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王玉强老师介绍
王玉强现任暨南大学药学院教授，院长。专业为药物化学，从事抗肿瘤及抗病毒药物、心、脑血管系统疾病药物、 治疗老年性痴呆和糖尿病药物的设计、化学合成、作用机理研究和活性评价。
王玉强教授已从事抗肿瘤药物的设计与化学合成二十多年，他的实验室已经合成了100多个CC－1065衍生物。CC-1065类化合物高度选择性的结合到B型DNA双螺旋链小沟区 (minor groove) 的AT碱基区并和腺嘌呤的N-3发生化学反应，引起DNA链断裂，从而导致癌细胞死亡。他的实验室合成的抗癌药物YW-053是目前已知抗癌活性最强的少数化合物之一(IC50: 10-16 M in KB cells)，其体外抗癌活性比阿霉素强一百万倍。
王玉强教授及其团队在美国成功开发抗老年痴呆药物memantine，并首次在世界上设计合成了可以释放一氧化氮的memantine衍生物。Memantine高度靶向性的结合到大脑神经细胞的NMDA受体并在大脑神经细胞内释放一氧化氮。这类化合物既是NMDA受体的拮抗剂，又能通过一氧化氮的释放而抑制自由基的产生以达到保护神经细胞的目的，因而具有双重作用。
王玉强的实验室近年在中药如穿心莲、川芎及丹参有效成份化学结构修饰方面卓有成效，已合成和发现了比天然产物疗效更高，毒性更低的新化合物。
王玉强教授1981年毕业于山东师范大学化学系，1987年于 The University of Texas Health Science Center at Houston and The University of Texas M . D. Anderson Cancer Center 获得博士学位。博士毕业后，进入美国耶鲁大学医学院药理系做博士后，师从世界著名抗肿瘤药物研究专家Alan C. Sartorelli教授。随后，他师从加拿大 The University of Alberta 的J. William Lown 教授从事抗肿瘤药物CC-1065衍生物的研究。J. William Lown教授因研究抗肿瘤药物阿霉素衍生物和DNA minor groove-binding药物而著名世界。1993年进入美国硅谷的生物技术公司Panorama Research, Inc. 从事药物的研究与开发工作，2005年加入暨南大学药学院。
代表性论文
1.Wang, Y.; Farquhar, D. Aldophosphamide acetal diacetate and structural analogues: synthesis and cytotoxicity studies. J. Med. Chem. 34, 197, 1991.
2.Wang, Y.; Liu, M. C.; Lin, T. S.; Sartorelli, A. C. Synthesis and biological evaluation of novel antitumor 3- and 5-hydroxy-4-methyl-2-formylpyridine thiosemicarbazones and their iron-chelates. J. Med. Chem. 35, 3667, 1992.
3.Wang, Y.; Gupta, R.; Huang, L.; Lown, J. W. Synthesis and antitumor activity of CC-1065 functional analogues possessing different electron-withdrawing substituents and leaving groups. J. Med. Chem. 36, 4172, 1993.
4.Fregeau, N. L.; Wang, Y.; Pon, R, T.; Wylie, W. A.; Lown, J. W. Characterization of a CPI-Lexitropsin Conjugate: Oligonucleotide covalent complex by 1H NMR and restrained molecular dynamics simulation. J. Amer. Chem. Soc. 117, 8917, 1995.
5.Wang, Y.; Gupta, R.; Huang, L.; Luo, W.; Lown, J. W. Design, synthesis, cytotoxic properties and preliminary DNA sequencing evaluation of CPI-N-methylpyrrole hybrids. Enhancing effect of a trans double bond linker and role of the terminal amide functionality on cytotoxic potency. Anti-Cancer Drug Design 11, 15, 1996.
6.Wang, Y.; Yuan, H.; Ye, W.; Wang, H.; Wright, S. C.; Larrick, J. W. Synthesis and preliminary biological evaluations of CC-1065 analogs: effects of different linkers and terminal amides on biological activity. J. Med. Chem. 43, 1541. 2000.
7.Wang, Y.; Wright, S. C.; Larrick, J. W. Synthesis and cytotoxicity of nitrogen mustard derivatives of distamycin A. Bioorg. Med. Chem. Lett. 13, 461, 2003.
