鲁桂

鲁桂

教授

研究领域：(1) 新型抗病毒、抗肿瘤药物的设计、合成和生物活性研究；
(2) 药物及其中间体高效合成方法的研究；
(3) 不对称催化反应和手性催化剂的设计合成。

办公电话： 020-39943048

联系邮箱： lugui@mail.sysu.edu.cn

鲁桂，女，1971年7月生，教授，博士生导师。1993年和1996年分获浙江大学学士、硕士学位，2003年获香港理工大学有机化学博士学位。1996-2005年在浙江大学化学系工作，历任助教、讲师、副教授；2003-2004年香港理工大学博士后；2005-2006年德国Erlangen-Nürnberg大学洪堡学者。2006年10月起任教bm11222宝马娱乐网站，2007年入选教育部新世纪优秀人才支持计划。主要从事新型抗病毒、抗肿瘤药物的设计、合成和生物活性研究；药物及其中间体高效合成方法的研究；不对称催化反应和手性催化剂的设计合成。目前已在国内外核心专业期刊上发表学术论文60余篇，其中IF>5.0的有15篇，申请国内外专利18项，授权12项，论文他引超过1000次。先后主持国家自然科学基金、国家863计划子课题、第7届欧盟框架项目分课题、科技部对欧盟科技合作专项经费、广东省引进创新科研团队项目分课题、教育部留学回国人员科研启动基金、广东省自然科学基金以及广州市科技计划等。

教学情况

本科生《有机化学》、研究生《现代制药工艺学》等课程。

研究方向

(1) 新型抗病毒、抗肿瘤药物的设计、合成和生物活性研究；

(2) 药物及其中间体高效合成方法的研究；

(3) 不对称催化反应和手性催化剂的设计合成。

科研项目

(1) 国家自然科学基金面上项目：靶向Aurora A和PI3K信号通路的新型乳腺癌治疗药物的分子构建及作用机制研究，负责人，2020-2023年。

(2) 教育部新世纪优秀人才支持计划，2007-2010年。

(3) 科技部对欧盟科技合作专项经费：有机催化方法合成易得、经济和高产的达菲及其衍生物，负责人，2008-2011年。

(4) 第7届欧盟框架项目：Organocatalytic approaches towards easily synthesized, economical and high yielding Tamiflu derivatives，分课题负责人，2008-2011年。

(5) 教育部留学回国人员科研启动基金，2008-2011年。

(6) 广东省引进创新科研团队项目：重大人类致病病毒特异性药物的研发与免疫细胞的再生工程，分课题负责人，2010-2015年。

代表性科研论文

1. Zhang, B.‡; Zhu, C.‡; Chan, A. S. C.; Lu, G.* Discovery of the first-in-class Aurora A covalent inhibitor for the treatment of triple negative breast cancer. Eur. J. Med. Chem. 2023, 256, 115457.

2. Zeng, W.-T.‡; Han, X.‡; Huang, G.-B.; Weng, J.; Chan, A. S. C.; Lu, G.* Cooperative NHC and nickel-catalyzed asymmetric reductive coupling of nitrobenzyl bromides and cyclic ketimines via SET process. Org. Chem. Front. 2023, 10(6), 1463–1469.

3. Guo, J.‡; Xie, Y.‡; Lai, Z.-M.; Weng, J.*; Chan, A. S. C.; Lu, G.* Enantioselective hydroalkylation of alkenylpyridines enabled by merging photoactive electron donor-acceptor complexes with chiral bifunctional organocatalysis. ACS Catal. 2022, 12, 13065–13074.

4. Zhu, W.-R.‡; Su, Q.‡; Deng, X.-Y.; Liu, J.-S.; Zhong, T.; Meng, S.-S.; Yi, J.-T.; Weng, J.*; Lu, G.* Organocatalytic enantioselective SN1-type dehydrative nucleophilic substitution: Access to bis(indolyl)methanes bearing quaternary carbon stereocenters. Chem. Sci. 2022, 13, 170–177.

5. Yi, J.-T.; Zhou, X.; Chen, Q.-L.; Chen, Z.-D.; Lu, G.*; Weng, J.* Copper-catalyzed direct decarboxylative fluorosulfonylation of aliphatic carboxylic acids. Chem. Commun., 2022, 58, 9409–9412.

6. Zhong, T.; Chen, Z.; Yi, J.; Lu, G.*; Weng, J.* Recent progress in the synthesis of sulfonyl fluorides for SuFEx click chemistry. Chin. Chem. Lett. 2021, 9, 2736–2750.

7. Zhu, W.-R.; Liu, K.; Weng, J.*; Huang, W.-H.; Huang, W.-J.; Chen, Q.; Lin, N.*; Lu, G.* Catalytic asymmetric synthesis of vicinal tetrasubstituted diamines via umpolung cross-Mannich reaction of cyclic ketimines. Org. Lett. 2020, 22, 5014–5019.

