Hurley Research Group Home Page

Hariprasad Vankayalapati, Ph.D.
Research Associate
College of Pharmacy
Pharmacology and Toxicology
hari@pharmacy.arizona.edu
Arizona Cancer Center Room 4956
1515 North Campbell Avenue
Tucson, Arizona 85724
Telephone: (520) 626-7818, or 0106
Fax: (520) 626-5623

Current Research :

Application Computational Chemistry methods including; Structure-Based, de novo, based design, Docking, Virtual Screening, Molecular Dynamics, Homology Modeling, Pharmacophore Maping, QSAR, 3D- QSAR, Semiempirical and 2D, 3D-Database Searching on;

Serine/Threonine (Aurora2 Kinase ) and Tyrosine Kinases
Topoisomerase-II
G-Quadruplexes

Synthesis of small Molecule Heterocyclics as Kinase Inhibitors, Topoisomerase-II and G-quadruplex interactive agents.

Research Experiences

Nov.2000 -present
Associate Research Scientist, Medicinal Chemistry, Arizona Cancer Center, University of Arizona Health Sciences Center, Tucson, Arizona.
Design and Development of New Anticancer Agents.

1998 - 2000

Postdoctoral Fellow, Organic Chemistry, School of Health Sciences, University of Sunderland, England (UK).
New Glycosylation Methods based on Glycosyl Phosphates as Glycosyl Donors.
Regio/Stereoselective Methods for -O, C- and N- Glycosides, Glycopeptides and Gycomimetics.
Stereoselective one-pot Glycosylation Methods and the assembly of Oligosaccharides.
Synthesized New Selectine-E Inhibitors as Anti-inflammatory Agents.

1997 - 1998

Research Scientist, New Drug Discovery Research (NDDR), Medicinal Chemistry Group, Ranbaxy Research Laboratories., New Delhi, India.
Synthesis of New Chemical Entities as Potential Anti-fungal Agents.
Synthesis of Fluconazole Potentiators.

1991 - 1993

Lecturer, Pharmaceutical Chemistry, J.S.S College of Pharmacy, University of Mysore, India.
Medicinal Chemistry I & II. Education:

Ph.D., 1996, Medicinal Chemistry, UDCT, University of Bombay, India.
Design and Synthesis of new potential anti-inflammatory and anti-HIV compounds.

M.Pharm., 1991, Pharmaceutical Chemistry, K.L.E's College of Pharmacy, Belgaum, Karnatak University, India.
Synthesis and Evaluation of Substituted Fluorine-Heterocycle Derivatives as Anti- inflammatory and Chemotherapeutic Agents.

B.Pharm., 1988, Pharmaceutical Sciences, H.K.E's College of Pharmacy, Gulbarga University Gulbarga, India.

Publications:

1.Kim, M.-Y, Hariprasad, V, Shin-ya, K, Wierzba, K and Hurley, L.H. Telomestatin, a Potent Telomerase Inhibitor That Interacts Quite Specifically with the Human Telomeric Interamoleular G- Quadruplex. J.Am.Chem.Soc. 2002, 124(10), 2098-2099.

2.Hariprasad, V, Shende Jiang and Gurdial Singh. Glycosylation Based on Glycosyl Phosphates as Glycosyl Donors. Syn Lett. 2002, 1, 16-25.

3.Duan, W, Rangan, A, Hariprasad, V, F, Mu-Yong, K, Zeng, Q, Sun, D, Han, H, Fedoroff, O.Yu, Nishioka, D, Rha, S.Y, Izbicka, E, Von Hoff, D.D, and Hurley, L.H. Design and Synthesis of Fluoroquinophenoxazines that Interact with G-Quadruplexes and their Biological Efects. Molecular Cancer Therapeutics. 2001, 1, 103-120.

4.Emmanuelle, J. M, Daruka, M, Hariprasad, V, Margareta, B, Ryan, W, Amy, C, Alan, P.K and Garth, P. Specific Inhibition of the Akt1 Pleckstrine Homology Domain by D-3-Deoxy-Phosphatidyl-myo- Inositol Analogs. Molecular Cancer Therapeutics. 2002, (submitted).

5.Hariprasad, V, Bearss, D. J, Rubin, M, Sangeeta, R, Hurley, L.H, Von Hoff, D.D and Daruka Mahadevan. Targeting Aurora2 Kinase in Pancreatic Cancer: Structural bioinformatics approach to target validation and rational drug design. J.Med.Chem. 2002 (in preparation).

6.Hariprasad, V, Youngwa, N, Kim, M.-Y and Hurley, L.H. Derivation of Pharmacophore, CoMFA and COMSIA Studies on Some Quinobenzoxazines as Topoisomerase II Inhibitors. J.Med.Chem. 2002, (in preparation).

7.Hariprasad, V and Gurdial Singh. One Pot Synthesis of Oligosaccharides VIA Activation of anomeric Propane-1,3-diylphosphates. Tetrahedron Letters. 2002 (in preparation).

