Medical Design

GUO LI

Permanent resident of United States

Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907

Cell: 804-***-****,, Lab: 765-***-****, E-mail: *****@******.***

CAREER OBJECTION

Looking for a permanent position of organic chemist or medicinal chemist

SKILLS SUMMARY (HIGHLIGHTS OF QULIFICATIONS)

Organic Chemistry: design of efficient synthetic routes, mutlistep synthesis, purification and characterization

bioactive compounds(IR, UV, NMR, MS, Element Analysis), solid phase synthesis, drug conjugation, LC-MS

analysis, HPLC purification;

Medicinal Chemistry: lead compound identification and optimization, structure-activity relationships study,

homology modeling, docking study, structure-based drug design, design novel linkers;

Biology: cell culture, confocol microscopy, cytotoxicity assay, ligand binding assay, animal handling,

fluorescence and radio imaging, flowcytometry.

RESEARCH EXPERIENCE

Purdue University, IN

Postdoctoral research associate, Nov. 2009-Present

• Designed and synthesized of small molecular-targeted drug conjugates for both imaging and therapeutic

applications on a variety of human cancers, such as:

1. Targeting Mu Opioid Receptor for Lung Cancer;

2. Targeting somatostatin receptor 2(SST2) for most neuroendocrine tumors, and endocrine tumor s

(pancreatic cancer, and breast, colon cancer);

3. Targeting Endothelin receptor A (ETA) for ovarian, colorectal, lung, breast, bladder, and pancreatic cancer;

4. Targeting Chemokine receptor 2(CCR2) for prostate, breast, and small cell lung cancer.

• Methodology development for targeted drug delivery, such as developing different linkers for delivery and

using photo labeling method to explore the possible derivatization position of small molecular for drug

targeting;

Virginia Commonwealth University, VA

Postdoctoral fellow, 2005-2009

• Designed and synthesized of bivalent compounds of Chemokine receptor receptor 5 (CCR5) and Mu opioid

receptor (MOR) to explore the biological and pharmacological process of the putative MOR–CCR5

dimerization phenomenon. The overall reaction route to prepare the MOR–CCR5 bivalent ligand was

convergent and efficient, and involved sixteen steps with good yields.

• Structure-based design and synthesis of non-peptide selective Mu opioid receptor antagonists as

pharmacological probes and potential agents for drug addition treatment based on Molecular modeling and

docking studies of Opioid receptors;

• Natural product, Anibamine’s total synthesis and further structure modification for anti-HIV and anti -

prostate cancer applications. The anibamine and its (11E, 22E) isomer were synthesized from acetylacetone

and cyanoacetamide in 10 steps with 7.9 % overall yield;

• Designed and synthesized a series of selective ant agonists for chemokine receptor 5 as potential anti-HIV

and anti prostate cancer agents based on CCR5 receptor modeling;

• Accomplished the Molecular modeling and docking studies of Lysophospholipid 4 receptor (LPA4) using

SYBYL and GOLD programs, and further designed, synthesized novel LPA analogs for LPA4 receptor;

•Stereo selectively synthesized two major metabolites of Spironolactone for the Spironolactone’s metabolic

mechanism investigation

Beijing Pharmaron Medicinal Technology Ltd. China

Group Leader, Aug.2004–Dec. 2004

Custom Synthesis of fourteen requested compounds in multi-steps and kilogram scale involving effectively

synthetic route modifications and reaction yield optimizations

Institute of Materia Medica of Hebei Province, China

Research Associate, July 1997-July1999

Optimized the synthesis route for Gabapentin, a new drug for treatment of epilepsy

Prepared about 300 gram Gabapentin for preclinical study through the ion-exchange resin purification

EDUCATION

Chinese Academy of Medical Sciences & Peking Union Medical Colleg e, China

Graduate research with Professor Xiao -Tian Liang, Ph.D. in Medicinal Chemistry, Sept. 1999-July 2004

Thesis: “Design and synthesis of the Phthalide’s and Phthalan’s Derivatives as GABAa Receptor Modulator s.”

LanZhou University, China

B.S. in organic chemistry, Sept. 1993-June 1997

PUBLICATIONS

Peer-reviewed Articles:

1. Guo Li; Da-li Yin. New synthetic method for preparation of 3 -substituted phthalides. Jingxi Yu Zhuanyong

Huaxuepin, 2004, 12(12), 19-21;

2. Guo Li; Da-li Yin; Xiao-Tian Liang, A facile synthesis of 3-substituted phthalides. Synthetic Communications,

2004, 34(7), 1183–1189;

3. Guo Li; Yan Zhang. Stereoselective synthesis of the two major metabolites of spironolactone, 3alpha - and

3beta-hydroxy-7alpha-methylthio-17alpha–pregn- 4-ene-21,17- arbolactone. Steroids. 2007, 72(6-7),

569-72;

4. Guo Li; Karen Watson, Robert W. Buckheit; Yan Zhang. Total synthesis of anibamine, a novel natural

product as a chemokine receptor CCR5 antagonist. Org. Lett. 2007, 9(10), 2043-6;

5. Guo Li, Lindsey C. Aschenbach, Michael P. Cassidy, David L. Stevens, Bichoy Gabra, Dana E. Selley, William L.

Dewey, Richard B. Westkaemper, Yan Zhang. Design, Synthesis and biological evaluation of pyridinyl and

isoquinolinyl formamidyl 6α AND 6β naltrexamine derivatives as mu opioid receptor selective antagonists.

