研究方向
面向當前創(chuàng)新藥物研究中的挑戰(zhàn),何偉研究組主要在下述兩個方向展開研究。(1)金屬納米有機催化。根據(jù)精細化學(xué)品和藥物合成的需求,我們立足于金屬納米材料的可控合成,通過調(diào)控催化劑活性來實現(xiàn)高效高選擇性的有機反應(yīng), 包括含硅化合物的合成化學(xué)和化學(xué)生物學(xué)研究; (2)基于片段的藥物發(fā)現(xiàn)。我們結(jié)合片段篩選和基于結(jié)構(gòu)的藥物設(shè)計,發(fā)現(xiàn)特異性靶向新型、可藥性低的蛋白靶點的功能有機小分子(如溴域蛋白、去泛素化酶等),并展開化學(xué)生物學(xué)及早期藥物發(fā)現(xiàn)工作。
科學(xué)貢獻
用硅來替代藥物分子中的碳的策略是藥物研發(fā)中的一個合理而又誘人的途徑。要實現(xiàn)這一策略,必須克服方法,合成和概念上的諸多挑戰(zhàn)。我們從發(fā)展新化學(xué)方法入手,合成了多種新型的硅替代藥物單元和藥物分子,并在臨床前研究中展示了這一策略的誘人前景。我們在研究中,使用多學(xué)科交叉手段,包括納米材料合成,有機化學(xué),藥物化學(xué),以及基于片段的藥物設(shè)計等,促進了這些手段的融合。
獎勵
2013年 清華大學(xué)“221”基礎(chǔ)研究青年人才計劃
2011,2015, 2016, Bayer Investigator Award
2012, 2013, Janssen Investigator Award
發(fā)表文章
1.Liu, C.; Zhang, Q.; Li, H.; Guo, S.; Xiao, B.; Deng, W.; Liu, L.;
*He, W. Cu/Fe Catalyzed Intermolecular Oxidative Amination of Primary Benzylic C-H Bonds.
Chem. Eur. J.
2016, DOI: chem.201600107. (HOT paper)
2.Zhang, Q.-W.; An, K.; Liu, L.-C.; Guo, S.; Jiang, C.; Guo, H.;
*He, W. Silacyclobutane: a New C-H Silylation Reagent.
Angew. Chem. doi
:
10.1002/anie.201602376
3.Zhao, C.; Liu, L-C.; Wang, J.; Jiang, C.; Zhang, Q.-W.;
*He, W.
Rh(I)-Catalyzed Insertion of Allenes into C?C Bonds of Benzocyclobutenols.
Org. Lett.
2016,
18, 328-331.
4.Guo, H.; Chen, X.; Zhao, C.;
*He, W. Suzuki-type Cross Coupling between Aryl Halides and Silylboranes for the Syntheses of Aryl Silanes.
Chem. Commun.
2015,
51, 17410 – 17412.
5.Ji, Y.; Wu, Y.; Zhao, G.; Wang, D.; Liu, L.;
He, W.; *Li, Yadong.
Porous bimetallic Pt-Fe nanocatalysts for highly efficient hydrogenation of acetone.
Nano Research
2015.
8, 2706-2713.
6.Zhang, Q.; An, K.;
*He, W.
Rh Catalyzed Enantioselective Intramolecular C-H Silylation for the Syntheses of Planar Chiral Metallocene Siloles.
Angew. Chem. Int. Ed.,
2015,
54, 6918-6921.
7.Guo, H.; Xiuling Y;, Zhi, Y.; Li,Z.; Wu, C.; Zhao, C.; Wang, J.; Yu, Z.; *Ding, Y.;
*He, W.; Li. Y.
Nanostructuring Gold Wires for Highly Durable Nanocatalysts toward Selective reduction of nitro compounds and azides with organosilanes.
Nano Research
2015,
8, 1365-1372 (Cover story)
8.Xiao, B.; Niu, Z.; Wang, Y.; Jia, W.; Shang, J.; Zhang, L.; Wang, D.; Fu, Y.; Zeng, J.;
He, W.; Wu, K.; Li, J.; Yang, J.; *Liu, L.; *Li, Y.
Copper Nanocrystal Plane Effect on Stereoselectivity of Catalytic Deoxygenation of Aromatic Epoxides.
J. Am. Chem. Soc.
2015,
137, 3791-3794.
