg. Med. Chem. Lett. (Bioorganic & medicinal chemistry letters)
[2013, 23(5):1511-1518]

Cited: 3 times

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Traditional Chinese medicine preparation for treating kidney deficiency, waist and knees soreness and preparation method thereof

GUANGXIU DAI, YING YANG,

The invention discloses a Chinese medicinal preparation for treating kidney deficiency and lassitude in loin and legs and a preparation method thereof. The Chinese medicinal preparation comprises the following compositions in portion by weight: 10 to 30 portions of ginseng, 10 to 30 portions of semen plantaginis, 10 to 30 ... Read more >>

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Chinese medicament preparation for treating depression and anxiety as well as preparation method thereof

YING YANG, GUANGXIU DAI,

The invention discloses a traditional Chinese medicine preparation for treating depressive disorder and anxiety disorder and a preparation method thereof. The preparation comprises the following components in portion by weight: 10 to 30 portions of prepared rhizome of rehmannia, 10 to 30 portions of Flos Albiziae, 10 to 30 portions ... Read more >>

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Pd-catalyzed alkyl to aryl migration and cyclization: an efficient synthesis of fused polycycles via multiple C-H activation.

Qinhua Huang, Alessia Fazio, Guangxiu Dai, Marino A Campo, Richard C Larock,

A novel palladium migration methodology for the synthesis of complex fused polycycles has been developed. This process involves 1,4-palladium alkyl to aryl migrations via through-space C-H activation, followed by intramolecular arylation or an intermolecular Heck reaction providing a very efficient way to synthesize fused ring systems. ... Read more >>

J. Am. Chem. Soc. (Journal of the American Chemical Society)
[2004, 126(24):7460-7461]

Cited: 41 times

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Synthesis of 3-substituted 4-aroylisoquinolines via Pd-catalyzed carbonylative cyclization of 2-(1-alkynyl)benzaldimines.

Guangxiu Dai, Richard C Larock,

A number of 3-substituted 4-aroylisoquinolines have been prepared in good yields by treating N-tert-butyl-2-(1-alkynyl)benzaldimines with aryl halides in the presence of CO and a palladium catalyst. Synthetically the methodology provides a simple and convenient route to isoquinolines containing an aryl, alkyl, or vinylic group at C-3 and an aroyl group ... Read more >>

J. Org. Chem. (The Journal of organic chemistry)
[2002, 67(20):7042-7047]

Cited: 16 times

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Synthesis of 3,4-disubstituted isoquinolines via palladium-catalyzed cross-coupling of 2-(1-alkynyl)benzaldimines and organic halides.

Guangxiu Dai, Richard C Larock,

The palladium-catalyzed cross-coupling of readily available N-tert-butyl-2-(1-alkynyl)benzaldimines and aryl, allylic, benzylic, alkynyl halides, as well as a vinylic halide, provides a valuable new route to 3,4-disubstituted isoquinolines with aryl, allylic, benzylic, 1-alkynyl, and vinylic substituents, respectively, in the 4-position. The reaction appears to require an aryl group on the end ... Read more >>

J. Org. Chem. (The Journal of organic chemistry)
[2003, 68(3):920-928]

Cited: 20 times

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Synthesis of 3-substituted 4-aroylisoquinolines via Pd-catalyzed carbonylative cyclization of o-(1-alkynyl)benzaldimines.

Guangxiu Dai, Richard C Larock,

[reaction: see text] o-(1-Alkynyl)benzaldimines react with aryl iodides and 1 atm of CO in the presence of tri-n-butylamine and a Pd(PPh(3))(4) catalyst to afford good yields of 3-substituted 4-aroylisoquinolines by acylpalladation of the carbon-carbon triple bond and cyclization. ... Read more >>

Org. Lett. (Organic letters)
[2002, 4(2):193-196]

Cited: 3 times

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