Marc A. Ilies, Ph. D.
Assistant Professor of Medicinal Chemistry and Pharmaceutics

Department of Pharmaceutical Sciences

3307 N. Broad Street - Philadelphia, PA 19140
Room 517, Phone: 215-707-1749
mailies@temple.edu

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Recent Publications (pdf)

Scientific publications of Dr. Marc A. Ilies

A. Articles in peer-reviewed scientific periodicals

34. M.A. Ilies, W.A. Seitz, B.H. Johnson, E.L. Ezell, A.L. Miller, E.B. Thompson, A.T. Balaban, “Lipophilic Pyrylium Salts in the Synthesis of Efficient Pyridinium-Based Cationic Lipids, Gemini Surfactants, and Lipophilic Oligomers for Gene Delivery”, J. Med. Chem., 49, 3872-3887 (2006).

33. V. Percec, M. Peterca, M.J. Sienkowska, M.A. Ilies, E. Aqad, J. Smidrkal, P.A. Heiney, “Synthesis and Retrostructural Analysis of Libraries of AB3 and Constitutional Isomeric AB2 Phenylpropyl Ether-Based Supramolecular Dendrimers”, J. Am. Chem. Soc., 128, 3324-3334 (2006).

32. M.A. Ilies, B.H. Johnson, F. Makori, A. Miller, W.A. Seitz, E.B. Thompson, A.T. Balaban, “Pyridinium cationic lipids in gene delivery: An in vitro and in vivo comparison of transfection efficiency versus a tetraalkylammonium congener”, Arch. Biochem. Biophys., 435, 217-226 (2005).

31. M.A. Ilies, W.A. Seitz, I. Ghiviriga, B.H. Johnson, A. Miller, E.B. Thompson, A.T. Balaban, “Pyridinium cationic lipids in gene delivery: a structure-activity correlation study”, J. Med. Chem., 47, 3744-3754 (2004).

30. M.A. Ilies, B. Masereel, S. Rolin, A. Scozzafava, G. Cāmpeanu, V. Cīmpeanu, C.T. Supuran, “Carbonic anhydrase inhibitors: Aromatic and heterocyclic sulfonamides incorporating adamantyl moieties with strong anticonvulsant activity”, Bioorg. Med. Chem., 12, 2717-2726 (2004).

29. M.A. Ilies, W.A. Seitz, M.T. Caproiu, M. Wentz, R.E. Garfield and A.T. Balaban, “Pyridinium-Based Cationic Lipids as Gene Transfer Agents”, Eur. J. Org. Chem., 14, 2645-2655 (2003).

28. [M.A. Ilies] “Novel tripeptide inhibitors of hepatitis C virus NS3 serine protease. Bristol-Myers Squibb Co.: WO02060926”, Expert Opin. Ther. Patents, 13 (2), 267-272 (2003) – patent evaluation.

27. M.A. Ilies, D. Vullo, J. Pastorek, A. Scozzafava, M. Ilies, M.T. Caproiu, S. Pastorekova and C.T. Supuran, “Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogeno-aminobenzolamide derivatives”, J. Med. Chem., 46, 2187-2196 (2003).

26. M. Ilies, M.D. Banciu, A. Scozzafava, M.A. Ilies, M.T. Caproiu, and C.T. Supuran, “Protease inhibitors: Synthesis of bacterial collagenase and matrix metalloproteinase inhibitors incorporating arylsulfonylureido and 5-dibenzo-suberenyl/suberyl moieties”, Bioorg. Med. Chem., 11, 2227-2239 (2003).

25. M.A. Ilies, W.A. Seitz and A.T. Balaban, “Cationic lipids in gene delivery: principles, vector design and therapeutical applications”, Curr. Pharm. Des., 8 (27), 2441-2473 (2002).

24. M.A. Ilies, A. Scozzafava and C.T. Supuran, “Therapeutic applications of serine protease inhibitors”, Expert Opin. Ther. Patents, 12 (8), 1181-1214 (2002).

23. M. Ilies, M.D. Banciu, M.A. Ilies, A. Scozzafava, M.T. Caproiu and C.T. Supuran, “Carbonic anhydrase activators: Design of high affinity isozymes I, II and IV activators, incorporating tri-/tetrasubstituted-pyridinium-azole moieties”, J. Med. Chem., 45 (2), 504-510 (2002).

