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Chinese Chemical Letters 2006年第2期17卷 165-168页

作者： Lian You ZHENG Xu BAI The center for combinatorial chemistry and drug discovery Jilin University Changchun 130012

Grignard additions to a quinoxalinium salt were studied. Depending on the ratio of the reagents and reaction temperature, 1, 2, 3, 4-tetrahydroquinoxaline and 1, 2-dihydroquinoxaline derivatives could be resulted sele... 详细信息

关键词： Grignard addition quinoxalinium salt dihydroquinoxaline tetrahydroquinoxaline.

Synthesis and biological evaluation of 3-(piperidin-4-yl)isoxazolo[4,5-d]pyrimidine derivatives as novel PI3Kδ inhibitors

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Chinese Chemical Letters 2015年第10期26卷 1283-1288页

作者： Jia-Lin Guo Yun-Yong Liu Ya-Zhong Pei the center for combinatorial chemistry and drug discovery of jilin university School of Pharmaceutical Sciences Jilin University Nanjing Gator Medi Tech Company Ltd.

An efficient synthesis of novel 3-（piperidin-4-yl）isoxazolo[4,5-d]pyrimidine scaffold has been designed and deveopled. A series of 5-phenylurea derivatives was synthesized using this method. Their cytotoxic activities against breast cancer cell line BT-474 were evaluated by CCK-8 assay. Most of them showed potent anti-proliferative activities, of which compound 20 and 21 exhibited IC50 s of 1.565 mmol/L and1.311 mmol/L, respectively. Furthermore, compound 20 and 21 also showed potent inhibitory activities against PI3 Kd with IC50 s of 0.286 mmol/L and 0.452 mmol/L, respectively. These results indicate that these 3-（piperidin-4-yl）isoxazolo[4,5-d]pyrimidine derivatives are novel antitumor agents through the inhibition of PI3 Kd.

关键词： Synthesis Isoxazolopyrimidine PI3Kδ inhibitors Cytotoxicity

Synthesis of Novel 3-Aryl Isoindolinone Derivatives

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Chemical Research in Chinese Universities 2013年第3期29卷 487-494页

作者： HU Chen-ming ZHENG Lian-you PEI Ya-zhong BAI Xu center for combinatorial chemistry and drug discovery College of Chemistry and School of Pharmaceutical Sciences Jilin University Changchun 130021 P. R. China

A library of novel 3-aryl isoindolinone derivatives with aromatic amino acid derivative fragments was designed and synthesized. Two synthetic routes were employed to construct 3-aryl isoindolinone ring system for diff... 详细信息

关键词： Molecular library 3-Aryl isoindolinone Aromatic amino acid derivative

Chondroitinase ABC combined with Schwann cell transplantation enhances restoration of neural connection and functional recovery following acute and chronic spinal cord injury

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Neural Regeneration Research 2025年第5期20卷 1467-1482页

作者： Wenrui Qu Xiangbing Wu Wei Wu Ying Wang Yan Sun Lingxiao Deng Melissa Walker Chen Chen Heqiao Dai Qi Han Ying Ding Yongzhi Xia George Smith Rui Li Nai-Kui Liu Xiao-Ming Xu Spinal Cord and Brain Injury Research Group Stark Neurosciences Research InstituteDepartment of Neurological SurgeryIndiana University School of MedicineIndianapolisINUSA Department of Hand Surgery the Second Hospital of Jilin UniversityChangchunJilin ProvinceChina Shriners Hospitals Pediatric Research center Temple University School of MedicinePhiladelphiaPAUSA Department of Anatomy&Cell Biology Indiana University School of MedicineIndianapolisINUSA