8.Wang, Y.; Ye, W.; Li, L.; Tian, Z.; Jiang, W.; Wang, H.; Wright, S. C.; Larrick, J. W. CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity and preliminary toxicity study. J. Med. Chem. 46, 634, 2003.
9.Wang, Y.; Yuan, H.; Wang, H.; Wright, S. C.; Larrick, J. W. Synthesis and preliminary cytotoxicity study of glucuronide derivatives of CC-1065 analogues. Bioorg. Med. Chem. 11, 1569, 2003.
10.Wang, Y.; Li, L.; Jiang, W.; Larrick, J. W. Synthesis and evaluation of a DHA and 10-hydroxcamptothecin conjugate. Bioorg. Med. Chem. 13, 5592–5599, 2005.
11.Wang, Y.; Li, L.; Jiang, W.; Yang, Z.; Zhang, Z. Synthesis and preliminary antitumor activity evaluation of a DHA and doxorubicin conjugate. Bioorg. Med. Chem. Lett. 16， 2974-2977，2006.
12.Wang, Y.; Li, L.; Tian, Z.; Jiang, W.; Larrick, J. W. Synthesis and antitumor activity of CBI-bearing ester and carbamate prodrugs of CC-1065 analogue. Bioorg. Med. Chem. 14, 7854-7861, 2006.
13.Wang, Y.; Eu, J.; Washburn, M.; Gong, T.; Chen, H. S. V.; Larrick, J. W.; Lipton, S. A.; Stamler, J, S.; Went, G. T.; Porter, S. The Pharmacology of Aminoadamantane nitrates. Curr. Alzheimer Res. 3, 201-204, 2006.
14.Suo, X. B.; Zhang, H.; Wang, Y. HPLC determination of andrographolide in rat whole blood: study on the pharmacokinetics of andrographolide incorporated in liposomes and tablets.
Biomed Chromatogr. 21, 730-734, 2007.
15.suo, X. B.; Deng, Y. J.; Zhang, H.; Wang, Y. Degradation kinetics of water-insoluble lauroyl-indapamide in aqueous solutions: prediction of the stabilities of the drug in liposomes. Arch Pharm Res. 30, 876-883, 2007.
已授权专利
1.Farquhar, D., Wang, Y. Aldophosphamides for treatment of leukemia, US 4,841,085, June 1989.
2.Farquhar, D., Wang, Y. Novel antitumor aldophosphamide analogues, US 5,091,552, February 1992, PCT/US89/01214, Japanese Patent Application No. 505053/90, AU652119 (Austrialia), EP89904975 (European), CA2050664 (Canada).
3.Farquhar, D., Wang, Y. Novel antitumor aldophosphamide glycoside and dideoxyuridine derivatives, US 5,187,266, February 1993.
4.Lown, J. W., Wang, Y., Wei, L. Cyclopropylpyrroloindole-Oligopeptide Anticancer Agents, US 5,502,068, March 1996, AU698001 (Australia), CA2210093 (Canada), EP0800390 (European), WO9623497.
5.Wang, Y. Wright, S. C., Larrick, J. W. DNA-binding indole derivatives, their prodrugs and immunoconjugates, US 5,843,937, December 1998, 中国专利 ZL97194862.3 (2004), EP0918752 (European), WO9744000.
6.Wang, Y.,Ye, W., Larrick, J. W, Stamler, J. S., Lipton, S. A. Aminoadamantane derivatives as therapeutic agents, US 6,444,702, September 2002. CT/US/01/05967, EP01916217, Chinese Patent Application 01806892.8, Mexican Patent Application PA/a/2002/008170. Canadian Patent Application No. 2,400,916.
7.Wang, Y.,Ye, W., Larrick, J. W, Stamler, J. S., Lipton, S. A. Aminoadamantane derivatives as therapeutic agents, US 6,620,845, September 2003.
8.wang, Y., Larrick, J. W. Antioxidant nitroxides and nitrones as therapeutic agents. US 6,717,012, April 2004, PCT/US02/10361, 2002, pending, EP02757941.5, 2003, pending.
9.Wang, Y. Novel anticancer conjugates of camptothecin and unsaturated fatty acids. US 6,759416, 2004, PCT/US03/23983, July 31, 2003.