22. M.A. Ilies and A.T. Balaban, “Recent developments in cationic lipid-mediated gene delivery and gene therapy”, Expert Opin. Ther. Patents, 11 (11), 1729-1752 (2001);

21. [M.A. Ilies], "Novel N-substituted-2-cyanopyrrolidines as potent inhibitors of dipeptidyl peptidase IV in the treatment of non-insulin-dependent diabetes mellitus", Expert Opin. Ther. Patents, 10(12), 1937-1942 (2000);

20. A. Casini, A. Scozzafava, F. Mincione, L. Menabuoni, M.A. Ilies, C.T. Supuran, "Carbonic Anhydrase Inhibitors: Water-Soluble 4-Sulfamoylphenylthioureas as Topical Intraocular Pressure-Lowering Agents with Long-Lasting Effects", J. Med. Chem., 43 (25), 4884-4892 (2000);

19. A. Casini, F. Mincione, M.A. Ilies, L. Menabuoni, A. Scozzafava, C.T. Supuran, "Carbonic anhydrase inhibitors: Synthesis and inhibition against isozymes I, II and IV of topically acting antiglaucoma sulfonamides incorporating cis-5-norbornene-endo-3-carboxy-2-carboxamido moieties", J. Enzyme Inhib., 16 (2), 113-123 (2001);

18. C.T. Supuran, A. Scozzafava, M.A. Ilies, F. Briganti, "Carbonic anhydrase inhibitors: synthesis of sulfonamides incorporating 2,4,6-trisubstituted-pyridinium-ethylcarboxamido moieties possessing membrane-impermeability and in vivo selectivity for the membrane-bound (CA IV) versus the cytosolic (CA I and CA II) isozymes", J. Enzyme Inhib., 15(4), 381-401 (1999);

17. M.A. Ilies, C.T. Supuran, A. Scozzafava, "Metal complexes of heterocyclic sulfonamides as potential pharmacological agent in the treatment of gastric acid secretion imbalances", Metal Based Drugs, 7 (2), 57-62 (2000);

16. A. Scozzafava, M.A. Ilies, C.T. Supuran, "Carbonic anhydrase inhibitors. Part 89. Metal complexes of benzolamide with strong enzyme inhibitory and putative antiulcer properties", Rev. Roum. Chim., 45 (7-8), 771-778 (2000);

15. A. Scozzafava, M.A. Ilies, G. Manole, C.T. Supuran, "Protease inhibitors. Part 12. Synthesis of potent matrix metalloproteinase and bacterial collagenase inhibitors incorporating sulfonylated N-4-nitrobenzyl--alanine hydroxamate moieties", Eur. J. Pharm. Sci., 11(1), 69-79 (2000);

14. A. Scozzafava, F. Briganti, M.A. Ilies, C.T. Supuran, “Carbonic anhydrase inhibitors: Synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus the cytosolic isozymes”, J. Med. Chem, 43, 292-300 (2000);

13. Gh. Campeanu, M. Pele, M. Cimpeanu, M. Ilies, M.A. Ilies, “Evaluation of The Activity of Horseradish Peroxidase and Mushroom Polyphenoloxidase on Some Phenols”, Roum. Biotech. Lett., 4, 319-326 (1999);

12. I. Fenesan, R. Popescu, A. Scozzafava, V. Crucin, E. Mateiciuc, R. Bauer, M.A. Ilies, C.T. Supuran, “Carbonic Anhydrase Inhibitors. Phosphoryl-sulfonamides - A New Class of High Affinity Inhibitors of Izozymes I and II”, J. Enzyme Inhib., 15, (3), 297-310 (2000);

11. C.T. Supuran, F. Briganti, A. Scozzafava, M.A. Ilies, “Protease Inhibitors: Part 4. Synthesis of Weakly Basic Thrombin Inhibitors Incorporating Pyridinium-Sulfanilylaminoguanidine Moieties”, J. Enzyme Inhib., 15, 335-356 (2000);