J. Med. Chem. 2009, 52(5), 1416-1427;

6. Guo Li, Lindsey C. Aschenbach, Dana E. Selley, Yan Zhang. 14-O-Heterocyclic-Substituted Naltrexone

Derivatives as Non-Peptide Mu Opioid Receptor Selective Antagonists: Design, Synthesis and Biological

Studies. Bioorg. Med. Chem. Lett. 2009, 19, 1825-29;

7. Guo Li, Kendra M. Haney, Glen E. Kellogg, Yan Zhang. A Comparative Docking Study of Anibamine as the

First Natural Product CCR5 Antagonist in CCR5 Homology Models. J. Chem. Inf. Model. 2009, 49(1), 120-132;

8. Guo Li, Philip D. Mosier, Xianjun Fang; Yan Zhang. Toward the Three-dimensional Structure and

Lysophosphatidic Acid Binding Characteristics of the LPA4/GPR23 Recep tor: A Homology Modeling Study. J.

Mol. Graph. Model. 2009, 28, 70-9;

9. Kendra M. Haney, Feng Zhang, Christopher K. Arnatt, Yunyun Yuan, Guo Li, Joy L. Ware, David A. Gewirtz,

Yan Zhang. The natural product CCR5 antagonist anibamine and its analogs as anti -prostate cancer agents.

Bioorg. Med. Chem. Lett. 2011, 21(18),5159-63;

10. Yunyun Yuan, Guo Li, Hengjun He, David L. Stevens, Patrick Kozak, Krista L. Scoggins, Pallabi Mitra, Phillip

M. Gerk, Dana E. Selley, William L. Dewey, and Yan Zhang. Characterization of 6α -and 6β-N-Heterocyclic

Substituted Naltrexamine Derivatives as Novel Leads to Development of Mu Opioid Receptor Selective

Antagonists. ACS Chem. Neurosci., 2011, 2 (7), 346–351;

11. Yunyun Yuan, Christopher K. Arnatt, Guo Li, Kendra M. Haney, Derong Ding, Joanna C. Jacob,Dana E.

Selley and Yan Zhang. Design and synthesis of a bivalent ligand to explore the putative heterodimerization

of the mu opioid receptor and the chemokine receptor CCR5. Org. Biomol. Chem. 2012, 10(13): 2633-46;

12. Yunyun Yuan, Saheem A. Zaidi, Orgil Elbegdorj, Lindsey C. K. Aschenbach, Guo Li, David L. Stevens, Krista L.

Scoggins, William L. Dewey, Dana E. Selley, and Yan Zhang. Design, Synthesis, and Biological Evaluation of

14-Heteroaromatic-Substituted Naltrexone Derivatives: Pharmacological Profile Switch from Mu Opioi d

Receptor Selectivity to Mu/Kappa Opioid Receptor Dual Selectivity. J. Med. Chem. 2013, 56, 9156 9169;

13. Christopher K. Arnatt, Saheem A. Zaidi, Zhu Zhang, Guo Li, Amanda C. Richardson, Joy L. Ware, Yan Zhang.

Design, syntheses, and characterization of pharmacophore based chemokine receptor CCR5 antagonists as

anti prostate cancer agents. European J. Med. Chem. 2013, 69, 647-658;

14. Ajay Kumar, Venkatesh Chelvam, Mahalingam Sakkarapalayam, Guo Li, Pedro Sanchez-Cruz, Natasha S.

Piñero, Antonio E. Alegria, Philip S. Low, Synthesis and Evaluation of Folate-conjugated

Phenanthraquinones for Tumor-Targeted Chemotherapy. International Journal of Pharmaceutics. 2014

(manuscripts under review);

15. Guo Li, Chris Galliford, Philip S. Low, Using Endothelin receptor antagonist as targeting ligand in cancer

imaging application. 2014 (manuscripts in preparation);

16. Guo Li, Candice B. Kissinger, Philip S. Low, Evaluation of a small molecular targeting ligand for the

somatostatin receptor 2. (manuscripts in preparation).

HONORS AND AWARDS, & FELLOWSHIPS

1. First Rank Scholarship for Undergraduates, 1994-1995, Department of Chemistry, LanZhou University;

2. First Rank Scholarship for Undergraduates, 1995-1996, Department of Chemistry, LanZhou University;

3. Outstanding Undergraduate Award, 1997, Department of Chemistry, LanZhou University.

NAMES OF REFERENCES

1. Philip S. Low, Ph. D.,

Ralph C. Corley Distinguished Professor of Chemistry and Director of the Purdue Center for Drug Discovery,

Department of Chemistry, Purdue University;

720 Clinic Drive, Center for Drug Discovery, Office: 323, Purdue University, West Lafayette, IN 47907;

Email: ****@******.***; Phone: 765-***-****(office) or 765-***-****;

2. Yan Zhang, Ph. D.,

Associate Professor of Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth

University;

800 East Leigh Street, Suite 205, Room 251e, Biotech I, VA Research Park, Richmond, VA 23298,

Phone: 804-***-****, Email: *******@***.***;

3. Dali Yin, Ph. D.,

Professor of medicinal chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences &

Peking Union Medical College;

No.1 Xian Nong Tan Street, Beijing, 100050, P.R. China;

Tel: 86-10-631***** or 86-10-612*-****; Email: *******@***.**.**.

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