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Coupling Reaction of 4-Chloro-7-H-Pyrrolo[2,3-d]Pyrimidine with 2,3,5-Tri-O-Acetyl-b-D-Ribofuranosyl Chloride

Chinese Chemical Letters 2001年第5期12卷 391-394页

作者： Yun Long ZHANG Liang Ren ZHANG Zhen Jun YANG Ji Mei MIN Li He ZHANG Yang LU Ning Bo GONG Qi Tai ZHENG National Research Laboratory of Natural and Biomimetic Drugs Peking UniversityBeijing 100083 institue of materia medica Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050

Coupling reaction of 4-chloro-7-H-pyrrolo[2,3-d]pyrimidine with 2,3,5-tri-O-acetyl -β-D-ribofuranosyl chloride under the basic condition was investigated. An abnormal coupling reaction, in which the heterocyclic base attacked at the carbon of 1,2-O-methylidene moiety instead of anomeric carbon of ribose was observed and the structure of products 5a, 5b were identified by NMR and X-Ray diffraction.

关键词： Chloropyrrolo[2 3-d]pyrimidine 1-chloro-2 3 5-tri-O-acetyl-D-ribofuranose neigh-boring participation effect X-ray diffraction.

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Synthesis of 1-Aryl-1 H-indazoles via a Ligand-Free Copper- Catalyzed Intramolecular Amination Reaction

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Chinese Journal of Chemistry 2011年第6期29卷 1199-1204页

作者： Gao, Mingshan Liu, Xiujie Wang, Xianyang Cai, Qian Ding, Ke Key Laboratory of Regenerative Biology and institue of Chemical Biology Guangzhou Institutes of Biomedicine and Health Chinese Academy of Sciences Guangzhou Guangdong 510530 China Jiangsu Provincial Institute of materia medica Nanjing University of Technology Nanjing Jiangsu 210009 China

A general synthesis of 1-aryl-l-H-indazoles from o-halogenated aryl aldehydes or ketones and aryl hydrazines was described. This protocol included an intermolecular condensation and a ligand-free copper-catalyzed intramolecular Ullmann-type coupling reaction. This method was applied to a wide range of substrates to produce the indazole products in good yields.

关键词： copper amination ligand free

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Small molecule targeting of oncogenic FTO demethylation in acute myeloid leukemia

Small molecule targeting of oncogenic FTO demethylation in a...

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第十届全国化学生物学学术会议

作者： Yue Huang Hongjiao Xu Cai-Guang Yang Shanghai institue of materia medica Chinese Academy of Sciences

*** first mRNA demethytase,promotes leukemogenesis and Inhibits ATRA-mediated ***,we report the discovery of a novel Inhibitor for FTO demethylatlon that enables treatment of acute myeloid leukemia （AMD） with FTO-overexpresston.A number of assays were performed In order to understand the Inhibitor mode of action,and all the data point,towards direct Inhibition of FTO demethylatlon in vitro and in AML *** Inhibitor efficiently suppresses the development of leukemogenesis in *** together,our newfound inhibitors could servo as chemical probes to attenuate FTO activity and provide proot-of-concept that mRNA demethylase would be viewed as a druggable target against AML.

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Small molecule targeting of oncogenic FTO demethylation in acute myeloid leukemia

Small molecule targeting of oncogenic FTO demethylation in a...

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第十届全国化学生物学学术会议

作者： Y Yue Huang Hongjiao Xu Cai-Guang Yang Shanghai institue of materia medica Chinese Academy of Sciences

N6-methyladenosine(m A) is a prevalent modification in mRNA that significantly impacts biological regulation and human diseases. Recently, we demonstrated the critical functional importance of FTO, the first RNA demethylase, in leukemogensis and drug response. Achieving a chemical method to specific manipulate FTO demethylation would shed lights on RNA epigenetics, remaining a big challenge, however. Here, we have identified a new inhibitor derived from meclofenamic acid(MA) for FTO demethylation that enables treatment of acute myeloid leukemia(AML). A number of assays were performed in order to understand the inhibitor mode of action, and all the data point towards direct inhibitions of FTO demethylation in vitro and in AML cells. In addition, FTO inhibitor exhibits favorable pharmacokinetics and efficiently supresses the development of leukemogensis in mice. Taken together, these data reveal that our newfound inhibitor of FTO could serve as a chemical probe to attenuate FTO activity and provide proof-of-concept that mRNA demethylase would be viewed as a druggable target against AML..

