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Chinese Journal of Chemistry 2021年第3期39卷 671-676页

作者： Chen-Xi Yu Bing-Yan Wei Xue-Qing Kong Cai-Guang Yang fa-jun nan State Key Laboratory of Drug Research the National Center for Drug ScreeningShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing 100049China School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced StudyUCASHangzhouZhejiang 310024China Yantai Key Laboratory of nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaYantaiShandong 264000China

Main observation and conclusion Methicillin-resistant Staphylococcus aureus(MRSA)has become a major threat on public health because of the increase of clinically isolated strains that exhibit resistance to many ***,development of new antibiotics for the treatment of MRSA in-fection is a sustained *** have previously identified a ring-opened bengamide analogue L472-2 that displays moderate ac-tivity against the growth of *** our previous work,we started from L472-2 and identified a class of analogues containing al-kynyl groups which have the potential to activate SaCIpP activity but moderate antibacterial ***,we focused on the anti-bacterial activity of L472-2,and a novel series of ring-opened bengamide analogues were synthesized and their activities were evalu-ated against *** conducting a compact analysis of the structure-activity relationships(SAR)of these analogues,we found that an adamantane ethanol ester bengamide 2j showed excellent antibacterial activity towards six *** strains,including MRSA,while it does not activate ***,these bengamide analogues represent a new class of candidates that suppress MRSA via-bility..

关键词： Bengamides Staphylococcus aureus Antibiotics Structure-activity relationships Pharmacokinetic

Discovery of Novel Long-Chain Alkenyl Diacid Derivatives as ACLY Inhibitors

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Chinese Journal of Chemistry 2022年第22期40卷 2663-2670页

作者： Gao-Lei Song Lei Cao Mei Zhang Yu-Rou Yang Jie Ma Zhi-Fu Xie Jing-Ya Li fa-jun nan State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing 100049China Yantai Key Laboratory of nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaYantaiShandong 264000China

ATP citrate lyase(ACLY)synthesizes cytosolic acetyl coenzyme A(acetyl-CoA),an essential biosynthetic precursor for lipid synthesis and the acetyl donor required for protein *** aberrant expression and activity of ACLY has been documented in multiple human ***-1002 is an indirect ACLY inhibitor,and it has recently been approved by the FDA as an additional therapeutic option in high-risk hypercholesterolemia patients unable to meet goals with standard *** this work,we identified a series of novel long-chain alkenyl diacids as potent direct ACLY inhibitors,and comprehensive structure-activity relationship analysis showed that compound 18f was the most potent ACLY inhibitor with an IC50 value of 1.5μmol/*** ester formation of 18f gave a new series of compounds such as 25f that maintained ACLY inhibitory activity and improved antitumor cell proliferation effects.

关键词： Alkenyl diacid derivatives Cancer ACLY inhibitors Acetyl-CoA Structure-activity relationships

The hit-to-lead optimization of 1,2,3,4,4a,9a-hexahydro-1H-xanthenes as glucocorticoid receptor antagonists

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Chinese Chemical Letters 2014年第5期25卷 693-698页

作者： Yan-Hui Zhu Meng Zhang Qun-Yi Li Qing Liu Jie Zhang Yun-Yun Yuan fa-jun nan Ming-Wei Wang The National Center for Drug Screening Shanghai Institute of Materia MedicaChinese Academy of Sciences The CAS Key Laboratory of Receptor Research Shanghai Institute of Materia MedicaChinese Academy of Sciences

The structure–activity relationship（SAR） study of a 1 2 3 4 4a 9a-hexahydro-1H-xanthene series of selective,human glucocorticoid receptor a（hGRa） antagonists is *** were screened using hydroxyapatite-based GR binding and MMTV-Luc co-transfection reporter gene *** different regions of the scaffold were modified to assess the effects on hGRa antagonism and related *** 8d exhibits an 8-fold better bioactivity than the original hit 1a,as well as an improved chemical stability,which make it a promising lead for the subsequent optimization.

