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成果及论文


1.        S. Su, Z. Y, H. Gao, H. Yang, S. Zhu, Z. An, J. Wang, Q. Li, S. Chandarlapaty, H. Deng, W. Wu*, Y. Rao*, ‘Potent and Preferential Degradation of CDK6 via PROteolysis TArgeting Chimera Degraders. Journal of Medicinal Chemistry’, 2019, 62. DOI:10.1021/acs.jmedchem.9b00871.

2.         Y. Zong, F. Fang, K. J. Meyer, L. Wang, Z. Ni, H. Gao, K. Lewis, J. Zhang, Y. Rao*; ‘Gram-scale Total Synthesis of Teixobactin Promoting Binding Mode Study and Discovery of More Potent Antibiotic’, Nature communications, 2019, 10, DOI: 10.1038/s41467-019-11211-y.

3.        X. Yao, X. Sun, S. Jin, L. Yang, H. Xu, Y. Rao*, Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis, Journal of Medicinal Chemistry, 2019, 62DOI: 10.1021/acs.jmedchem.9b00329.

4.        Y. Yang, L. Cao, H. Gao, Y. Wu, Y. Wang, F. Fang, T. Lan, Z. Lou*, Y. Rao*, ‘Discovery, Optimization and Target Identification of Novel Potent Broad-Spectrum Antiviral Inhibitors’, Journal of Medicinal Chemistry, 2019, 62, DOI: 10.1021/acs.jmedchem.9b00091.

5.        Y. Sun, N. Ding, Y. Song, Z. Yang, W. Liu *, J. Zhu*, Y. Rao*, ‘Degradation of Bruton's tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant Non-Hodgkin lymphomas’, Leukemia, 2019, 33, DOI: 10.1038/s41375-019-0440-x.

6.        X. Sun, J. Wang, X. Yao, W. Zheng, Y. Mao, T. Lan, L. Wang, Y. Sun, X. Zhang, Q. Zhao, J. Zhao, R-P. Xiao, X. Zhang*, G. Ji*, Y. Rao*, ‘A Chemical Approach for Global Protein Knockdown from Mice to Non-human Primates’, Cell Discovery, 2019, DOI: 10.1038/s41421-018-0079-1. (Highlighted in Cell Research)

7.        Z. An, W. Lv, S. Su, W. Wu*, Y. Rao*, ‘Developing potent PROTACs tools for selective degradation of HDAC6 protein’, Protein & Cell, 2019, DOI: 10.1007/s13238-018-0602-z. (in press)

8.        Q. Zhao, T. Lan, S. Su, Y. Rao*, ‘Induction of Apoptosis in MDA-MB-231 Breast Cancer Cells by a PARP1-Targeting PROTAC Small Molecule’, Chem. Commun., 2019, 55, 369-372. DOI: 10.1039/c8cc07813k.

9.        X. Yang, X. Chen, Z. Yang, Y. Xi, L. Wang, Y. Wu, Y. Yan*, Y. Rao*,Synthesis, Evaluation, and Structure-Activity Relationship Study of Lanosterol Derivatives To Reverse Mutant-Crystallin-Induced Protein Aggregation’, Journal of Medicinal Chemistry, 2018, 61, 8693-8706. DOI: 10.1021/acs.jmedchem.8b00705.

10.     Y. Wang; S. Chi; G. Li; L. Wang; Q. Zhao; Y. Rao; L. Zu; W. He; B. Xiao*; ‘A lever-like transduction pathway for long-distance chemical- and mechano-gating of the mechanosensitive Piezo1 channel’, Nature communications, 2018, 9DOI: 10.1038/s41467-018-03570-9.

11.     Y. Sun, X. Zhao, N. Ding, H. Gao, Y. Wu, Y. Yang, M. Zhao, J. Hwang, Y. Song, W. Liu *, Y. Rao*,PROTAC-Induced BTK Degradation as a Novel Therapy for Mutated BTK C481S Induced Ibrutinib-Resistant B-Cell Malignancies’, Cell Research, 2018, 22, 779–781. DOI:10.1038/s41422-018-0055-1.

