黃雲生[廣東醫科大學教授]

廣東醫科大學教授,美國北卡大學藥物化學專業博士(PhD)。

簡介

2010至今研究方向:合成利用生物信息設計全新藥物;新藥合成設計與篩選;藥物分子模型計算。主要研究領域:以磷酸甘油脂為載體的靶向抗腫瘤藥物研究、Sigma-2受體靶向抗腫瘤藥物研究、以Hsp90為靶向的抗病毒藥物研究、有機合成肽類、核苷類、甾體類等小分子;發表SCI論文40餘篇,獲發明專利3項。

學歷

美國北卡州立大學工商碩士(MBA)

美國北卡大學藥化專業博士(PhD)

北京大學有機化學碩士(MS)

江西大學(現南昌大學)化學學士(BS)

工作經歷

1、2010-現在 廣東醫科大學藥學院教授,主要研究領域包括:

以磷酸甘油脂為載體的靶向抗腫瘤藥物研究

Sigma-2受體靶向抗腫瘤藥物研究

以Hsp90為靶向的抗病毒藥物研究

諾美孕酮及其衍生物的研究

以偕二磷酸為親骨性的靶向抗骨質疏鬆藥物研究

2、2007-2009 蘇州強達化學醫藥有限公司(美國公司),副總經理,技術總監

管理一支由近40人組成的研發和中試團隊

生物活性分子設計與合成

醫藥中間體的合成

醫藥中間體生產工藝的改進

暨南大學生物醫藥基地的顧問特聘客座教授,指導863合成和衍生物的設計

3、2005-2007 美國Pharmagra公司高級研究員,項目主管

負責抗癌藥物分子設計與合成

負責雜環化合物合成研究

負責小分子靶向藥物合成開發研究

4、2002-2005 美國Kucera製藥公司高級研究員,團隊主管

抗愛滋病藥物合成

抗腫瘤藥物合成

5、1999-2002 美國Anasazi 生物醫藥研究公司合伙人和項目主要負責人

乳腺癌診斷劑sigma-1、2受體開發

抗乳腺癌藥物研究開發

公司的項目和有關專利03年被Mallinckrodt公司收購。

6、1997-1999美國Wake Forest大學醫學院副教授

癌症診斷劑sigma-1、2受體設計與合成

7、1995-1996美國Wake Forest大學醫學院博士後研究

Sigma-2受體與多巴胺D3受體合成、分子模型設計

8、1989-1990 汕頭駝濱化學藥業總公司藥物研究所,合成一室主任

負責子宮頸成熟藥物“優利生”的合成,該項目已獲得國家二類新藥。

負責“萊普生 ”抗生素的合成工藝的改造,最佳化。

9、1984-1986江西大學助教

有機化學的教學和實驗指導工作

特長

有機合成

肽類、核苷類、甾體類等小分子合成

利用生物信息設計全新藥物

新藥合成設計與篩選

藥物分子模型計算

發表論文

Yu-Tong Sun, Gui-Fei Wang, Yi-Qiu Yang, Fujun Jin, Yifei Wang, Xiao-Yang Xie, Robert H. Mach and Yun-Sheng Huang. European Journal of Medicinal Chemistry. 2017. Accepted

Song S.Y., Lu H.L., Wang G.F., Yang Y.Q., Huang Y.S., An Improved and Scale-up Synthesis of 6-Hydroxybenzofuran.Res. Chem. Intermed. 2016. 42(5). 4433-4442

Wu Z.W., Song S.Y., Li L., Lu H.L., Lieberman B., Huang Y.S., Mach R.H., Synthesis and Evaluation of Tetrahydroindazole Derivatives as Sigma-2 Receptor Ligands. Biorg. Med. Chem. 2015. 23(7). 1463-1471

Lu H.L., Wu Z.W., Song S.Y., Liao X.D, Zhu Y., Huang Y.S., An Improved Synthesis of Nomegestrol Acetate.Org. Process Res. Dev. 2014. 18(3). 431-436

Huang Y.S.,Lu H.L., Zhang L.J., Wu Z.W., Sigma-2 Receptor Ligands and Their Perspectives in Cancer Diagnosis and Therapy.Med. Res. Rev. 2014. 34(3). 532-566

Zhang L.J., Lu H.L., Wu Z.W., Huang Y.S., Ytterbium Triflate: A Versatile Catalyst in Organic Synthesis.Curr. Org. Chem. 2013. 17(23). 2906-2920

Huang Y.S., Liu J.Q., Zhang L.J., Lu H.L., Synthesis of 1-Indanones from Benzoic Acids.Ind. Eng. Chem. Res. 2011. 51(3). 1105-1109