10. C.T. Supuran, A. Scozzafava, F. Briganti, M.A. Ilies, A. Jitianu, "Carbonic Anhydrase Inhibitors. Part 55. Metal Complexes of 1,3,4-Thiadiazole-2-Sulfonamide Derivatives: In Vitro Inhibition Studies With Carbonic Anhydrase Isozyme I, II and IV", Metal Based Drugs, 5, 103-114 (1998);

9. M. Ganciu, S. Udrea, M.C. Penache, I. Vata, I. Iovitz-Popescu, M.A. Ilies, M. Corcimaru, A. Papoiu, B. Serban, A.T. Balaban, "Corona Discharge Controlled Aggregation and Segregation of Solid Materials in Liquids and Associated EHD Phenomena", Rom. J. Phys, 43, 67-77 (1998); partially presented by french TV-channel ARTE on 22 september 1998 (http://www.arte-tv.com/hebdo/archimed/19980922/ftext/sujet3.html);

8. C.T. Supuran, A. Scozzafava, M.A. Ilies, B. Iorga, T. Cristea, F. Briganti, F. Chiraleu, M.D. Banciu, “Carbonic Anhydrase Inhibitors. Part 53. Synthesis of Substituted-Pyridinium Derivatives of Aromatic Sulfonamides: The First Non-Polymeric Membrane-Impermeable Inhibitors with Selectivity for Isozyme IV”, Eur. J. Med. Chem., 33, 577-594 (1998);

7. C.T. Supuran, F. Mincione, A. Scozzafava, F. Briganti, G. Mincione, M.A. Ilies, “Carbonic Anhydrase Inhibitors. Part 52. Metal Complexes of Heterocyclic Sulfonamides: A New Class of Strong Topical Intraocular Pressure-lowering Agents With Potential Use as Antiglaucoma Drugs”, Eur. J. Med. Chem., 33, 247-254 (1998);

6. C.T. Supuran, A. Scozzafava, B.C. Jurca, M.A. Ilies, “ Carbonic Anhydrase Inhibitors. Part 49. Synthesis of Substituted- Ureido and Thioureido Derivatives of Aromatic/ Heterocyclic Sulfonamides with Increased Affinities for Isozyme I”, Eur. J. Med. Chem., 33, 83-93 (1998);

5. M.A. Ilies, M.D. Banciu, M. Ilies, F. Chiraleu, F. Briganti, A. Scozzafava, C.T. Supuran, “Carbonic Anhydrase Activators. Part 17. Synthesis and activation study of 1-(1,2,4- triazole- (1H)-3- yl)-2,4,6- trisubstituted- pyridinium salts against isozymes I, II, IV”, Eur. J. Med. Chem., 32 (11), 911-918 (1997);

4. M. Brezeanu, D. Marinescu, M. Badea, N. Stanica, M.A. Ilies, C.T. Supuran, “1,3,4- Thiadiazole derivatives. Part 8. Binuclear complexes of Cu (II), Mn (II), Co(II), Ni(II), and Zn(II) with a Schiff base derived from 5- amino-1,3,4-thiadiazole-2-sulfonamide”, Rev. Roum. Chim., 42 (9), 727-732 (1997);

3. C.T. Supuran, M.A. Ilies, A. Scozzafava, “Carbonic anhydrase inhibitors. Part 29. Interaction of isozymes I, II and IV with benzolamide-like derivatives, possible precursors of inhibitors with applications in positron emission tomography imaging”, Eur. J. Med. Chem., 33, 739-751 (1998);

2. A. Jitianu, M.A. Ilies, F. Briganti, A. Scozzafava, C.T. Supuran “Complexes with biologically active ligands. Part 9. Metal complexes of 5-benzoylamino and 5-(3-benzoylamino)-1,3,4-thiadiazole-2-sulfonamide as carbonic anhydrase inhibitors”, Metal Based Drugs, 4(1), 1-8 (1997);

1. A. Jitianu, M.A. Ilies, A. Scozzafava, C.T. Supuran, “Complexes with biologically active ligands. Part 8. Synthesis and carbonic anhydrase inhibitory activity of 5- benzoylamido- and 5-(3-nitrobenzoylamido)-1,3,4-thiadiazole-2-sulfonamide and their metal complexes”, Main Group Metal Chem, 20, 151-156 (1997);

B. Book chapters

1. M.A. Ilies and M.D. Banciu, “Non-sulfonamide carbonic anhydrase inhibitors” in “Carbonic Anhydrase, Its Inhibitors and Activators”, C.T. Supuran, A. Scozzafava, J. Conway Eds., CRC Press, Boca Raton, 2004, pp. 207-239.

