魯桂，女，1971年7月生，教授，博士生導師。1993年和1996年分獲浙江大學學士、碩士學位，2003年獲香港理工大學有機化學博士學位。1996-2005年在浙江大學化學系工作，曆任助教、講師、副教授；2003-2004年香港理工大學博士後；2005-2006年德國Erlangen-Nürnberg大學洪堡學者。2006年10月起任教太阳集团1088vip，2007年入選教育部新世紀優秀人才支持計劃。主要從事新型抗病毒、抗腫瘤藥物的設計、合成和生物活性研究；藥物及其中間體高效合成方法的研究；不對稱催化反應和手性催化劑的設計合成。目前已在國内外核心專業期刊上發表學術論文60餘篇，其中IF>5.0的有15篇，申請國内外專利18項，授權12項，論文他引超過1000次。先後主持國家自然科學基金、國家863計劃子課題、第7屆歐盟框架項目分課題、科技部對歐盟科技合作專項經費、廣東省引進創新科研團隊項目分課題、教育部留學回國人員科研啟動基金、廣東省自然科學基金以及廣州市科技計劃等。

教學情況

本科生《有機化學》、研究生《現代制藥工藝學》等課程。

研究方向

(1) 新型抗病毒、抗腫瘤藥物的設計、合成和生物活性研究；

(2) 藥物及其中間體高效合成方法的研究；

(3) 不對稱催化反應和手性催化劑的設計合成。

科研項目

(1) 國家自然科學基金面上項目：靶向Aurora A和PI3K信号通路的新型乳腺癌治療藥物的分子構建及作用機制研究，負責人，2020-2023年。

(2) 教育部新世紀優秀人才支持計劃，2007-2010年。

(3) 科技部對歐盟科技合作專項經費：有機催化方法合成易得、經濟和高産的達菲及其衍生物，負責人，2008-2011年。

(4) 第7屆歐盟框架項目：Organocatalytic approaches towards easily synthesized, economical and high yielding Tamiflu derivatives，分課題負責人，2008-2011年。

(5) 教育部留學回國人員科研啟動基金，2008-2011年。

(6) 廣東省引進創新科研團隊項目：重大人類緻病病毒特異性藥物的研發與免疫細胞的再生工程，分課題負責人，2010-2015年。

代表性科研論文

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. 尤義鵬，聶林，劉晉彪，豐亞輝，魯桂*。新型磷酰胺類神經氨酸酶抑制劑的設計合成及抗病毒活性研究。高等學校化學學報，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.

授權發明專利

  1. 一種具有抗乙肝病毒活性和抗菌活性的苯并咪唑類化合物及其合成方法和應用，中國發明專利，授權時間：2022.02.22。
  2. 一種手性氨基化合物及其制備方法和應用、及由其制備依度沙班中間體的制備方法，中國發明專利，授權時間：2021.10.26。
  3. Aurora激酶抑制劑在制備抑制腫瘤微環境藥物方面的應用，中國發明專利，授權時間：2021.02.19。
  4. 一種嘧啶化合物及其制備方法和應用，中國發明專利，授權時間：2019.06.18。
  5. 選擇性Aurora A激酶抑制活性的喹唑啉衍生物及其制備方法以及應用，中國發明專利，授權時間：2019.06.04。
  6. 一種3,3’-雙吲哚化合物的制備方法，中國發明專利，授權時間：2018.08.03。
  7. 具有Aurora激酶抑制活性的取代喹唑啉類衍生物及其制備方法以及應用，中國發明專利，授權時間：2018.06.29。
  8. 神經氨酸酶抑制劑及制備方法及在制備抗流感病毒藥物中的應用，中國發明專利，授權時間：2018.01.23。
  9. PI3K激酶抑制劑，包含其的藥物組合物及其應用，中國發明專利，授權時間：2016.07.06。
  10. 嘧啶化合物、PI3K抑制劑、包含PI3K抑制劑的藥物組合物及應用，中國發明專利，授權時間：2016.04.27。
  11. Intermediates for antiviral drugs and method of their preparation, 歐洲發明專利，授權時間：2015.12.02。
  12. 一種嘧啶衍生物在制備預防和/或治療和/或輔助治療腫瘤的藥物中的用途，中國發明專利，授權時間：2015.11.25。
  13. 一種嘧啶衍生物在制備預防和/或治療和/或輔助治療癌症的藥物中的用途，中國發明專利，授權時間：2015.04.29。
  14. 具有Aurora激酶抑制活性的嘧啶衍生物及其制備方法以及應用，中國發明專利，授權時間：2015.04.22。
  15. 一種醋酸阿比特龍的制備方法，中國發明專利，授權時間：2015.04.15。
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