10.Wang, Y., Larrick, J. W. Antioxidant nitroxides and nitrones as therapeutic agents. US 6,852,889, February, 2005.
王玉强教授已从事抗肿瘤药物的设计与化学合成二十多年，他的实验室已经合成了100多个CC－1065衍生物。CC-1065类化合物高度选择性的结合到B型DNA双螺旋链小沟区 (minor groove) 的AT碱基区并和腺嘌呤的N-3发生化学反应，引起DNA链断裂，从而导致癌细胞死亡。他的实验室合成的抗癌药物YW-053是目前已知抗癌活性最强的少数化合物之一(IC50: 10-16 M in KB cells)，其体外抗癌活性比阿霉素强一百万倍。
王玉强教授及其团队在美国成功开发抗老年痴呆药物memantine，并首次在世界上设计合成了可以释放一氧化氮的memantine衍生物。Memantine高度靶向性的结合到大脑神经细胞的NMDA受体并在大脑神经细胞内释放一氧化氮。这类化合物既是NMDA受体的拮抗剂，又能通过一氧化氮的释放而抑制自由基的产生以达到保护神经细胞的目的，因而具有双重作用。
王玉强的实验室近年在中药如穿心莲、川芎及丹参有效成份化学结构修饰方面卓有成效，已合成和发现了比天然产物疗效更高，毒性更低的新化合物。
王玉强教授1981年毕业于山东师范大学化学系，1987年于 The University of Texas Health Science Center at Houston and The University of Texas M . D. Anderson Cancer Center 获得博士学位。博士毕业后，进入美国耶鲁大学医学院药理系做博士后，师从世界著名抗肿瘤药物研究专家Alan C. Sartorelli教授。随后，他师从加拿大 The University of Alberta 的J. William Lown 教授从事抗肿瘤药物CC-1065衍生物的研究。J. William Lown教授因研究抗肿瘤药物阿霉素衍生物和DNA minor groove-binding药物而著名世界。1993年进入美国硅谷的生物技术公司Panorama Research, Inc. 从事药物的研究与开发工作，2005年加入暨南大学药学院。
代表性论文
1.Wang, Y.; Farquhar, D. Aldophosphamide acetal diacetate and structural analogues: synthesis and cytotoxicity studies. J. Med. Chem. 34, 197, 1991.
2.Wang, Y.; Liu, M. C.; Lin, T. S.; Sartorelli, A. C. Synthesis and biological evaluation of novel antitumor 3- and 5-hydroxy-4-methyl-2-formylpyridine thiosemicarbazones and their iron-chelates. J. Med. Chem. 35, 3667, 1992.
3.Wang, Y.; Gupta, R.; Huang, L.; Lown, J. W. Synthesis and antitumor activity of CC-1065 functional analogues possessing different electron-withdrawing substituents and leaving groups. J. Med. Chem. 36, 4172, 1993.
4.Fregeau, N. L.; Wang, Y.; Pon, R, T.; Wylie, W. A.; Lown, J. W. Characterization of a CPI-Lexitropsin Conjugate: Oligonucleotide covalent complex by 1H NMR and restrained molecular dynamics simulation. J. Amer. Chem. Soc. 117, 8917, 1995.
5.Wang, Y.; Gupta, R.; Huang, L.; Luo, W.; Lown, J. W. Design, synthesis, cytotoxic properties and preliminary DNA sequencing evaluation of CPI-N-methylpyrrole hybrids. Enhancing effect of a trans double bond linker and role of the terminal amide functionality on cytotoxic potency. Anti-Cancer Drug Design 11, 15, 1996.
6.Wang, Y.; Yuan, H.; Ye, W.; Wang, H.; Wright, S. C.; Larrick, J. W. Synthesis and preliminary biological evaluations of CC-1065 analogs: effects of different linkers and terminal amides on biological activity. J. Med. Chem. 43, 1541. 2000.
7.Wang, Y.; Wright, S. C.; Larrick, J. W. Synthesis and cytotoxicity of nitrogen mustard derivatives of distamycin A. Bioorg. Med. Chem. Lett. 13, 461, 2003.
8.Wang, Y.; Ye, W.; Li, L.; Tian, Z.; Jiang, W.; Wang, H.; Wright, S. C.; Larrick, J. W. CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity and preliminary toxicity study. J. Med. Chem. 46, 634, 2003.
