Fordham University            The Jesuit University of New York
 


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Dr. Martin Di Grandi, Ph.D











Martin Di Grandi, Ph.D.

Assistant Professor of Chemistry
Department of Natural Sciences
College at Lincoln Center

 

 Office:

              Fordham University                    Rose Hill:
               Lincoln Center                          John Mulcahy Hall
              113 West 60th Street                 441 East Fordham Road
              Room LL 808C                          JMH 538 (office), JMH 542 (lab)
              New York, NY 10023                 Bronx, NY 10458
 
Email:     
               
mdigrandi@fordham.edu

Phone:
      
               LC: (212) 636-7141; RH: (718) 817-4447


Fax:
                    (212) 636-6754

Courses Taught in the Department of Natural Sciences:
               Organic Chemistry Lecture and Lab 

Education and Work Experience:

      Ph.D.          March, 1990            New York University
      M.Sc.         June, 1986              New York University
      B.Sc.          May, 1984               Fordham University

      1989-1991: Postdoctoral Fellowship, Hoffmann-La Roche, Nutley, NJ
      1992-1993: Postdoctoral Fellowship, Memorial-Sloan Kettering Cancer Center, NY, NY
      1993-1994: Senior Research Scientist, Lederle Laboratories, Pearl River, NY
      1994-2009: Senior Research Scientist, Wyeth Research, Pearl River, NY
      2009-2010: Senior Research Scientist, Pfizer, Pearl River, NY

Current Interests and Research:
        
       Using medicinal chemistry to improve the biological activity of natural products for the treatment of viral infections and cancer; the total synthesis of natural products.


PUBLICATIONS:

 Publications
 
1.     Wilson, S. R.; Di Grandi, M. J. “The Cinchona Alkaloids: A Silicon Directed Synthesis of Some Advanced Intermediates”, J. Org. Chem., 1991, 56(15), 4766-4772.
 
2.     Di Grandi, M. J.; Wilson, S. R.; Spector, A. “The Design of Peptide Secondary Structure: An Application to Thioredoxin”, Peptides: Chemistry and Biology—Proceedings of the Twelfth American Peptide Symposium, 1992, 337-338.
 
3.     Wilson, S. R.; Tam, K. K.; Di Grandi, M. J.; Cui, W. “The Calculation and Synthesis of a Template Molecule”, Tetrahedron, 1993, 49(17), 3655-3663.
 
4.     Isaacs, R. C. A.; Di Grandi, M. J.; Danishefsky, S. J. “Synthesis of an Enantiomerically Pure Intermediate Containing the CD Substructure of Taxol”, J. Org. Chem., 1993, 58(15), 3938-3941.
 
5.     Di Grandi, M. J.; Jung, D. K.; Krol, W. J.; Danishefsky, S. J. “The Synthesis of Competent Nucleophiles for Delivering the A Ring of Taxol”, J. Org. Chem., 1993, 58(18), 4989-4892.
 
6.     Di Grandi, M. J.; Coburn, C. A.; Isaacs, R. C. A.; Danishefsky, S. J. “Degradative Routes to Electrophilic CD-Substructures of Taxol”, J. Org. Chem., 1993, 58(27), 7728-7731.
 
7.     Danishefsky, S. J.; Masters, J. J.; Young, W.; Link, J. T.; Schnyder, L. W.; Magee, T. V.; Jung, D. K.; Isaacs, R. C. A.; Bornmann, W. G.; Alaimo, C. A.; Coburn, C. A.; Di Grandi, M. J. “The Total Synthesis of Baccatin III and Taxol”, J. Am. Chem. Soc., 1996, 118(12), 2843-2859.
 
8.     Baum, E. Z.; Ding, W.-D.; Siegel, M. M.; Hulmes, J.; Bebernitz, G. A.; Sridharan, L.; Tabei, K.; Krishnamurthy, G.; Carofigli, T.; Groves, J. T.; Bloom, J. D.; Di Grandi, M. J.; Bradley, M.; Ellestad, G.; Seddon, A. P.; Gluzman, Y. “Flavins Inhibit Human Cytomegalovirus UL80 Protease via Disulfide Bond Formation”, Biochemistry, 1996, 35(18), 5847-5855.
 