8. Zhu, W.-R.; Su, Q.; Diao, H.-J.; Wang, E.-X.; Wu, F.; Zhao, Y.-L.; Weng, J.*; Lu, G.* Enantioselective dehydrative γ-arylation of α-indolyl propargylic alcohols with phenols: Access to chiral tetrasubstituted allenes and naphthopyrans. Org. Lett. 2020, 22, 6873–6878.

9. Guo, J.; Xie, Y.; Zeng, W.-T.; Wu, Q.-L.; Weng, J.*; Lu, G.* Visible-light catalyzed [1+2+2] cycloaddition reactions enabled by the redox-neutral formation of methylene nitrones. Adv. Synth. Catal. 2020, 362, 5450–5456.

10. Wang, J.‡; Zhang, L.‡; Huang, Z.; Zhang, X.; Jiang, Y.; Liu, F.; Long, L.; Xue, M.; Lu, G.*; Liu, Q.*; Long, Z.* Aurora kinase inhibitor restrains STAT5-activated leukemic cell proliferation by inducing mitochondrial impairment. J. Cell. Physiol. 2020, 235, 8358–8370.

11. Wang, J.-D.‡; Zhang, W.‡; Zhang, J.-W.; Zhang, L.; Wang, L.-X.; Zhou, H.-S.; Long, L.; Lu, G.*; Liu, Q.*; Long, Z.-J.* A novel aurora kinase inhibitor attenuates leukemic cells proliferation induced by mesenchymal stem cells. Mol. Ther.–Oncolytics 2020, 18, 491–503.

12. Huang, W.-H.‡; Huang, G.-B.‡; Zhu, W.-R.; Weng, J.*; Lu, G.* Transition metal-free synthesis of α-aryl ketones via oxyallyl cation capture with arylboronic acids. Org. Chem. Front. 2020, 7, 2480–2485.

13. Zhu, W.-R.; Su, Q.; Lin, N.*; Chen, Q.; Zhang, Z.-W.; Weng, J.; Lu, G.* Organocatalytic synthesis of chiral CF3-containing oxazolidines and 1,2-amino alcohols: Asymmetric oxa-1,3-dipolar cycloaddition of trifluoroethylamine-derived azomethine ylide. Org. Chem. Front. 2020, 7, 3452–3458.

14. Wu, Q.-L.‡; Guo, J.‡; Huang, G.-B.; Chan, A. S. C.; Weng, J.*; Lu, G.* Visible-light-promoted radical cross-coupling of para-quinone methides with N-substituted anilines: An efficient approach to 2,2-diarylethylamines. Org. Biomol. Chem. 2020, 18, 860–864.

15. Luo, R.-S.; Chen, M.-M.; Ouyang, L.; Chan, A. S. C.; Lu, G.* Enantioselective Reformatsky reaction of ketones catalyzed by chiral indolinylmethanol. Eur. J. Org. Chem. 2020, 4805–4811.

16. Xiong, Y.-S.‡; Yu, Y.‡; You, Y.-P.; Weng, J.*; Lu, G.* Metal-free aerobic sulfenyllactonization of unsaturated carboxylic acids with thiols using air as sole oxidant. ChemistrySelect 2020, 5, 7382–7386.

17. 尤义鹏，聂林，刘晋彪，丰亚辉，鲁桂*。新型磷酰胺类神经氨酸酶抑制剂的设计合成及抗病毒活性研究。高等学校化学学报，2020, 41, 2279–2286.

18. Huang, G.-B.; Huang, W.-H.; Guo, J.; Xu, D.-L.; Qu, X.-C.; Zhou, G.-L.; Zheng, X.-H.; Zhai, P.-H.; Weng, J.*; Lu, G.* Enantioselective synthesis of triarylmethanes via organocatalytic 1,6-addition of arylboronic acids to para-quinone methides. Adv. Synth. Catal. 2019, 361, 1241–1246.

19. Xiong, Y.-S.; Zhang, B.; Yu, Y.; Weng, J.*; Lu, G.* Construction of sulfonyl phthalides via copper-catalyzed oxysulfonylation of 2-vinylbenzoic acids with sulfinates. J. Org. Chem. 2019, 84, 13465–13472.

20. Guo, J.; Huang, G.-B.; Wu, Q.-L.; Xie, Y.; Weng, J.*; Lu, G.* An efficient approach to access 1,1,2-triarylethanes enabled by the organo-photoredox-catalyzed decarboxylative addition reaction. Org. Chem. Front. 2019, 6, 1955–1960.

21. Xie, L.-H.; Cheng, J.; Luo, Z.-W.; Lu, G.* Mannich reaction of indole with cyclic imines in water. Tetrahedron Lett. 2018, 59, 457–461.