关键词： AML FTO inhibitor demethylation chemical probe

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Inhibition of acetylcholinesterase by two genistein derivatives:kinetic analysis,molecular docking and molecular dynamics simulation

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Acta Pharmaceutica Sinica B 2014年第6期4卷 430-437页

作者： Jiansong Fang Ping Wu Ranyao Yang Li Gao Chao Li Dongmei Wang Song Wu Ai-Lin Liu Guan-Hua Du Institute of materia medica Chinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China Beijing Key Laboratory of Drug Target Research and Drug Screening Beijing 100050China State Key Laboratory of Bioactive Substance and Function of Natural Medicines Beijing 100050China

In this study two genistein derivatives(G1 and G2)are reported as inhibitors of acetylcholinesterase(AChE)and butyrylcholinesterase(BuChE),and differences in the inhibition of AChE are *** they differ in structure by a single methyl group,the inhibitory effect of G1(IC50¼264 nmol/L)on AChE was 80 times stronger than that of G2(IC50¼21,210 nmol/L).Enzyme-kinetic analysis,molecular docking and molecular dynamics(MD)simulations were conducted to better understand the molecular basis for this *** results obtained by kinetic analysis demonstrated that G1 can interact with both the catalytic active site and peripheral anionic site of *** predicted binding free energies of two complexes calculated by the molecular mechanics/generalized born surface area(MM/GBSA)method were consistent with the experimental *** analysis of the individual energy terms suggested that a difference between the net electrostatic contributions(ΔEele+ΔGGB)was responsible for the binding affinities of these two ***,analysis of the molecular mechanics and MM/GBSA free energy decomposition revealed that the difference between G1 and G2 originated from interactions with Tyr124,Glu292,Val294 and Phe338 of *** conclusion,the results reveal significant differences at the molecular level in the mechanism of inhibition of AChE by these structurally related compounds.

关键词： Genistein derivatives Acetylcholinesterase(AChE) Kinetics analysis Molecular docking Molecular dynamics simulation MM/GBSA

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Establishment of NaLuF_(4):15%Tb-based low dose X-PDT agent and its application on efficient antitumor therapy

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International Journal of Minerals,Metallurgy and materials 2024年第3期31卷 599-610页

作者： Yi Tian Zhiguang Fu Xiaosheng Zhu Chunjing Zhan Jinwei Hu Li Fan Chaojun Song Qian Yang Yu Wang Mei Shi Department of Radiation Oncology Xijing HospitalThe Fourth Military Medical UniversityXi’an 710032China Department of Oncology Air Force Medical CenterPLAThe Fourth Military Medical UniversityBeijing 100142China Department of Tumor Radiotherapy Air Force Medical CenterPLAThe Fourth Military Medical UniversityBeijing 100142China Department of Gastroenterology Air Force Hospital of Southern Theater CommandGuangzhou 510062China Department of Pharmaceutical Chemistry and Analysis School of PharmacyThe Fourth Military Medical UniversityXi’an 710032China School of Life Sciences Northwestern Polytechnical UniversityXi’an 710072China institue of materia medica School of PharmacyThe Fourth Military Medical UniversityXi’an 710032China