12.     Y. Zong, X. Sun, H. Gao, K. Meyer, K. Lewis, Y. Rao*, ‘Developing Equipotent Teixobactin Analogues Against Drug-Resistant Bacteria and Discovering A Hydrophobic Interaction Between Lipid II and Teixobactin’, Journal of Medicinal Chemistry, 2018, 61, 3409-3421. DOI:10.1021/acs.jmedchem.7b01241.

13.     C. Zhang, Y. Song, Z. Sang, L. Zhan, Y. Rao*, ‘Mixing O-Containing and N-Containing Directing Groups for C-H Activation: A Strategy for the Synthesis of Highly Functionalized 2,2'-Biaryls’,  Journal of Organic Chemistry, 2018, 83, 2582-2591. DOI:10.1021/acs.joc.7b02863.

14.     Y. Wu, Y. Zong, Y. Sun, A. Tan,* Y. Rao*, ‘Design and synthesis of CNX-774 analogues as BTK-related cancer inhibitors’, Chinese Journal of Medicinal Chemistry, 2018, 28, 276-284.    1005-0108(2018)28:4<276:DBXGAX>2.0.TX;2-4.

15.     G. Dong, W. Chen, X. Wang, X. Yang, T. Xu, P. Wang, W. Zhang, Y. Rao*, C. Miao*, C. Sheng*, ‘Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors’, Journal of Medicinal Chemistry, 2017, 60, 7965–7983. DOI: 10.1021/acs.jmedchem.7b00467.

16.     H. Gao, Z. Yang, X. Yang, Y. Rao*, ‘Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors’, Bioorganic & Medicinal Chemistry, 2017, 25, 4553-4559. DOI:10.1016/j.bmc.2017.06.004.

17.     X. Yao, L. Jin, Y. Rao*, ‘Synthesis of Phosphaisoquinolin-1-one by Annulation of Aryl Phosphinamides with Allenes through Cobalt-Promoted C-H Functionalization’, Asian JOC, 2017, 6, 825-830. DOI:10.1002/ajoc.201700215.

18.     T. Lan, L. Wang, Y. Rao*, ‘Regioselective Annulation of Aryl Sulfonamides with Allenes through Cobalt-Promoted C-H Functionalization’, Org. Lett. 2017, 19, 972-975. DOI:10.1021/acs.orglett.6b03510.

19.     Y. Yang, Y. Yu, X. Li, J. Li, Y. Wu, J. Yu, J. Ge, Z. Huang, L. Jiang*; Y. Rao*, M. Yang*, ‘Target Elucidation by Cocrystal Structures of NADH-Ubiquinone Oxidoreductase of Plasmodium falciparum (PfNDH2) with Small Molecule To Eliminate Drug-Resistant Malaria Journal of Medicinal Chemistry, 2017, 60, 1994-2005. DOI:10.1021/acs.jmedchem.6b01733.

20.     X. Yang, G. Shan, Z. Yang, G. Huang, G. Dong, C. Sheng*, Y. Rao*One-Step Synthesis of Quaternary Carbon Centered Cyclobutanes via Pd(II)-catalyzed Cascade C(sp3)-H Activations’, Chem. Commun., 2017, 53, 1534-1537. DOI:10.1039/c6cc06897a.

21.     T. Li, C. Zhang, Y. Tan, W. Pan and Y. Rao*Cobalt-catalyzed C-H activation and regioselective intermolecular annulation with allenes’, Org. Chem. Front., 2017, 4, 204-209.<span style="font-size:14px;line-height:150%;font-family:"&color:#2A2D35">  DOI:10.1039/c6qo00567e.