关键词： Glucocorticoid receptor Antagonist 1 2 3 4 4a 9a-Hexahydroxanthene Structure–activity relationship Lead optimization

Design,Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators

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Chinese Journal of Chemistry 2020年第10期38卷 1111-1115页

作者： Xue-Qing Kong Bing-Yan Wei Chen-Xi Yu Xiang Na Guan Wei-Ping Ma Gang Liu Cai-Guang Yang fa-jun nan Chinese National Center for Drug Screening CAS Key Laboratory of Receptor ResearchStote Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai 201203China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing 100049China Yantai Key Laboratory of nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaNo.39Science and Technology AvenueHigh-tech Industrial Development ZoneYantaiShandong 264000China

Summary of main observation and conclusion To combat multidrug-resistant Gram-positive bacteria,new antimicrobials particularly those with novel mechanism of action are badly *** with conventional antibiotics which are typical inhibitors,small-molecule activators of bacterial CIpP represent a new class of *** ClpP activator has been developed for clinical ***,we conducted a screening on our library of benga-mide-like ring opened analogues and found that L472-2 possesses a low minimum inhibitory concentration(MIC)against *** and shows no activity for ClpP activation in vitro,but it displayed reduced antibacterial activity against *** with clpP *** order to obtain bengamide analogues that activate ClpP in vitro as well as possess antibacterial activity,we perform further structural modifications starting from *** 37 re-mains the antimicrobial activity and activation of ClpP protein in vitro,which could be viewed as a new chemical scaffold for ClpP activators and worthy of further investigation.

关键词： analogues activation starting

In vitro Potentiation of Antimalarial Activities by Daphnetin Derivatives Against Plasmodium falciparum

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Biomedical and Environmental Sciences 2006年第5期19卷 367-370页

作者： faNG HUANG LIN-HUA TANG LIN-QIAN YU YI-CHANG NI QIN-MEI WANG fa-jun nan National Institute of Parasite Diseases Chinese Center for Disease Control and Prevention Shanghai 200025 China Chinese National Center for Drug Screening Shanghai Institute of Materia Medica Shanghai Institute for Biological Sciences Graduate School of the Chinese Academy of Sciences Shanghai 201203 China

Objective To screen the antimalarial compounds of daphnetin derivatives against Plasmodium falciparum in vitro. Method Plasmodium faciparum （FCC1） was cultured in vitro by a modified method of Trager and Jensen. Antimalarial compounds were screened by microscopy-based assay and microfluorimetric method. Results DA79 and DA78 showed potent antimalarial activity against Plasmodiumfalciparum cultured in vitro. Conclusion Though the relationship between the structures of daphnetin derivatives and their antimalarial activities has not been clarified yet, this study may provide a new direction for discovery of more potential antimalarial compounds.

关键词： Daphnetin Antimalarial Drug screening

A faCILE TOTAL SYNTHESIS OF (±)-SELINA-3,11-DIEN-9-OL

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Chinese Chemical Letters 1994年第9期5卷 721-724页

作者： Li jun LIU Zhao Ming XIONG fa jun nan Tong Shuang LI Yu Lin LI(State Key Laboratory of Applied Organic Chemistry and Institute or Organic Chemistry, Lanzhou University. Lanzhou 730000)

A ffcile tatal synthesis of (±)-selina-3. 11-dien-9-ol (1) has been described. The key step is the onepot reductive fragmentation of α,β-unsaturated p-tosylhydrazone and deduction of 9-carbonyl of 5 With sodium bor... 详细信息

关键词： SELINA-3,11-DIEN-9-OL TOTAL A faCILE TOTAL SYNTHESIS OF

SYNTHESIS OF 2,3-DEHYDRO-4, 9β-DIHYDROXY-β-DIHYDROAGAROFURAN

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Chinese Chemical Letters 1995年第12期6卷 1037-1040页

作者： fa jun nan Zhao Ming XIONG Li jun LIU Tong Shang LI Yu Lin LI (State Key Laboratory of Applied Organic Chemistry and Institute of Organic Chemistry,Lanzhou University, Lanzhou 730000) (Department of Chemistry, Hebei University, Baoding 071002)

Dehydro-4β, 9β-dihydraxy-β-dihydroagarofuran (2), possible precursor of 1α,9β- dibenzoylaxy-2β, 3β, 4β-trihydraxy-β-dihydroagarofuran(1), was synthesized from(-) -carvone via thirteensteps.