C. Laboratory textbooks

1. G. Campeanu, M. Ilies, M.A. Ilies, and C. Voaides, “Laboratory works in inorganic chemistry”, Relal Promex Ed., Bucharest, 2003, 87 pages (in Romanian).

2. G. Campeanu, M. Ilies, M.A. Ilies, and C. Voaides, “Experimental Techniques and Laboratory Experiments of Organic Chemistry”, Relal Promex Ed., Bucharest, 2002, 121 pages (in Romanian).

D. Patents:

1. A. T. Balaban, W.A. Seitz, M.A. Ilies, E.B. Thompson, R.E. Garfield, B. H. Johnson, A. Miller, M. Wentz, “Pyridinium cationic lipids as gene transfer agents”, U.S. Patent 20050196863 A1.

E. International Conferences and Congresses, Invited Lectures

- Oxford, UK (1995): Vth International Congress On Carbonic Anhydrases (poster);
- Brasov, Romania (1995): The International Congress on Nuclear Magnetic Resonance;
- Lille, France (1996): “Journees Francophones des Jeunes Physico - Chimistes” (poster);
- Brasov, Romania (1997): International Conference on Imaging NMR Spectrometry;
- Neptun, Romania (1998): “Modern Spectrometric Techniques in Biophysics”;
- Halkidiki, Greece (1999): First International Conference of Balkans' National Chemical Societies (poster);
- Calimanesti-Caciulata, Romania (1999): XXVth National Chemical Conference (with international participation) (poster);
- Calimanesti-Caciulata, Romania (2000): XXVIth National Chemical Conference (with international participation) - (plenary lecture: “Pyridinium Carbonic Anhydrase Inhibitors with Selectivity Against Membrane-Bound Isozyme CA IV”)
- Florence, Italy (2001): Invited lecture at the University of Florence, Department of Chemistry – “Selective Carbonic Anhydrase Inhibitors and Activators”;
- Boston, MA (2001): Drug Discovery Technology 2001 (2 posters);
- Houston, TX (2001): The Welch Conference 2001;
- Galveston, TX (2002): Symposium of Structural Biology 2002;
- Houston, TX (2002): The Keck/GCC 2002 Bioinformatics Symposium;
- Santa Clara, CA (2002): Biophex/Interphex 2002 (2 posters);
- Houston, TX (2002): The Welch Conference 2002;
- Florence, Italy (2002): Invited lecture at the University of Florence, Department of Chemistry – “Pyridinium Group - A Versatile Moiety in Drug Targeting”;
- New Orleans, LA (2003): 225th ACS National Meeting (lecture in the Division of Medicinal Chemistry “Heterocyclic Cationic Lipids As Gene Transfer Agents” – A.T. Balaban, M.A. Ilies, W.A. Seitz, M. Wentz, and R.E. Garfield);
- Galveston, TX (2003): Symposium of Structural Biology 2003;
- Houston, TX (2003): The Welch Conference 2003;
- Anaheim, CA (2004): 227th ACS National Meeting (lecture in the Division of Colloid and Surface Chemistry “Lipophilic pyrylium salts in the synthesis of pyridinium-based cationic lipids and gemini surfactants for gene transfer”– M.A. Ilies, W.A. Seitz, B.H. Johnson, A. Miller, E.B. Thompson, A.T. Balaban); also one poster in the Division of Medicinal Chemistry
- Galveston, TX (2004): Symposium of Structural Biology 2004; (poster)
- Minneapolis, MN (2004): American Society of Gene Therapy’s 7th Annual Meeting; (poster);
- Philadelphia, PA (2004): 228th ACS National Meeting; (poster);
- St. Louis, MO (2005): American Society of Gene Therapy’s 8th Annual Meeting; (poster).
- Long Beach, CA (2007): Controlled Release Society National Meeting; (poster)
- Boston, MA (2007): 234th ACS National Meeting; (lecture in the Division of Polymer and Material Science and Engineering).

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