Schwann cell transplantation is considered one of the most promising cell-based therapy to repair injured spinal cord due to its unique growth-promoting and myelin-forming properties.A the Food and drug Administration-approved Phase I clinical trial has been conducted to evaluate the safety of transplanted human autologous Schwann cells to treat patients with spinal cord injury.A major challenge for Schwann cell transplantation is that grafted Schwann cells are confined within the lesion cavity,and they do not migrate into the host environment due to the inhibitory barrier formed by injury-induced glial scar,thus limiting axonal reentry into the host spinal *** we introduce a combinatorial strategy by suppressing the inhibitory extracellular environment with injection of lentivirus-mediated transfection of chondroitinase ABC gene at the rostral and caudal borders of the lesion site and simultaneously leveraging the repair capacity of transplanted Schwann cells in adult rats following a mid-thoracic contusive spinal cord *** report that when the glial scar was degraded by chondroitinase ABC at the rostral and caudal lesion borders,Schwann cells migrated for considerable distances in both rostral and caudal *** Schwann cell migration led to enhanced axonal regrowth,including the serotonergic and dopaminergic axons originating from supraspinal regions,and promoted recovery of locomotor and urinary bladder ***,the Schwann cell survival and axonal regrowth persisted up to 6 months after the injury,even when treatment was delayed for 3 months to mimic chronic spinal cord *** findings collectively show promising evidence for a combinatorial strategy with chondroitinase ABC and Schwann cells in promoting remodeling and recovery of function following spinal cord injury.

关键词： axonal regrowth bladder function chondroitinase ABC functional recovery glial scar lentivirus migration Schwann cell spinal cord injury transplantation

Merger of Ezetimibe and Statin:a Potential Dual Inhibitor

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Chemical Research in Chinese Universities 2011年第2期27卷 232-236页

作者： HE Xing-lian XU Xian-xiu ZHENG Lian-you BAI Xu center for combinatorial chemistry and drug discovery School of Pharmaceutical Sciences Jilin University Changchun 130021 P R. China College of chemistry Jilin University Changchun 130012 P R. China College of chemistry Northeast Normal University Changchun 130024 P R. China

A potential dual inhibitor（4） for exogenous absorption and endogenic synthesis of cholesterol was designed based on the conjugation of the β-lactam pharmacophore of ezetimibe and the δ-lactone pharmacophore of statins. The merger of ezetimibe and statin 4 was synthesized from p-hydroxybenzaldehyde through a ten-step route. 1H NMR analysis showed existence of four pairs of enantiomers（5.7：5.7：1：1, molar ratio）. And compound 4 was found to lower total glucose（TG） level in rat serum via a high-cholesterol and high-fat feeding experiment.

关键词： Multi-target drug Ezetimibe Statin

New glowing dyes in vivo imaging with wavelengths beyond 1500 nm

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Science China chemistry 2019年第1期62卷 7-8页

作者： Jing Yang Xuechuan Hong State Key Laboratory of Virology Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals Wuhan University School of Pharmaceutical Sciences

Near-infrared (NIR)fluorescence imaging in the second near-infrared region (NIR-H,1000-1700 nm)is an important and attractive imaging method for biomedical research and clinical applications,and can achieve high spatial resolution, high signal-to-background ratio (SBR)and deeper tissue imaging owing to nearly zero auto-fluorescence background and tissue scattering .Smaller optical sub-window such as NIR-IIb (1500-1700 nm)has provided significant improvements in in vivo fluorescence imaging clarity and penetration depth.

关键词： Near-infrared (NIR)fluorescence Smaller optical fluorescence

Applications of Ene-like Reactions in Construction of Nitrogen-containing Cyclic Scaffolds

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Applications of Ene-like Reactions in Construction of Nitrog...

Stereoselective Synthesis of 3-Carboxy-4,5-dihydropyrroles via an Intramolecular Iminium Cyclization Reaction

中国化学会第九届全国有机化学学术会议

作者： Yuewei Zhang Qun Dang Xu Bai the center for combinatorial chemistry and drug discovery of jilin university The College of Chemistry and The School of Pharmaceutical Sciences Jilin University

＜正＞Rapid access to diverse heterocyclic scaffolds are often required in medicinal ***,development of new methodologies continues to be a focus in organic *** ene reaction has achieved wide recognition as a synthetically powerful carbon-carbon bond forming method in organic synthesis.[1]Recently we investigated on-demand selection of the reaction path

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Stereoselective Synthesis of 3-Carboxy-4,5-dihydropyrroles v...