9.     Di Grandi, M. J.; Tilley, J. W. “The Direct Preparation of Protected Hydrazines from Alcohols Via Mitsunobu Chemistry”, Tetrahedron Lett., 1996, 37(25), 4327-4330;Corrigendum: Tetrahedron Lett. 1996, 37(46), 8261.
 
10.   Plotch, S. J.; O'Hara, B.; Morin, J.; Palant, O.; LaRocque, J.; Bloom, J. D.; Lang Jr., S. L.; Di Grandi, M. J.; Bradley, M.; Nilakantan, R.; Gluzman, Y. “Inhibition of Influenza A Virus Replication by Compounds Interfering with the Fusogenic Function of the Viral Hemagglutinin”, J. Virology, 1999, 73(1), 140-151.
 
11.   Visalli, R. J.; Fairhurst, J.; Srinivas, S.; Hu, W.; Feld, B.; Di Grandi, M. J.; Curran, K.; Ross, A.; Bloom, J. D.; van Zeijl, M.; Jones, T. R.; O’Connell, J.; Cohen, J. I. “Identification of Small Molecule Compounds that Selectively Inhibit Varicella-Zoster Virus Replication”, J. Virology, 2003, 77(4), 2349-2358.
 
12.   Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Curran, K. J.; Ross, A. A.; Norton, E. B.; Terefenko, E.; Jones, T. R.; Feld, B.; Lang, S. A. “Thiourea Inhibitors of Herpes Viruses Part 1: Bis-(Aryl)thiourea Inhibitors of CMV”, Bioorg. Med. Chem. Lett., 2003, 13(17), 2929-2932.
 
13.   Di Grandi, M. J.; Curran, K. A.; Baum, E. Z.; Bebernitz, G.; Ellestad, G. A.; Ding, W.-D.; Lang, S. A.; Rossi, M.; Bloom, J. D. “Pyrido[1,2-b] [1,2,4,5]tetrazines: A New Class of Heterocycles with Flavin-like Redox Properties”, Bioorg. Med. Chem. Lett., 2003, 13(20), 3483-3486.
 
14.   Skotnicki, J. S.; Di Grandi, M. J., Levin, J. I. “Design Strategies for the Identification of MMP-13 and TACE Inhibitors”, Curr. Op. Drug Discovery Develop. 2003, 6, 742-759.
 
15.   Bloom, J. D.; Dushin, R. G.; Curran, K. J.; Donahue, F.; Norton, E. B.; Terefenko, E.; Jones, T. R.; Ross, A. A.; Feld, B.; Lang, S. A.; Di Grandi, M. J. “Thiourea Inhibitors of Herpesviruses: Part 2: N-Benzyl-N’-Arylthiourea Inhibitors of CMV”, Bioorg. Med. Chem. Lett., 2004, 14(13), 3401-3406.
 
16.   Di Grandi, M. J.; Curran, K. J.; Feigelson, G.; Prashad, A.; Ross, A. A.; Visalli, R.; Fairhurst, J.; Feld, B.; Bloom, J. D. “Thiourea Inhibitors of Herpesviruses: Part 3: Inhibitors of Varicella Zoster Virus”, Bioorg. Med. Chem. Lett., 2004, 14(16), 4157-4160.
 
17.   Hu, Y.; Xiang, J. S; Di Grandi, M. J.; Du, X.; Ipek, M.; Laakso, L. M.; Li, J.; Li, W.; Rush, T. S.; Schmid, J.; Skotnicki, J. S.; Tam, S.; Thomason, J. R.; Wang, Q.; Levin, J. I. “Potent, Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitors for the Treatment of Osteoarthritis”, Bioorg. Med. Chem., 2005, 13, 6629-6644.
 