Jia J., Gu Z.Y., Li R.C., Huang M.H., Xu C.S., Wang Y.F., Xing G.W., Huang Y.S., Design and Synthesis of Fluorescent Sensors for Zinc Ion Derived from 2-Aminobenzamide.Eur. J. Org. Chem. 2011. 2011(24). 4609-4615

Huang Y.S., Zhang W.Q., Zhang X., Wang J.Z., Manufacturing Synthesis of 5-Hydroxy-2-Methyl-1h-Indole.Res. Chem. Intermed. 2010. 36(8). 975-983

Huang Y.S., Zhang W.Q., Zhang P.F., Liu X.G., Industrial Production of Tert-Butyl-4-Oxoazepane-1-Carboxylate.Ind. Eng. Chem. Res. 2010. 49(23). 12164-12167

Liu J.Q., Wang Y.Y., Huang Y.S., Structural Variability of Co (Ii) and Ni (Ii) Entangled Metal–Organic Frameworks: Effect of N-Donor Ligands and Metal Ions.CrystEngComm. 2011. 13(11). 3733-3740

Liu J.Q., Huang Y.S., Zhao Y.Y., Jia Z.B., Molecular Tectonics of Entangled Metal? Organic Frameworks Based on Different Conformational Carboxylates Mixed with a Flexible N, N′-Type Ligand.Cryst Growth & Des. 2010. 11(2). 569-574

Mach R.H., Gage H.D., Buchheimer N., Huang Y .S.,Kuhner R., Wu L., Morton T.E., Ehrenkaufer R.L.[18F]4’-Fluorobenzyl-4-(2-fluorophenyl)acetamide ([18F]FBFPA): A Potential Fluorine-18 Labeled PET Radiotracer for Imaging Sigma-1 Receptors in the CNS.Synapse. 2005. 58(4). 267-274

Mach R.H., Huang Y .S., Freeman R.A., Wu L., Vangveravong S., Luedtke R.R. Conformationally-flexible benzamide analogs as dopamine D3 and Sigma-2 receptor ligands.Bioorg. Med. Chem. Lett. 2004. 14(1). 195-202

Mach R.H., Huang Y .S.,Freeman R.A., Wu L.,Blair S., Luedtke R.R.,Synthesis of2-(5-bromo-2,3-dimethoxyphenyl)-5-(aminomethyl)-1H-pyrrole analogues and their binding affinities for dopamine D2, D3, and D4 receptors.Biorg. Med. Chem. 2003. 11(2). 225-233

Mach R.H., Vangveravong S., Huang Y .S.,Yang B., Blair J.B., Wu L. Synthesis of N-substituted 9-azabicyclo[3.3.1]nonan-3a-yl phenylcarbamate analogs as Sigma-2 receptor ligands.Med. Chem. Res. 2002. 11(7). 380-398

Huang Y.S., Hammond P.S., Wu L., Mach R.H.,Synthesis and structure-activity relationships of N- (1-benzylpiperidin-4-yl)aryllacetamide analogues as potent Sigma-1 receptor ligands.J. Med. Chem. 2001. 44(25). 4404-4415

Huang Y.S., Luedtke R.R., Freeman R.A., Wu L., Mach R.H.,Synthesis and Structure-ActivityRelationship of naphtnamides as dopamine D3 receptor ligands.J. Med. Chem. 2001. 44(11). 1815-1826

Huang Y.S., Luedtke R.R., Freeman R.A., Wu L., Mach R.H.,Synthesis of 2-(2,3-dimethoxyphenyl)-4-(aminomethyl)imidazole analogues and their binding affinities for dopamine D2 and D3 receptors.Biorg. Med. Chem. 2001. 9(12). 3113-3122

Mach R.H., Huang Y.S., Buchheimer N., Kuhner R., Wu L., Morton T.E., Wang, L.M., Ehrenkaufer R.L.,Wallen C.A., Wheeler K.T., [18F]N-4’-fluorobenzyl-4-(3-bromophenyl) acetamide for imaging the sigma receptor status of tumors: comparison with [18F]FDG and [125I]IUDR.Nucl. Med. Biol. 2001. 28(4). 451-458

Luedtke R.R., Freeman R.A., Boundy V.A., Martin M.W., Huang Y.S., Mach R.H., Characterization ofI-IABN, a novel azabicyclononane benzamide selective for D2-like dopamine receptors.Synapse. 2000. 38(4). 438-449

Mach R.H., Hammond P.S., Huang Y .S., Yang B., Xu Y., Cheney J.T., Freeman R. and Luedtke R.R. Structure-activity relationship studies of N-(9-benzyl)-9-azabicyclo[3.3.1]nonan-3ß-yl benzamide analogues for dopamine D2 and D3 receptors.Med. Chem. Res. 1999. 9(6). 355-373

Huang Y.S., Hammond P.S., Whirrett B.R., Ross J.K., Wu L., Childers S.R., and Mach R.H., Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective Sigma-1 ligands.J. Med. Chem. 1998. 41(13). 2361-2370