New NIR-Ⅱ dyes without a benzobisthiadiazole core

中国化学会第九届全国有机化学学术会议

作者： XIANG Jin-Bao Xie Hong-Xiang Li Zhuo Dang Qun Bai Xu the center for combinatorial chemistry and drug discovery of jilin university The School of Pharmaceutical Sciences The College of chemistry jilin university

The dihydropyrrole framework is a valuable structural motif found in a number of natural products and pharmaceutical agents. 3-Carboxy-4,5-dihydropyrroles were not only shown to possess interesting biological activiti...

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Chinese Chemical Letters 2018年第10期29卷 1425-1428页

作者： Hui Zhou Yuling Xiao Xuechuan Hong State Key Laboratory of Virology Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) and Hubei Province Engineering and Technology Research Center for Fluorinated PharmaceuticalsSchool of Pharmaceutical SciencesWuhan University Medical College Tibet University

Fluorescent NIR-Ⅱ imaging has a wide range of benefits not offered by other imaging modalities for biomedical applications, derived from its combination of high spatial and temporal resolution due to reduced photon absorption, scattering and tissue auto-fluorescence. Compared to the well-studied NIR-Ⅰ small-molecule fluorophores, the structures of NIR-Ⅱ fluorophores are scarce. To date, the main fluorophore units are composed of conjugated π system with a benzobisthiadiazole（BBTD） core and donor-acceptor-donor（D-A-D） structure. Herein, researchers Yang et al. and Zhang et al. have reported new NIR-Ⅱ probes ECX and FD-1080 respectively without a BBTD core which are highlighted.

关键词： NIR-Ⅱ dyes Fluorescence imaging D-A-D structure 1064 nm excitation In vivo imaging

Design and Synthesis of Tri-substituted Chiral Pyrrolidin-2-one Derivatives as CCR4 Antagonists

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Chinese Journal of chemistry 2013年第9期31卷 1144-1152页

作者： Wei Sun Linjie Tian Hui Qi Dan Jiang Ying Wang Song Li Junhai Xiao Xiaohong Yang School of Pharmaceutical Sciences Jilin University Changchun Jilin 130021 China Laboratory of Computer-Aided drug Design & discovery Beijing Institute of Pharmacology & Toxicology Beij'ing 100850 China center for Human Disease Genomics Peking University Beijing 100083 China

A series of tri-substituted chiral pyrrolidin-2-one derivatives have been designed and synthesized as CC chemokine receptor 4 （CCR4） antagonists. The structure of CCR4 was built by homology modeling. Asymmetric synthesis was applied to synthesize the R,R configuration chiral pyrrolidin-2-one scaffold. The stereoisomeric con- figurations of the compounds were identified by 2D I H-~H COSY spectroscopy and 1D NOESY spectroscopy. This method was more economical and convenient than traditional X-ray single crystal diffraction. In addition, the inter- actions between these compounds and the N-terminal extracellular tail of CCR4 were studied using capillary zone electrophoresis. The CCR4 chemotaxis inhibition effect was tested in CCR4-transfected HEK293 cells. Several compounds showed potent activities as CCR4 antagonists. Among these compounds, lc is the most active one. Its apparent binding constant of CZE experiment result is （1.569±0.11）× 10s L·mol ^-1, and its percentage inhibition of the HEK293/CCR4 cells migration with the concentration of I gmol·L ^-1 in DMSO is 59%. And compound If has slightly higher affinity to N-terminal of CCR4 according to its apparent binding constant than lb because of the in- troduced ester linkage. Further studies on the mechanism of these compounds are in progress.

关键词： CCR4 antagonists tri-substituted chiral pyrrolidin-2-one derivatives synthesis