22. Xiong, Y.-S.; Yu, Y.; Weng, J.*; Lu, G.* Copper-catalyzed peri-selective direct sulfenylation of 1-naphthylamines with disulfides. Org. Chem. Front. 2018, 5, 982–989.

23. Long, L.; Luo, Y.; Hou, Z.-J.; Ma, H.-J.; Long, Z.-J.; Tu, Z.-C.; Huang, L.-J.; Liu, Q.*; Lu, G.* Synthesis and biological evaluation of aurora kinases inhibitors based on N-trisubstituted pyrimidine scaffold. Eur. J. Med. Chem. 2018, 145, 805–812.

24. Xiong, Y.-S.; Weng, J.*; Lu, G.* Manganese(III)-mediated and -catalyzed decarboxylative hydroxysulfonylation of arylpropiolicacids with sodium sulfinates in water. Adv. Synth. Catal. 2018, 360, 1611–1616.

25. Zhu, W.-R.‡; Chen, Q.‡; Lin, N.*; Chen, K.-B.; Zhang, Z.-W.; Fang, G.; Weng, J.; Lu, G.* Organocatalytic Michael/cyclization cascade reactions of 3-isothiocyanato oxindoles with 3-trifluoroethylidene oxindoles: Approach for the synthesis of 3’-trifluoromethyl substituted 3,2’-pyrrolidinyl-bispirooxindoles. Org. Chem. Front. 2018, 5, 1375–1380.

26. Guo, J.; Xie, Y.; Wu, Q.-L.; Zeng, W.-T.; Chan, A. S. C.; Weng, J.*; Lu, G.* Copper-catalyzed aerobic decarboxylative coupling between cyclic α-amino acids and diverse C–H nucleophiles with low catalyst loading. RSC Adv. 2018, 8, 16202–16206.

27. Li, J.-M.‡; Yu, Y.‡; Weng, J.*; Lu, G.* Nickel-catalyzeddirect C-H Bond sulfenylation of arylhydrazines. Org. Biomol. Chem. 2018, 16, 6047–6056.

28. Long, L.‡; Wang, Y.-H.‡; Zhuo, J.-X.‡; Tu, Z.-C.; Wu, R.; Yan, M.*; Liu, Q.*; Lu, G.* Structure-based drug design: Synthesis and biological evaluation of quinazolin-4-amine derivatives as selective aurora A kinase inhibitors. Eur. J. Med. Chem. 2018, 157, 1361–1375.

29. Guo, J.; Wu, Q.-L.; Xie, Y.; Weng, J.*; Lu, G.* Visible light photocatalytic direct decarboxylative alkylation of imines. J. Org. Chem. 2018, 83, 12559–12567.

30. Li, J.-M.; Wang, Y.-H.; Yu, Y.; Wu, R.-B.; Weng, J.*; Lu, G.* Copper-catalyzed remote C–H functionalizations of naphthylamides through coordinating activation strategy and single-electron-transfer (SET) mechanism. ACS Catal. 2017, 7, 2661–2667.

31. Zhang, J.-Q.; Luo, Y.-J.; Xiong, Y.-S.; Yu, Y.; Tu, Z.-C.; Long, Z.-J.; Lai, X.-J.; Chen, H.-X.; Luo, Y.; Weng, J.; Lu, G.* Design, synthesis, and biological evaluation of substituted pyrimidines as potential phosphatidylinositol 3-kinase (PI3K) inhibitors. J. Med. Chem. 2016, 59, 7268–7274.

32. Peng, W.; Tu, Z.-C.; Long, Z.-J.; Liu, Q.; Lu, G.* Discovery of 2-(2-aminopyrimidin-5-yl)-4- morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. Eur. J. Med. Chem. 2016, 108, 644–654.

33. Guo, J.; Lin, Z.-H.; Chen, K.-B.; Xie, Y.; Chan, A. S. C.; Weng, J.*; Lu, G.* Asymmetric amination of 2-substituted indolin-3-ones catalyzed by natural cinchona alkaloids. Org. Chem. Front. 2017, 4, 1400–1406.

34. Huang, W.-J.; Chen, Q.; Lin, N.*; Long, X.-W.; Pan, W.-G.; Xiong, Y.-S.; Weng, J.*; Lu, G.* Asymmetric synthesis of trifluoromethyl-substituted 3,3’-pyrrolidinyl-dispirooxindoles through organocatalytic 1,3-dipolar cycloaddition reactions. Org. Chem. Front. 2017, 4, 472–482.

35. Luo, Y.; Chen, H.; Weng, J.; Lu, G.* Synthesis of pelorol and its analogs and their inhibitory effects on phosphatidylinositol 3-kinase. Mar. Drugs, 2016, 14, 118.