Huang Y.S.,Hall I.H., Antineoplastic and cytotoxic activity of beta-alkylamino-(para-substituted)propiophenone and beta-alkylamino-(6-methyl) naphthone derivatives in murine and human tissue culture cells.Pharmazie. 1998. 53(2). 117-123

Huang Y.S.,andHall I.H., Hypolipidemic effects of alpha, beta, and gama-alkylaminophenone analogues in rodents.Eur. J. Med. Chem. 1996. 31(4). 281-290

Huang Y.S.,andHall I.H., Synthesis and pharmacological studies of 3-amino-2-methyl-1-phenyl- propiophenones as hypolipidemic agents in rodents.Arch. Pharm. Pharm.Med. Chem.1996. 329(7). 329-338

Huang Y.S.,andHall I.H., Hypolipidemic activity of 3-amino-1-(2,3,4-mononitro-,mono-, or dihalo- phenyl)propan-1-ones in rodents.Arch. Pharm. Pharm. Med. Chem.1996. 329(7). 339-346

Huang Y.S.,andHall I.H.,Synthesis and hypolipidemic evaluation of beta-alkylaminopropiophenone and beta-alkylaminopropio-2’-naphthone derivatives in rodents.Pharmazie. 1996. 51(4). 199-206

Huang Y.S.,andHall I.H.,Anti-inflammatory activity of alpha-, beta-, and gama-alkylaminoketones in CFmice.Res. Comm. Pharm. & Toxi.1996 . 1. 17-37
Huang Y.S.,andHall I.H.,Antineoplastic activities of alpha-, beta-, and gama-alkylaminopropiophenone derivatives in mice and in murine and human tissue culture cells.Anticancer Res. 1996. 16(2). 597-604

Huang Y.S.,andHall I.H.,Antineoplastic activities of 2,3,4-chlorosubstituted beta-alkylamino-propiophenone derivatives in CFmice and in murine and human tumor cells.Anticancer Drugs. 1996. 7(5). 613-620

Butner L., Huang Y.S., Tse E., and Hall I.H., Anti-inflammatory activity of 2,3-dihydrophthalazine-1,4-diones in CFmice.Int. J. Tissue React.-Exp. Clin. Asp. 1996. 18(2-3). 47-55

Butner L., Huang Y.S., Tse E., and Hall I.H.,Anti-inflammatory and analgesic activities of 3-imino-1- oxoisoindolines in CFmice.Biomed. Pharmacother. 1996. 50(6–7). 290-296

Tse E., Butner L., Huang Y.S., and Hall I.H.,The anti-inflammatory activity of N-substituted indazolones in mice.Arch. Pharm. Pharm. Med. Chem.1996. 329(1). 35-40

Huang Y.S.,andHall I.H.,Antineoplastic activities of alpha-methyl-beta-alkylaminopropiophenonederivatives in tissue culture cells.Anticancer Res. 1996. 16(6b). 3589-3595

Ye Y., Huang Y.S., Wang Z., Chen S., and Tian Y., Synthesis of new amino acid and peptide derivatives of estradiol and their binding affinities for the estrogen receptor.Steroids1993. 58 (1), 35-39

He M., Ye Y., He X.,Huang Y.S., Lin X., and Yu Z., Mass spectrometric study of novel estrone derivatives of amino acids and peptides.Org. Mass Spectr.1992, 27, 636-638
Chen S.,Huang Y.S.,and Ye Y.,13C-NMR study of amino acid, peptide derivatives of estrogenic steroids.Chinese J. Magnetic Resonance.1991, 8 (2), 153-158
Huang Y.S.,and Ye Y., Synthesis of new estrone derivatives of amino acids and peptides.Chinese Chem. Lett.1991. 2 (2). 99-101

Ye Y. and Huang Y.S.,Amino acid, peptide steroidal derivatives: A review.Chinese J. Med. Chem.1991. 1. 41-48

申請專利

Robert Mach, Yunsheng Huang, Steven Childers, and Kenneth Wheeler, Sigma-1 Ligands for Determining Carcinoma Proliferative Status. WO 2000/71171 A3

Ronald A. Fleming, Jan V. Hes, Yunsheng Huang, Russ Read, Susan Morris-Natschke, Khalid Ishaq, Louis S. Kucera, Phillip A. Furman, Phospholipids for the Treatment of Infection by Togaviruses, Herpes Viruses, and Coronaviruses. US20050187192

Louis S. Kucera, Ronald A. Fleming, Jan V. Hes, Yunsheng Huang, Russ H. Read, Phillip A. Furman, Susan L. Morris-Natschke, Khalid S. Ishaq, Methods and Compositions for the Treatment of Respiratory Syncytial Virus. WO 2005/099719 A2

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