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研究领域

1. 靶向性抗肿瘤和抗病毒药物先导化合物的发现和结构优化研究; 2. 基于优势骨架的化学结构多样性和生物活性多样性研究。

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Yang, C.; Xu, Z.; Zhao, Z.; Li, L.; Zhao, T.; Peng, D.; Xu, M.; Rong, R.*; Long, Y.*; Zhu, T.* A Novel Proteolysis-resistant Cyclic Helix B Peptide Ameliorates Kidney Ischemia Reperfusion Injury. Biochim. Biophys. Acta-Mol. Basis Dis.2014, DOI: 10.1016/j.bbadis.2014.09.001. (IF: 5.089) Lin, J.-P.; Zhang, F.-H.; Long, Y.-Q.*Solvent/oxidant-switchable synthesis of multisubstitutedquinazolines and benzimidazoles via metal-free selective oxidative annulation of arylamidines. Org. Lett.2014, 16, 2822-2825. (IF: 6.324) Xue, D.; Long, Y.-Q.* Metal-Free TEMPO-Promoted C(sp3)–H Amination to Afford MultisubstitutedBenzimidazoles.J. Org. Chem.2014, 79, 4727-4734.(IF: 4.638) Li, B.-W.; Zhang, F.-H.; Serrao, E.; Chen, H.; Sanchezc, T. W.; Yang, L.-M.; Neamati, N.; Zheng, Y.-T.; Wang, H.*; Long, Y.-Q.* Design and discovery of flavonoid-based HIV-1 integrase inhibitors targeting both the active site and the interaction with LEDGF/p75. Bioorg. Med. Chem.2014, 22, 3146-3158.(IF: 2.951) Zhi, Y.;Gao,L.-X.; Jin, Y.; Tang, C.-L.; Li, J.-Y.; Li, J.*; Long, Y.-Q.* 3-Carboxyl-4-quinolones as cell-permeable inhibitors of protein tyrosine phosphatase 1B. Bioorg. Med. Chem.2014, 22, 3670-3683. Wang, S.-F.; Lin,J.-P.; He, P.-L.; Zuo, J.-P.*; Long, Y.-Q.* 2-Aryl-3-carbonylquinolones: design, synthesis and biological evaulation of novel HCV NS5B polymerase inhibitors.ActaChimicaSinica2014, 72, 906-913 (Cover Paper). (IF: 0.874) Serrao, E.; Xu, Z.-L.; Debnath, B.; Christ, F.; Debyser, Z.; Long, Y.-Q.* and Neamati, N.*Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase-LEDGF/p75 interaction. Bioorg. Med. Chem.2013, 21, 5963-5972. Long, Y.-Q.*; Huang, S.-X.; Zawahir, Z.; Xu, Z.-L.; Li, H.-Y.; Sanchez, T.; Zhi, Y.; De Houwer, S.; Christ, F.; Debyser, Z.; Neamati, N.*Design of Cell-Permeable Stapled-Peptides as HIV-1 Integrase Inhibitors. J. Med. Chem. 2013, 56, 5601-5612.(IF: 5.480) Lin, J.-P.; Long, Y.-Q.*Transition Metal-Free One-Pot Synthesis of 2-Substituted 3-Carboxy-4-Quinolone and Chromone Derivatives.Chem. Commun., 2013, 49 (46), 5313 - 5315.(IF: 6.718) Xiaoxiao Sun, X. X.; Ai, M. D.; Wang, Y.; Shen, S. S.; Gu, Y.; Jin, Y.;Zhou, Z.Y.; Long, Y.-Q.and Yu, Q. Selective induction of tumor cell apoptosis by a novel P450-mediated reactive oxygen species (ROS) inducer methyl 3-(4-nitrophenyl) propiolate. J. Biol. Chem. 2013,288, 8826-8837.(IF: 4.60) Wang, Y.; Xu,Z.-L.;Ai, J.; Peng, X.; Lin, J.-P.; Ji, Y.-C.; Geng, M.-Y.*; Long, Y.-Q.*Investigation on the 1,6-naphthyridine motif: discovery and SAR study of 1H-imidazo[4,5-h][1,6]naphthyridin-2(3H)-one-based c-Met kinase inhibitors.Org. Biomol. Chem.2013, 11 (9),1545-1562.(IF: 3.487) Peng, D. Xu, Z. L.; Yang, C. Rong, R.M.; Zhu, T.Y.*; Long, Y.Q.*Metabolically stabilized structural modification on the helix Bsurface peptide of erythropoietin: Design, synthesis and improvedrenoprotective effect.ScientiaSinicaChimica2013, 43(8), 1033-1040. (in Chinese) (Cover paper) Zeng, L.-F.; Wang, Y.;Kazemi, R.; Xu, S.; Xu, Z.-L.; Sanchez, T. W.; Yang, L.-M.;Debnath, B.;Odde, S.; Xie, H.; Zheng, Y.-T.; Ding, J.;Neamati, N. and Long, Y.-Q.*Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.J. Med. Chem.2012, 55(22), 9492-9509. Cao, B.; Wang, Y.; Ding, K.; Neamati, N.; Long, Y.-Q.*Synthesis of the pyridinyl analogues of dibenzylideneacetone (pyr-dba) via an improvedClaisen-Schmidt condensation, displaying diverse biological activities as curcumin analogues.Org. Biomol. Chem.2012, 10, 1239-1245. Liu, Z.-L.; Zhou, Z.-Y.; Tian, W.; Fan, X.; Xue, D.; Yu, Q.*; Long, Y.-Q.*Discovery of novel 2-N-aryl substituted benzenesulfonamidoacetamides: orally bioavailable tubulin polymerization inhibitors with marked antitumor activities. ChemMedChem2012, 7(4), 680-693. (IF: 3.046) Huang, S.-X.; Cao, B.; Morisseau, C.; Jin, Y.; Hammock, B. D.;Long, Y.-Q.*Structure-based optimization of the piperazino-containing 1,3-disubstituted ureas affording sub-nanomolar inhibitors of soluble epoxide hydrolase. Med. Chem. Commun.2012, 3, 379-384. (IF: 2.626) Huang, S.-X.; Wang, Y.; Long, Y.-Q.*Advances in the research of human soluble epoxide hydrolase inhibitors.Chinese J. Org. Chem.2012, 32(5), 877-888 (in Chinese).(IF: 0.858) Fan, X.; Zhang, F.-H.; Al-Safi, R. I.; Zeng, L.-F.;Shabaik, Y.; Debnath, B.; Sanchez, T. W.;Odde, S.; Neamati,N. and Long, Y.-Q.*Design of HIV-1 Integrase inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75: a scaffold hopping approach using salicylate and catechol groups. Bioorg. Med. Chem.2011, 19(16), 4935-4952. Peng, D.; Zhi, Y.; Xue, T.; Gao, H.-Y.; Long, Y.-Q.*The ligand-based structural optimization of Grb2-SH2 inhibitors: high affinity, low charge and reduced peptidic nature.Chinese J. Org. Chem.2011, 31(12), 2019-2033(in Chinese). Wang, Y.; Long, Y.-Q.*Advances in Small-molecule Inhibitors of Protein Tyrosine Kinases.Chinese J. Org. Chem.2011, 31(10), 1595-1606(in Chinese).

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