18.   Nittoli, T.; Curran, K.; Insaf, S.; Di Grandi, M.; Orlowski, M.; Chopra, R.v; Agarwal, A.; Howe, A. Y. M.; Prashad, A.; Floyd, M. B.; Johnson, B.; Sutherland, A.; Wheless, K.; Feld, B.; O'Connell, J.; Mansour, T. S.; Bloom, J. “Identification of Anthranilic Acid Derivatives as a Novel Class of Allosteric Inhibitors of Hepatitis C NS5B Polymerase”, J. Med. Chem., 2007, 50(9), 2108-2116; Corrigendum: J. Med. Chem., 2007, 50(24), 6290.
 
19.   Di Grandi, M.; Berger, D. M.; Hopper, D. W.; Zhang, C.; Dutia, M.; Dunnick, A. L.; Torres, N.; Levin, J. I.; Diamantidis; G.; Zapf, C. W.; Bloom, J. D.; Hu, Y.; Powell, D.; Wojciechowicz; D.; Collins, K.; Frommer, E. “Novel Pyrazolopyrimidines as Highly Potent B-Raf Inhibitors”, Bioorg. Med. Chem. Lett., 2009, 19(24), 6957-6961.
  

20.   Di Grandi, M.; Olson, M.; Prashad, A. S.; Bebernitz, G.; Luckay, A.; Mullen, S.; Hu, Y.; Krishnamurthy, G.; Pitts, K.; O’Connell, J. “Small Molecule Inhibitors of HIV RT Ribonuclease H”, Bioorg. Med. Chem. Lett., 2010, 20(1), 398-402.

 

Patents

 

1.                    Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; O’Hara, B. “Diaminopuridine-Containing Thiourea Inhibitors Of Herpes Viruses.” 2000, US Patent 6,166,028 A December 26, 2000.

 

2.                    Bloom, J. D.; Curran, K.: Di Grandi, M. J.; Dushin, R. G.; Jones, T.; Lang, S. A.; Ross, A.; Terefenko, E.; O’Hara, B. “Heterocyclic Carboxamide-Containing Thiourea Inhibitors Of Herpes Viruses Containing A Phenylenediamine Group.” 2001, US Patent 6,197,803 B1, March 6, 2001.

 

3.                    Bloom, J. D.; Curran, K.: Di Grandi, M. J.; Dushin, R. G.; Jones, T.; Lang, S. A.; Ross, A.; Terefenko, E.; O’Hara, B. “Heterocyclic Carboxamide-Containing Thiourea Inhibitors Of Herpes Viruses Containing A Substituted Phenylenediamine Group.” 2001, US Patent 6,201,013 B1, March 13, 2001.

 

4.                    Bloom, J. D.; Curran, K. J.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; Norton, E.; Ross, A.; O’Hara, B. “Alpha-Methylbenzyl-Containing Thiourea Inhibitors Of Herpes Viruses Containing A Substituted Phenylenediamine Group.” 2001, US Patent 6,207,715 B1, March 27, 2001.

 

5.                    Bloom, J. D.; Curran, K. J.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; Norton, E.; Ross, A.; O’Hara, B. “Alpha-Methylbenzyl-Containing Thiourea Inhibitors Of Herpes Viruses Containing A Phenylenediamine Group.” 2001, US Patent 6,255,349 B1, July 3, 2001.

 

6.                    Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; O’Hara, B. “Diaminopyridine-Containing Thiourea Inhibitors Of Herpes Viruses.” 2001, US Patent 6,262,082 B1, July 17, 2001.

 

7.                    Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; O’Hara, B. “Aminopyridine-Containing Thiourea Inhibitors Of Herpes Viruses.” 2001, US Patent 6,262,090 B1, July 17, 2001.

 

8.                    Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; O’Hara, B. “Diaminopyridine-Containing Thiourea Inhibitors Of Herpes Viruses.”  2001, US Patent 6,271,236 B1, August 7, 2001.

 

9.                    Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; Ross, A.; O’Hara, B. “Acetamide And Substituted Acetamide-Containing Thiourea Inhibitors Of Herpes Viruses.” 2002, US Patent 6,335,350 B1, January 1, 2002.

 

10.                 Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; O’Hara, B. “Aminopyridine-Containing Thiourea Inhibitors Of Herpes Viruses.” 2002, US Patent 6,380,243 B1, April 30, 2002.