36. Zhang, J.-Q.; Xiong, Y.-S.; Chan, A. S. C.; Lu, G.* Cu(II)-catalyzed cross-dehydrogenative coupling reaction of N’-acyl arylhydrazines and phosphites. RSC Adv. 2016, 6, 84587–84591.

37. Wang, L.-X.; Wang, J.-D.; Chen, J.-J.; Long, B.; Liu, L.-L.; Tu, X.-X.; Luo, Y.; Hu, Y.; Lin, D.-J.; Lu, G.*; Long, Z.-J.*; Liu, Q.* Aurora A kinase inhibitor AKI603 induces cellular senescence in chronic myeloid leukemia cells harboring T315I mutation. Sci. Rep. 2016, 6, 35533.

38. Weng, J.*; Wang, S.; Huang, L.-J.; Luo, Z.-Y.; Lu, G.* Stereoselective synthesis of epoxyisoprostanes: An organocatalytic and “pot-economy” approach. Chem. Commun. 2015, 51, 10170–10173.

39. Huang, L.-J.; Weng, J.*; Wang, S.; Lu, G.* Organocatalytic Diels-Alder reaction of 2-vinylindoles with methyleneindolinones: An efficient approach to functionalized carbazolespirooxindoles. Adv. Synth. Catal. 2015, 357, 993–1003.

40. Zheng, F.-M.; Long, Z.-J.; Hou, Z.-J.; Luo, Y.; Lai, X.-J.; Yan, M.; Lam, E. W.-F.; Lu, G.*; Liu, Q.* A novel small molecule aurora kinase inhibitor attenuates breast tumor-initiating cell and overcomes drug resistance. Mol. Cancer Ther. 2014, 13, 1991–2003.

41. Luo, Y.; Deng, Y.-Q.; Wang, J.; Long, Z.-J.; Tu, Z.-C.; Peng, W.; Zhang, J.-Q.; Liu, Q.*; Lu, G.* Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors. Eur. J. Med. Chem. 2014, 78, 65–71.

42. Long, Z.-J.; Wang, L.-X.; Zheng, F.-M.; Chen, J.-J.; Luo, Y.; Tu, X.-X.; Lin, D.-J.; Lu, G.*; Liu, Q.* A novel compound against oncogenic Aurora kinase A overcomes imatinib resistance and promotes differentiation in chronic myeloid leukemia cells. Int. J. Oncol. 2015, 46, 2488–2496.

授权发明专利

  1. 一种具有抗乙肝病毒活性和抗菌活性的苯并咪唑类化合物及其合成方法和应用，中国发明专利，授权时间：2022.02.22。
  2. 一种手性氨基化合物及其制备方法和应用、及由其制备依度沙班中间体的制备方法，中国发明专利，授权时间：2021.10.26。
  3. Aurora激酶抑制剂在制备抑制肿瘤微环境药物方面的应用，中国发明专利，授权时间：2021.02.19。
  4. 一种嘧啶化合物及其制备方法和应用，中国发明专利，授权时间：2019.06.18。
  5. 选择性Aurora A激酶抑制活性的喹唑啉衍生物及其制备方法以及应用，中国发明专利，授权时间：2019.06.04。
  6. 一种3,3’-双吲哚化合物的制备方法，中国发明专利，授权时间：2018.08.03。
  7. 具有Aurora激酶抑制活性的取代喹唑啉类衍生物及其制备方法以及应用，中国发明专利，授权时间：2018.06.29。
  8. 神经氨酸酶抑制剂及制备方法及在制备抗流感病毒药物中的应用，中国发明专利，授权时间：2018.01.23。
  9. PI3K激酶抑制剂，包含其的药物组合物及其应用，中国发明专利，授权时间：2016.07.06。
  10. 嘧啶化合物、PI3K抑制剂、包含PI3K抑制剂的药物组合物及应用，中国发明专利，授权时间：2016.04.27。
  11. Intermediates for antiviral drugs and method of their preparation, 欧洲发明专利，授权时间：2015.12.02。
  12. 一种嘧啶衍生物在制备预防和/或治疗和/或辅助治疗肿瘤的药物中的用途，中国发明专利，授权时间：2015.11.25。
  13. 一种嘧啶衍生物在制备预防和/或治疗和/或辅助治疗癌症的药物中的用途，中国发明专利，授权时间：2015.04.29。
  14. 具有Aurora激酶抑制活性的嘧啶衍生物及其制备方法以及应用，中国发明专利，授权时间：2015.04.22。
  15. 一种醋酸阿比特龙的制备方法，中国发明专利，授权时间：2015.04.15。
  16. 一种具有流感病毒神经氨酸酶抑制活性的环己烯化合物及其制备方法以及其应用，中国发明专利，授权时间：2015.03.01。