关键词：

TOTAL　SYNTHESIS　OF　3α，4α－OXIDOAGAROFURAN　AND　（－）－3β，4α－DIHYDROXY－β－DIHYDROAGAROFURAN

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Chinese Chemical Letters 1994年第1期5卷 15-18页

作者： fa jun nan Xin CHEN Zhao Ming XIONG Tong Shuang LI Yu Lin LI(State Key Laboratory of Applied Organic Chemistry and Institute of Organic Chemistry, Lanzhou University, Lanzhou 730000.)

The first stereoselective total synthesis of (-)-3β, 4α-dihydrocy-β-dihydroagarofuran (1) and 3α, 4α-oxidoagarofuran (2) has been described. The key step is the expoxidation of α-agarofuran (6)with dimethyldioxi... 详细信息

关键词： TOTAL SYNTHESIS OXIDOAGAROFURAN DIHYDROXY OF AND DIHYDROAGAROFURAN

STEREOSELECTIVE TOTAL SYNTHESIS OF(±)-4α(H)-EUDESMANE

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Chinese Chemical Letters 1992年第12期3卷 965-966页

作者： Xin CHEN fa jun nan Si Chang SHAO Li Yuan MIN Tong Shuang LI Yu Lin LI Key Laboratory of Applied Organic Chemistry and Institute of Organic Chemistry,Lanzhou University,Lanzhou 730000

The first stereoselective total synthesis of the biomarker(±)-4α(H)-eudesmane 1,starting from (-)-carvone in five steps,has been described.

关键词： TOTAL STEREOSELECTIVE TOTAL SYNTHESIS OF EUDESMANE

Type I methionine aminopeptidase from Saccharomyces cerevisiae is a potential target for antifungal drug screening

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Acta Pharmacologica Sinica 2004年第7期25卷 61-68页

作者： Ling-ling CHEN, Jia LI, Jing-ya LI, Qun-li LUO, Wei-feng MAO, Qiang SHEN, fa-jun nan3, Qi-zhuang YE2,3 NationalCenter for Drug Screening, Instituteof Materia Medica, Shanghai Institutes for BiologicalSciences, Chinese AcademyofSciences, Shanghai 201203, China 2 The High Throughput Screening Laboratory, University of Kansas, Lawrence, Kansas 66047, USA National Center for Drug Screening Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China

AIM: To screen antifungal drug candidates using in vitro and in vivo assays based on type I methionine aminopep- tidase from Saccharomyces cerevisiae (ScMetAP1). METHODS: A colorimetric assay suitable for high throughput screening (HTS) using recombinant ScMetAP1 protein expressed in Escherichia coli was established for antifungal lead discovery. A series of pyridine-2-carboxylic acid derivatives were characterized and a chemical library of 12 800 pure organic compounds was screened with the in vitro ScMetAP1 assay. Active compounds from the in vitro assay were further evaluated by a growth inhibition assay on yeast strain with deletion of ScMetAP1 gene map1 in comparison with the wild-type yeast strain and the yeast strain with deletion of type II enzyme (ScMetAP2) gene map2. RESULTS: Active ScMetAP1 inhibitors were identified from HTS. Some of the pyridine-2-carboxylic acid derivatives (compound 2 and 3) had selective inhibition of the growth of map2 deletion yeast and weak inhibition on wild-type yeast growth, while no inhibition on map1 deletion yeast. CONCLUSION: ScMetAP1 is a novel potential target for developing antifungal drugs. The in vitro and in vivo ScMetAP1 assays can serve as tools in discovering antifungal drug candidates.

关键词： methionine aminopeptidase high-throughput screening antifungal agent