X-ray excited photodynamic therapy(X-PDT)is the bravo answer of photodynamic therapy(PDT)for deep-seated tumors,as it employs X-ray as the irradiation source to overcome the limitation of light penetration ***,high X-ray irradiation dose caused organ lesions and side effects became the major barrier to X-PDT *** address this issue,this work employed a classic-al co-precipitation reaction to synthesize NaLuF_(4):15%Tb^(3+)(NLF)with an average particle size of(23.48±0.91)nm,which was then coupled with the photosensitizer merocyanine 540(MC540)to form the X-PDT system NLF-MC540 with high production of singlet *** system could induce antitumor efficacy to about 24%in relative low dose X-ray irradiation range(0.1-0.3 Gy).In vivo,when NLF-MC540 irradiated by 0.1 Gy X-ray,the tumor inhibition percentage reached 89.5%±5.7%.The therapeutic mechanism of low dose X-PDT was found.A significant increase of neutrophils in serum was found on the third day after *** immunohistochemical staining of tumor sections,the Ly6G^(+),CD8^(+),and CD11c^(+)cells infiltrated in the tumor microenvironment were *** the bilat-eral tumor model,the NLF-MC540 with 0.1 Gy X-ray irradiation could inhibit both the primary tumor and the distant tumor ***-tected by enzyme linked immunosorbent assay(ELISA),two cytokines IFN-γand TNF-αin serum were upregulated 7 and 6 times than negative control,*** by enzyme linked immune spot assay(ELISPOT),the number of immune cells attributable to the IFN-γand TNF-αlevels in the group of low dose X-PDT were 14 and 6 times greater than that in the negative control group,***,it conclude that low dose X-PDT system could successfully upregulate the levels of immune cells,stimulate the secretion of cy-tokines(especially IFN-γand TNF-α),activate antitumor immunity,and finally inhibit colon tumor growth.

关键词： X-ray excited photodynamic therapy singlet oxygen low dose X-Ray irradiation efficient antitumor therapy anti-tumor immunity

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Effects of triterpenic acid from Prunella vulgaris L. on glycemia and pancreas in rat model of streptozotozin diabetes

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Chinese medical Journal 2013年第9期126卷 1647-1653页

作者： ZHOU Qiao-xia LIU Feng ZHANG Jing-shuo LU Ji-guang GU Zhen-lun GU Gui-xiong Institute of Pediatric Medicine Soochow University Affiliated Children's Hospital Suzhou Jiangsu 215003 China Department of Pediatrics Department of Cardiology Department of Pharmacy Suzhou Kowloon Hospital Affiliated to Shanghai Jiaotong University Suzhou Jiangsu 215021 China Department of Pharmaceutic Analysis College of Pharmaceutical Science Soochow University Suzhou Jiangsu 215123 China Department of Pharmacology Suzhou Institue of Chinese Materia Medica Soochow University Suzhou Jiangsu 215007 China

Background The effects of triterpenic acid from Prunella vulgaris L. （TAP） on diabetes and its mechanism are uncertain. The aim of this study was to investigate the effects of TAP on antihyperglycemic, antioxidant, and pancreas-protective in streptozotozin （STZ）-diabetic rats. Methods The diabetic model was produced by injection of 60 mg/kg STZ. Blood was drawn from the tail vein of rats after 72 hours. Rats with blood glucose 〉16.7 mmol/L were considered diabetic. Diabetic rats were randomly divided into four groups：（1） Diabetes rat （STZ）, （2） Diabetic rats treated with 50 mg/kg of triterpenic acid from Prunella vulgaris L （STZ＋TAP50）, （3） Diabetic rats treated with 100 mg/kg TAP （STZ＋TAP100）, and （4） Diabetic rats treated with 200 mg/kg TAP （STZ＋TAP200）. Normal rats （n=10） acted as the control group （NC）. TAP was administered by the intragastric route once each day for six weeks. Body weight and the concentration of blood glucose （BG） were measured after three and six weeks. Fructosamine （FMN）, malondialdehyde （MDA）, and nitric oxide （NO）, and the activities of nitric oxide synthase （NOS） and superoxide dismutase （SOD） in serum were determined after six weeks using commercially available kits following the manufacturer＇s instructions. Pathologic changes in pancreatic β-cells were also investigated by microscopic examination after hematoxylin-eosin （HE） staining. The level of SOD mRNA in pancreatic β-cells was measured by polymerase chain reaction （PCR）. Results The levels of BG, FMN, NO, and MDA and the activities of NOS in serum in the four diabetes groups were significantly increased compared with the control group （P 〈0.01）. The activity of SOD in serum and the body weight was significantly decreased compared with the control group （P 〈0.01）. After administration of TAP to diabetic rats for six weeks, the body weight and the levels of BG, FMN, MDA, NO and the activity of NOS in serum decreased significantly compared with the STZ group in a dose-dependent manne

关键词： diabetes mellitus oxidative stress lipid peroxidas free radicals antioxidant triterpenic acid Prunella vulgaris L.

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