 

11.                 Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; O’Hara, B. “Diaminopyridine-Containing Thiourea Inhibitors Of Herpes Viruses.” 2002, US Patent 6,403,617 B1, June 11, 2002.

 

12.                 Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; O’Hara, B. “Diaminopyridine-Containing Thiourea Inhibitors Of Herpes Viruses.” 2002, US Patent 6,407,123 B1, June 18, 2002.

 

13.                 Bloom, J. D.; Curran, K.: Di Grandi, M. J.; Dushin, R. G.; Jones, T.; Lang, S. A.; Ross, A.; Terefenko, E. A.; O’Hara, B. “Heterocyclic Carboxamide-Containing Thiourea Inhibitors Of Herpes Viruses Containing A Substituted Phenylenediamine Group.” 2002, US Patent 6,407,249 B1, June 18, 2002.

 

14.                 Bloom, J. D.; Curran, K.: Di Grandi, M. J.; Dushin, R. G.; Jones, T.; Lang, S. A.; Ross, A.; Terefenko, E. A.; O’Hara, B. “Heterocyclic Carboxamide-Containing Thiourea Inhibitors Of Her­pes Viruses Containing A Substituted Phenylenediamine Group.” 2002, US Patent 6,410,571 B1, June 25, 2002.

 

15.                 Bloom, J. D.; Curran, K.: Di Grandi, M. J.; Dushin, R. G.; Jones, T.; Lang, S. A.; Ross, A.; Terefenko, E. A.; O’Hara, B. “Heterocyclic Carboxamide-Containing Thiourea Inhibitors Of Herpes Viruses Containing A Phenylenediamine Group.” 2002, US Patent 6,426,355 B1, July 30, 2002.

 

16.            Bloom, J. D.; Curran, K.: Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; Norton, E.;  Ross, A.; O’Hara, B. “Alpha-Methylbenzyl-Containing Thiourea Inhibitors Of Herpes Viruses Containing A Phenylenediamine Group.” 2002, US Patent 6,462,055 B2, October 8, 2002.

 

17.                 Bloom, J. D.; Di Grandi, M. J.; Dushin, R. G.; Lang, S. A.; O’Hara, B. “Diaminopyridine-Containing Thiourea Inhibitors Of Herpes Viruses.” 2003, US Patent 6,555,561 B2, April 29, 2003.

 

18.         Olson, M. W.; Di Grandi, M.; Prashad, A. “Preparation of Hydantoins Having RNASE Modulatory Activity.” U.S. Pat. Appl. Publ. 2005; 16 pp.; US 2005203156 A1.

 

19.        Olson, M. W.; Di Grandi, M.; Prashad, A. “Carbamates as HIV Anti-viral Agents.” U.S. Pat. Appl. Publ. 2005, 15 pp.; US 2005203176 A1.

 

20.         Hu, Y.; Sum, F.-W.; Di Grandi, M.; Norton, E. “Preparation of anilino-pyrimidine phenyl and benzothiophene analogs as protein kinase inhibitors for treating inflammatory, autoimmune, cardiovascular and other disease.” U.S. Pat. Appl. Publ. 2007, 36pp; US 2007244140 A1.

 

21.         Olson, M.; Di Grandi, M.; Prashad, A. “Preparation of 1,2-Dihydroquinoline Derivatives as Inhibitors of RNase H and HIV Reverse Transcriptase.” 2009, US Patent 7,553,967, June 30, 2009.

 

22.        Olson; M.; Di Grandi, M. “Preparation of Triazole Derivatives for Treating HIV Infections.” 2009, US Patent 7,563,905, July 21, 2009.

 

      23.        Levin, J. I.; Hopper, D. W.; Torres, N.; Dutia, M. D.; Berger, D. M.; Wang, X.; Di Grandi, M. J.; Zhang, C.; Dunnick,A.L. “Preparation of       bridged, bicyclic heterocyclic or spiro bicyclic heterocyclic derivatives of pyrazolo[1,5-a]pyrimidines as Raf kinase inhibitors”,PCT
     Int.Appl., 2009, 159pp; WO 2009108838 A1.


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