9.Wang, Y.; Yuan, H.; Wang, H.; Wright, S. C.; Larrick, J. W. Synthesis and preliminary cytotoxicity study of glucuronide derivatives of CC-1065 analogues. Bioorg. Med. Chem. 11, 1569, 2003.
10.Wang, Y.; Li, L.; Jiang, W.; Larrick, J. W. Synthesis and evaluation of a DHA and 10-hydroxcamptothecin conjugate. Bioorg. Med. Chem. 13, 5592–5599, 2005.
11.Wang, Y.; Li, L.; Jiang, W.; Yang, Z.; Zhang, Z. Synthesis and preliminary antitumor activity evaluation of a DHA and doxorubicin conjugate. Bioorg. Med. Chem. Lett. 16， 2974-2977，2006.
12.Wang, Y.; Li, L.; Tian, Z.; Jiang, W.; Larrick, J. W. Synthesis and antitumor activity of CBI-bearing ester and carbamate prodrugs of CC-1065 analogue. Bioorg. Med. Chem. 14, 7854-7861, 2006.
13.Wang, Y.; Eu, J.; Washburn, M.; Gong, T.; Chen, H. S. V.; Larrick, J. W.; Lipton, S. A.; Stamler, J, S.; Went, G. T.; Porter, S. The Pharmacology of Aminoadamantane nitrates. Curr. Alzheimer Res. 3, 201-204, 2006.
14.Suo, X. B.; Zhang, H.; Wang, Y. HPLC determination of andrographolide in rat whole blood: study on the pharmacokinetics of andrographolide incorporated in liposomes and tablets.
Biomed Chromatogr. 21, 730-734, 2007.
15.suo, X. B.; Deng, Y. J.; Zhang, H.; Wang, Y. Degradation kinetics of water-insoluble lauroyl-indapamide in aqueous solutions: prediction of the stabilities of the drug in liposomes. Arch Pharm Res. 30, 876-883, 2007.
已授权专利
1.Farquhar, D., Wang, Y. Aldophosphamides for treatment of leukemia, US 4,841,085, June 1989.
2.Farquhar, D., Wang, Y. Novel antitumor aldophosphamide analogues, US 5,091,552, February 1992, PCT/US89/01214, Japanese Patent Application No. 505053/90, AU652119 (Austrialia), EP89904975 (European), CA2050664 (Canada).
3.Farquhar, D., Wang, Y. Novel antitumor aldophosphamide glycoside and dideoxyuridine derivatives, US 5,187,266, February 1993.
4.Lown, J. W., Wang, Y., Wei, L. Cyclopropylpyrroloindole-Oligopeptide Anticancer Agents, US 5,502,068, March 1996, AU698001 (Australia), CA2210093 (Canada), EP0800390 (European), WO9623497.
5.Wang, Y. Wright, S. C., Larrick, J. W. DNA-binding indole derivatives, their prodrugs and immunoconjugates, US 5,843,937, December 1998, 中国专利 ZL97194862.3 (2004), EP0918752 (European), WO9744000.
6.Wang, Y.,Ye, W., Larrick, J. W, Stamler, J. S., Lipton, S. A. Aminoadamantane derivatives as therapeutic agents, US 6,444,702, September 2002. CT/US/01/05967, EP01916217, Chinese Patent Application 01806892.8, Mexican Patent Application PA/a/2002/008170. Canadian Patent Application No. 2,400,916.
7.Wang, Y.,Ye, W., Larrick, J. W, Stamler, J. S., Lipton, S. A. Aminoadamantane derivatives as therapeutic agents, US 6,620,845, September 2003.
8.wang, Y., Larrick, J. W. Antioxidant nitroxides and nitrones as therapeutic agents. US 6,717,012, April 2004, PCT/US02/10361, 2002, pending, EP02757941.5, 2003, pending.
9.Wang, Y. Novel anticancer conjugates of camptothecin and unsaturated fatty acids. US 6,759416, 2004, PCT/US03/23983, July 31, 2003.
10.Wang, Y., Larrick, J. W. Antioxidant nitroxides and nitrones as therapeutic agents. US 6,852,889, February, 2005.
王玉强老师相关教学资源