8.Hariprasad, V and Gurdial Singh. Stereoselective Synthesis of S-Linked ?-Mannopyranosides using glycosyl donor substituted by propane 1,3-diyl phosphates as anomeric leaving group. (in preparation).

9.Hariprasad, V, Gurdial Singh and Isabelle Tranoy. Stereoselective O-glycosylation reactions using glycosyl donors substituted by diphenylphosphinate and propane-1,3-diyl phosphate as anomeric leaving groups. Tetrahedron: Asymmetry. 2001, 12, 1373-1381.

10.Hariprasad, V and Gurdial Singh. Efficient Stereocontrolled Synthesis of C-glycosides using glycosyl donors substituted by propane 1,3-diyl phosphate as the anomeric-leaving group. Tetrahedron: Asymmetry. 2001, 12, 1727-1735.

11.Hariprasad, V and Gurdial Singh. New Glysosylation Strategy for the Synthesis of Mannopyranosides. Tetrahedron Asymmetry. 2000, 11, 125-138.

12.Mark P. Prickett, Gurdial Singh and Hariprasad, V. Synthesis of a novel oxoxanthenoisoquinoline via a palladium-catalysed cross-coupling reaction; as a fluorophore. Tetrahedron Letters. 2000, 41, 2987-2990.

13.Hariprasad, V and Gurdial Singh. Stereoselective synthesis of ?-L-Fucp-(1,2)- and -(1,3)-?-D- Galp(1)-4-methylumbelliferone using glycosyl donor substituted by propane-1,3-diyl phosphate as leaving group. J. Chem.Soc. Perkin Trans.1. 2000, 2187-2193.

14.George, L, Paul, L. C, Hariprasad, V and Gurdial Singh. A Simple Polar Deacetylated Caloporoside derivative is a positive modulator of the GABAA chloride channel complex in cortical mammalian neurones. Bioorg. Med. Chem. Lett. 2000, 10, 1759-1761.

15.Hariprasad, V and Gurdial Singh. Synthesis of Fucosidase Substrates using Propane-1,3-diyl phosphate as the Anomeric Leaving Group. Tetrahedron Letters. 1999, 40, 3925-3928.

16.Hariprasad, V, Gurdial Singh and Isabelle Tranoy. Stereoselective O-Glycosylation Reactions Employing O-Diphenylphosphinate and Propane-1,3-diyl Phosphate as Anomeric Leaving Groups. J. Chem. Soc. Chem.Commun. 1998, 2129-2130.

17.Hariprasad, V, Talele, T.T and Kulkarni, V.M. Crystal-Structure-Based Design and Synthesis of Novel Series of Non-peptidic Potential HIV-1 Protease Inhibitors. Pharm.Pharmcol. Commun. 1998, 4, 365-372.

18.Talele, T. T, Hariprasad, V and Kulkarni, V.M. Docking analysis of Series of Cytochrome P-450 14? DM Inhibiting Azole Antifungals. Drug Design and Discovery. 1998, 15, 181-190.

19.Hariprasad,V and Kulkarni, V.M. Docking of a Series of Peptide-Based Interleukin-1?? Converting Enzyme Inhibitors with Aspartyl Hemiacetals, ?-((2,6-Dichlorobenzyl)oxy)methyl and (Acyloxy)methyl Ketone moieties. J. Mol. Modeling. 1997, 3, 443-454.

20.Hariprasad, V and Kulkarni, V.M. A Molecular Dynamics Study of the Three-Dimentional Model of the Human Synovial Fluid Phospholipase A2 - Transition State Mimic Complexes. J. Mol. Recogn. 1996, 9, 95-102.

21.Hariprasad, V and Kulkarni, V.M. A Proposed Common Spatial Pharmacophore and the Corresponding Active Conformations of some Peptide Leukotriene Receptor Antagonists. J. Comput.- Aided. Mol. Design. 1996, 10, 284-292.

22.Nargund, L.V.G, Mamle Desai, S.N, Shishoo, C.J and Hariprasad, V. 2,4-N-Aryl-as-triazines as Potential Antiinflammatory agents. Indian. J. Chem. 1996, 35B, 83-85.

23.Nargund, L.V.G, Reddy, G.R.N, and Hariprasad, V. Synthesis and Antibacterial Activity of a Series of 5-(4-acetamido phenoxymethyl)-1-aryl-1,3,4-Triazoles Thiadiazoles and 1-p-acetamido phenoxy methane carbonyl-N'-[3',4',5'-trisubstituted]-Pyrazoles. Indian. J. Chem. 1996, 35B, 499-502.

24.Nargund, L.V.G, Reddy, G.R.N and Hariprasad, V. Antiinflammatory Activity of Substituted 1,3,4- Oxadiazoles. J. Pharm. Sci. 1994, 83, 246-248.

25.Nargund, L.V.G, Manohara, Y.L.N and Hariprasad, V. Synthesis and Biological Activity of 6- Fluorocinnolins. Indian. J. Chem. 1994, 33B, 1001.