22.     C. Zhang, T. Li, L. Wang and Y. Rao*Synthesis of diverse heterocycles via one-pot cascade cross-dehydrogenative-coupling (CDC)/cyclization reaction’, Org. Chem. Front., 2017, 4, 386-391. DOI:10.1039/c6qo00522e.

23.     X. Sun, Y. Sun, Y. Rao* ‘Cyclobutanones as Useful Synthons for the Preparation of Bioactive Molecules and Fused-Ring Chemicals’. Current Organic Chemistry, 2016, 20 (18), 1878-1901. (Invited review) DOI:10.2174/1385272820666160331235519.

24.     Y. Lin, X. Yang, W. Pan*, and Y. Rao.* " One-Step Synthesis of Diverse Pyridine-Containing Heterocycles with 3-Ethoxycyclobutanones at Room Temperature". Org. Lett. 2016, 18, 2304-2307. DOI:10.1021/acs.orglett.6b01027.

25.     X. Yang, Y. Sun, T. Sun, and Y. Rao.* "Auxiliary-assisted palladium-catalyzed halogenation of unactivated C(sp3)-H bonds at room temperature". Chem. Commun., 2016, 52, 6423-6426.  DOI:10.1039/c6cc00234j.

26.     X. Yang, G. Shan, L. Wang, Y. Rao* ‘Recent advances in transition metal (Pd, Ni)-catalyzed C(sp3)-H bond activation with bidentate directing groups’. Tetrahedron Letters, 2016, 57, 819-836. DOI:10.1016/j.tetlet.2016.01.009.

27.     X. Yang, T. Sun, Y. Rao* ‘A Preliminary Study of Diastereoselectivity in Pd(II)-catalyzed C(sp3)-H Alkoxylation of Cyclic system’. Chem. Eur. J., 2016, 22, 3273-3277. DOI:10.1002/chem.201503967.

28.     Y. Sun, T. Sun, Y. Wu, X. Zhang*, and Y. Rao* ‘A Diversity-Oriented Synthesis of Bioactive Benzanilides by a Regioselective C(sp2)-H Hydroxylation Strategy’. Chemical Science, 2016, 7, 2229-2238. DOI:10.1039/c5sc03905c.

29.     C. Zhang and Y. Rao*. ‘Weak Coordination Promoted Regioselective Oxidative Coupling Reaction for 2,2’-Difunctional Biaryl Synthesis in Hexafluoroisopropanol’. Org. Lett. 2015, 17, 4456-4459 . DOI:10.1021/acs.orglett.5b02115.

30.     G. Shan, G. Huang, Y. Rao*, H. Zhang*. ‘Palladium-catalyzed ortho-selective C-H bond chlorination of aromatic ketones", Chinese Chem. Lett., 2015, 26, 1236-1240.

31.     J. Hu, T. Lan, Y. Sun, H. Chen*, J. Yao, and Y. Rao*. ‘ Unactivated C(sp3)-H Hydroxylation through Palladium Catalysis with H2O as the Oxygen Source’ . Chem. Commun., 2015, 51, 14929-14932. DOI:10.1039/c5cc04952k.

32.     Y. Lin, L. Zhu, Y. Lan* and Y. Rao*. ‘Development of Rhodium(II)-Catalyzed Chemoselective C(SP3)-H Oxygenation’. Chem. Eur. J., 2015, 21, 14937-14942. DOI:10.1002/chem.201502140.

33.     X. Sun, X. Yao, C. Zhang, and Y. Rao*. ‘Palladium Catalyzed ortho C-H Iodination of Phenylcarbamates at Room Temperature with Cyclic Hypervalent Iodine Reagents’. Chem. Commun., 2015, 51, 10014-10017. DOI:10.1039/C5CC02533H

34.     G. Shan, G. Huang and Y. Rao*. ‘Palladium Catalyzed unactivated β-methylene C(sp3)-H Bond Alkenylation of Aliphatic Amides and Application in A sequential C(sp3)-H/C(sp2)-H Bond Alkenylation’. Org. Biomol. Chem. 2015, 13, 697-701. DOI: 10.1039/c4ob02389g.