9.Zhang, Q.; An, K.;
*He, W.
Catalytic Synthesis of π-Conjugated Silole through Si-C (sp3) Bond Activation.
Synlett,
2015,
26, 1145-1152.
10.Dang, S.; Wu, S.; Wang, J.; Li, H.; Huang, M.;
He, W.; Li, Y.; Wong, C. C. L.; *Shi, Y.
Cleavage of amyloid precursor protein by an archaeal presenilin homologue PSH.
PNAS
2015,
112, 3344-3349.
11.Zhao, C.; Jiang, C.; Wang, J.; Wu, C.; Zhang, Q.;
*He, W.
Enantioselective Syntheses of α-Silyl Amines via a Copper-N-HeterocyclicCarbene Catalyzed Nucleophilic Silicon Transfer to Imines.
Asian. J. Org. Chem.
2014,
3, 851-855. (Cover story)
12.Zhang, Z.; Chen, Y.; He, S.; Zhang, J.; Xu, X.; Yang, Y.; Nosheen, F.; Saleem, F.;
He, W.;*Wang, X.
Hierarchical Zn/Ni-MOF-2 Nanosheet-Assembled Hollow Nanocubes for Multicomponent Catalytic Reactions.
Angew. Chem. Int. Ed.,
2014,
53, 12517-12521.
13.Zhang, Q.; An, K.;
*He, W.
Rh Catalyzed Tandem Cyclization/Si-C Activation Reaction for the Synthesis of Siloles.
Angew. Chem. Int. Ed.
2014,
53, 5667-5671.
14.Zhang, Z.; Chen, Y.; Xu, X.; Zhang, J.; Xiang, G.;
He, W.; *Wang, X.
Well-Defined Metal-Organic Framework Hollow Nanocages.
Angew. Chem. Int. Ed.,
2014,
53, 429-433.
15.Li, L.; Niu, Z.; Cai, S.; Zhi, Y.; Li, H.; Rong, H.; Liu, L.; Liu, L.;
*He, W.; *Li, Y.
A PdAg Bimetallic Nanocatalyst for Selective Reductive Amination of Nitroarenes.
Chem. Comm.
2013,
49, 6843.
16.Zhang, Q.; Cai, S.; Li, L.; Chen, Y.; Rong, H.; Niu, Z.; Liu, J.;
*He, W.; *Li, Y.
Direct Syntheses of Vinyl Ethers from Benzyl Alcohols via Ag Nanoparticles Catalyzed Tandem Aerobic Oxidation.
ACS Catalysis,
2013,
3, 1681-1684.
17.Liu, J.; *Liu, C.;
*He, W.
Fluorophores and Their Applications as Molecular Probes in Living Cells.
Current Organic Chemistry
2013, 17, 564-579.
18.Huang, W.; Choi, W.; Chen, Y.; Zhang, Q.; Deng, H.;
He, W.; *Shi, Y.
A Proposed Role for Glutamine in Cancer Cell Growth through Acid Resistance.
Cell Research
2013,
23, 724-727.
19.Cai, S.; Duan, H.; Rong, H.; Wang, D.; Li, L.;
*He, W.; *Li, Y.
Highly Active and Selective Catalysis of Bimetallic Rh3Ni1 Nanoparticles in the Hydrogenation of Nitroarenes
ACS Catalysis,
2013,
3, 608-612.
20.Cai, S.; Rong, H.; Yu, X.; Liu, X.; Wang, D.;
*He, W.; *Li, Y.
Room Temperature Activation of Oxygen by Monodispersed Metal Nanoparticles: Oxidative Dehydrogenative Coupling of Anilines for Azobenzene Syntheses.
ACS Catalysis,
2013,
3, 478-486.
21.Wu, Y.; Cai, S.; Wang, D.; *
He, W.; *Li, Y.
Syntheses of Water-Soluble Octahedral, Truncated Octahedral and Cubic Pt?Ni Nanocrystals and Their Structure?Activity Study in Model Hydrogenation Reactions.
J. Am. Chem. Soc.
2012.
134, 8975-8981.
22. Niu, Z.; Peng, Q.; Zhuang, Z.;
*He, W.; *Li, Y.
Evidence of an Oxidative-Addition-Promoted Pd-Leaching Mechanism in the Suzuki Reaction by Using a Pd-Nanostructure Design.
Chem. Eur. J.
2012,
18, 9813-9817.