26.Nargund, L.V.G, Reddy, G.R.N and Hariprasad, V. Inhibition of Albumin Denaturation and Antiinflammatory Activity of Acetamido [(phenyl-4'yl)-oxymethyl)] 2-(p-substituted phenylamino)- 1,2,4-triazoles and 1,3,4-thiadiazoles. Indian. J. Exp. Biol. 1993, 31, 395-396.

27.Nargund, L.V.G, Reddy, G.R.N, and Hariprasad, V. Synthesis of Fluorinated Phenyl Styryl Ketones and N-phenyl-5-substituted Aryl-3-p(fluorophenyl) Pyrazoles and Pyrazolins as potential Antimicrobial agents. Indian. J. Pharm. Sci. 1993, 55(1), 1-5. 502.

28.Hariprasad, V and Nargund, L.V.G. Carcinogenic N-Notrosamines (Review), Pharmag (Published by Indian Pharmaceutical Association, Manipal, India). 1993, 5, 1-4.

29.Nargund, L.V.G, Hariprasad, V and Reddy, G.R.N. Synthesis and Antiinflammatory Activity of Fluorinated Phenyl Styryl Ketones and N-phenyl-5-substituted Aryl-3-p(fluorophenyl) Pyrazoles and Pyrazolins. J. Pharm. Sci. 1992, 81, 892-894.

Patents 30.Hriprasad, V, Talele, T.T and Kulkarni, V.M. Substituted alkenoyl 4-hydroxycoumarins as HIV-1 protease inhibitors: Patent No:182397 (Application No.369/Bom/96 dated 15-7-1997).

31.Hariprasad, V, Talele, T.T and Kulkarni, V.M. 2-Substituted-3-hydroxy-4-oxo-4H-1-benzopyrans as HIV-1 protease inhibitors: Patent No: awaiting (Applicatin No:368/Bom/96 dated 15-7-1996).

Presentations:

1.Hariprasad V*, Daruka, M, Sangeeta R, David J. Bearss, and Hurley, L.H. Structure-based design of aurora kinase-2 inhibitors: homology modeling and molecular dynamics docking simulation studies, *Scheduled for presentation in the Poster discussion session Chemistry 7 on Tuesday, April 9, 2002 at AACR 93rd annual meeting, San Francisco, USA.

2.Hariprasad, V*, Kim, M.-Y and Hurley, L.H. Docking and molecular dynamics simulations of telomestatin: a novel human telomeric G quadruplex-interactive agent. Scheduled for presentation at the Poster session Chemistry 6 on Tuesday, April 9, 2002 at AACR 93rd annual meeting, San Francisco, USA.

3.Hariprasad,V and Kulkarni, V.M*. Docking of a Series of Peptide-Based Interleukin-1?? Converting Enzyme Inhibitors with Aspartyl Hemiacetals, ?-((2,6-Dichlorobenzyl)oxy)methyl and (Acyloxy)methyl Ketone moieties. *Presented at 20th IUPAC on the Chemistry of Natural Products in Biomolecules (Sep.96) at Chicago, USA.

4.*Hariprasad, V and Kulkarni, V.M. Modeling of Competitive Peptide Bradykinin Receptor Antagonists from Conformationally Restricted Linear Peptides.*Presented at 46th Indian Pharmaceutical Congress (Dec.94), Chandighar, India.

5.Nargund, L.V.G, Reddy, G.R.N, and *Hariprasad, V. Synthesis and Antibacterial Activity of a Series of 5-(4-acetamido phenoxymethyl)-1-aryl-1,3,4-Triazoles Thiadiazoles and 1-p-acetamido phenoxy methane carbonyl-N'-[3',4',5'-trisubstituted]-Pyrazoles. Presented at 46th Indian Pharmaceutical Congress (Dec.94), Chandighar, India.

6.Nargund, L.V.G, Reddy, G.R.N, Hariprasad, V and *Hukkeri, V.T. Synthesis of Fluorinated Phenyl Styryl Ketones and N-phenyl-5-substituted Aryl-3-p(fluorophenyl) Pyrazoles and Pyrazolins as potential Antimicrobial agents. Presented at 43rd Indian Pharmaceutical Congress (Dec.91), Goa, India.

7.Hariprasad, V and Kulkarni, V.M. A *Molecular Dynamics Study of the Three-Dimentional Model of the Human Synovial Fluid Phospholipase A2 - Transition State Mimic Complexes. *Accepted for poster for 36th Annual Buafalo Med. Chem. on Mol. Recogn. in Drug Design (May.95) at University of Baffalo, USA.

8.Hariprasad, V, Talele, T.T and Kulkarni, V.M. *Crystal-Structure-Based Design and Synthesis of Novel Series of Non-peptidic Potential HIV-1 Protease Inhibitors. *Accepted for poster for Structure- Based Drug Design symposium (June. 95) at Rutgers, the State University of New Jersey, USA.