35.     S. Chen, G. Shan, P. Nie and Y. Rao*. ‘3-Alkyloxycyclobutanones as Useful Synthons for Heterocycle and Carbocycle Synthesis’. Asian JOC, 2015, 4, 16-26. (Invited review)  DOI: 10.1002/ajoc.201402200.

36.     Y. Yang, Z. Chen and Y. Rao*. ‘Synthesis of Diarylsulfones with Simple Arenes and K2S2O8 through Double C-S Bond Formation. Chem. Commun., 2014, 50, 15037 -15040. DOI: 10.1039/c4cc05964f.

37.     Y. Zong and Y. Rao*. ‘Developing Pd(II) catalyzed double sp3 C-H alkoxylation for synthesis of symmetric and unsymmetric acetals’. Org. Lett. 2014, 16, 5278-5281. DOI: 10.1021/ol502377x.

38.     Y. Rao*, G. Shan, X. Yang. ‘Some recent advances in transition-metal-catalyzed ortho SP2 C–H functionalization using Ru, Rh, and Pd’, Science China Chemistry, 2014, 57, 930–944. (Invited review) DOI: 10.1007/s11426-014-5130-y.

39.     X. Yang, Y. Sun, Z. Chen, Y. Rao*. ‘A General Approach towards Catechol and Pyrogallol through Ruthenium and Palladium-Catalyzed C-H Hydroxylation by Weak Coordination’. Adv. Synth. Catal. 2014, 356, 1625-1630. DOI: 10.1002/adsc.201300999.

40.     X. Sun, Y. Sun, Y. Rao*. ‘A gram-scale synthesis of multi-substituted arenes via palladium catalyzed C-H halogenation’. Chinese Chem. Lett., 2014, 25, 667-669. (Invited paper) DOI: 10.1016/j.cclet.2014.03.021.

41.     J. Hu, H. Xu, P. Nie, X. Xie, Z. Nie* and Y. Rao*. ‘Synthesis of Indazoles and Azaindazoles by Aerobic Oxidative C-N Coupling under Transition Metal Free Conditions’. Chem. Eur. J., 2014, 20, 3932-3938. (Highlighted by SynFacts 2014, 10(7), 0690) DOI: 10.1002/chem.201304923.

42.     X. Sun, Y. Sun, C. Zhang, and Yu Rao*. ‘Room-Temperature Palladium-Catalyzed C-H Chlorination by Weak Coordination: One-Pot Synthesis of 2-Chlorophenols with Excellent Regioselectivity’. Chem. Commun., 2014, 50, 1262-1264. DOI: 10.1039/c3cc47431c.

43.     G. Shan, X. Yang, Y. Zong and Y. Rao*. ‘An Efficient Palladium Catalyzed C-H Alkoxylation of Unactivated Methylene and Methyl Groups with Cyclic Hypervalent Iodine (I3+) Oxidants’. Angew. Chem. Int. Ed. 2013, 52, 13606-13610. DOI: 10.1002/anie.201311147.

44.     Y. Rao*. ‘Pd-Catalyzed sp2 C-H Hydroxylation with TFA/TFAA via Weak Coordinations’. SYNLETT, 2013, 24, 2472-2476. (Invited paper) DOI: 10.1055/s-0033-1339871.

45.     X. Yang, G. Shan, and Y. Rao*. ‘Synthesis of 2-Aminophenols and Heterocycles by Ru Catalyzed Mono- and Double C-H Hydroxylation’. Org. Lett. 2013, 15, 2334–2337. DOI: 10.1021/ol400437a. DOI: 10.1021/ol400437a.

46.     X. Sun, G. Shan, Y. Sun, and Y. Rao*. ‘A General Approach for Regio- and Chemoselective C-H Chlorination/Bromination of Electron-Deficient Arenes via Weak Coordination and A Preliminary Study of Priority Order of Relative Directing Group Ability’. Angew. Chem. Int. Ed. 2013, 52, 4440-4444. DOI: 10.1002/anie.201300176.

47.     G. Shan, X. Han, Y.Lin, S. Yu,a and Yu Rao*. ‘Broadening the Catalyst and Reaction Scope of Regio- and Chemoselective C-H Oxygenation: A Convenient and Scalable Approach to 2-Acylphenols by Intriguing Rh(II) and Ru(II) Catalysis’. Org. Biomol. Chem. 2013, 11, 2318-2322. (Highlighted by OBC as a hot article) DOI: 10.1039/c3ob27457h.

48.     G. Shan, X. Yang, L. Ma, and Y. Rao*. ‘Pd-Catalyzed C-H Oxygenation with TFA/TFAA: Expedient Access to Oxygen-Containing Heterocycles and Late-Stage Drug Modification’. Angew. Chem. Int. Ed. 2012, 51, 13070-13074. (Highlighted by SYNPACTS and Chin. J. Org. Chem) DOI: 10.1002/anie.201207458.

49.     L. Sun, X. Zeng, C. Yan, X. Sun, X. Gong, Y. Rao and Nieng Yan*, ‘Crystal structure of a bacterial homologue of glucose transporters GLUT1–4’. Nature, 2012, 490, 361-366. DOI: 10.1038/nature11524.

50.     J. Hu, S. Chen, Y. Sun, J. Yang, and Y. Rao*. ‘Synthesis of Tri- and Tetrasubstituted Pyrazoles via Ru(II) Catalysis: Intramolecular Aerobic Oxidative C–N Coupling’. Org. Lett. 2012, 14, 5030-5033. (Highlighted by SynFacts 2012, 8(12), 1304) DOI: 10.1021/ol3022353.

51.     Y. Yang, Y. Lin, and Y. Rao*. ‘Ruthenium(II)-Catalyzed Synthesis of Hydroxylated Arenes with Ester as an Effective Directing Group’. Org. Lett. 2012, 14, 2874-2877. DOI: 10.1021/ol301104n.

52.     Yongfeng Cheng, Xuesong Han, Huangche Ouyang, and Y. Rao*. ‘A New Practical Approach Towards the Synthesis of Unsymmetric and Symmetric 1,10-Phenanthroline Derivatives at Room Temperature’. Chem. Commun., 2012, 48, 2906-2908. DOI: 10.1039/c2cc17208a.

53.     Pengfei Liu, Gang Shan, Shi Chen and Y. Rao*.A New Regio- and Stereoselective Synthesis of β-Enamino Ketones with 3-Ethoxycyclobutanones and Substituted Amines’. Tetrahedron Lett. 2012, 53, 936-939. DOI: 10.1016/j.tetlet.2011.12.040.

54.     G. Shan, X. Sun, Q. Xia and Y. Rao*. ‘A Facile Synthesis of Substituted 2-Alkylquinolines Through [3+3] Annulation between 3-Ethoxycyclobutanones and Aromatic Amines at Room Temperature’. Org. Lett. 2011, 13, 5770-5773. DOI: 10.1021/ol202334s.

55.     J. Hu, Y. Cheng, Y. Yang and Y. Rao*. ‘A general and efficient approach to 2H-indazoles and 1H-pyrazoles through copper-catalyzed intramolecular N–N bond formation under mild conditions’. Chem. Commun., 2011, 47, 10133-10135. DOI: 10.1039/c1cc13908h.

56.     G. Shan, P. Liu and Y. Rao*. ‘A New Synthesis of Pyrazoles through Lewis Acid-Catalyzed-Union of 3-Ethoxycyclobutanones with Monosubstituted Hydrazines’. Org. Lett. 2011, 13, 1746-1749. DOI: 10.1021/ol2002682.