Department


Basic & Clinical Sciences
Pharmaceutical Sciences

Assistant Professor
Focus: Medicinal Chemistry

Contact Information
(518) 694-7224
Christopher.Cioffi@acphs.edu


Speaker Request
Christopher Cioffi, PH.D.

PRIMARY ACADEMIC APPOINTMENT - Dept. of Basic and Clinical Sciences

SECONDARY ACADEMIC APPOINTMENT - Dept. of Pharmaceutical Sciences (Albany Campus)

* * * * *

EDUCATION

  • Ph.D. in Organic Chemistry, Rensselaer Polytechnic Institute, Troy, NY
  • B.S. in Chemistry, Rensselaer Polytechnic Institute, Troy, NY

COURSES TAUGHT AT ACPHS

  • Organic Chemistry I

RESEARCH INTERESTS

  • Medicinal chemistry and small molecule drug discovery
  • Structure- and ligand-based drug design
  • Synthesis of molecular probes for identifying novel targets and elucidating cellular and molecular pharmacology 

RESEARCH GRANTS

Project Title: Pharmacological treatment for atrophic age-related macular degeneration compounded by common forms of age-related amyloid disease
Funding Agency: National Institutes of Health/National Eye Institute
Amount: $1.45 million
Term: February 1, 2018 - January 31, 2021
Role: Co-Principal Investigator 

PROFESSIONAL ORGANIZATION MEMBERSHIPS

  • American Chemical Society
  • The New York Academy of Science

SELECTED PUBLICATIONS

PUBLICATIONS

Shin Y, Moiseyev G, Petrukhin K, Cioffi CL, Muthuraman P, Takahashi Y, Ma JX. A novel RPE65 inhibitor CU239 suppresses visual cycle and prevents retinal degeneration. Biochimica et Biophysica Acta 2018, 1864, 2420-2429. PMID: 29684583.

Racz B, Varadi A, Kong J, Allikmets R, Pearson PG, Johnson G, Cioffi CL, Petrukhin KA. Non-retinoid antagonist of retinol-binding protein 4 rescues phenotype in a mouse model of Stargardt disease without inhibiting the visual cycle. Journal of Biological Chemistry 2018, 293, 11574-11588. PMID: 29871924.

Cioffi CL. Modulation of glycine-mediated spinal neurotransmission for the treatment of chronic pain. Journal of Medicinal Chemistry 2018, 61, 2652-2679. PMID: 28876062.

Cioffi CL. Glycine transporter-1 inhibitors: a patent review (2011-2016). Expert Opinion on Therapeutic Patents 2018, 28, 197-210. PMID: 29338548.

Cioffi, C. “Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain” J. Med. Chem. 2017, In Press. doi: 10.1021/acs.jmedchem.7b00956; PMID:28876062.

Cioffi, C.; Liu, S.; Wolf, M. A.; Guzzo, P. R.; Sadalapure, K.; Parthasarathy, V.; Loong, D. T.; Maeng, J. H.; Carulli, E.; Fang, X.; Karunakaran, K.; Matta, L.; Choo, S. H.; Panduga, S.; Buckle, R. N.; Davis, R. N.; Sakwa, S. A.; Gupta, P.; Sargent, B. J.; Moore, N. A.; Luche, M. M.; Carr, G. J.; Khmelnitsky, Y. L.; Ismail, J.; Chung, M.; Bai, M.; Leong, W. Y.; Sachdev, N.; Swaminathan, S.; Mhyre, A. J. “Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1”   J. Med. Chem. 2016, 59, 8473.

Cioffi, C.; Guzzo, P. “Inhibitors of Glycine Transporter-1: Potential Therapeutics for the Treatment of CNS Disorders” Curr. Top. Med. Chem. 2016, 16, 3404.

Cioffi, C.; Racz, B.; Freeman, E.; Conlon, M.; Chen, P.; Stafford, D.; Schwarz, D.; Zhu, L.; Kitchen, D.; Barnes, K.; Dobri, N.; Michelotti, E.; Cywin, C.; Martin, W.; Pearson, P.; Johnson, G.; Petrukhin, K. “Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4 (RBP4): Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease” J. Med. Chem. 2015, 58, 5863.

Cioffi, C.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Stafford, D.; Schwarz, D.; Golden, K.; Zhu, L.; Kitchen, D.; Barnes, K.; Racz, B.; Qin, Q.; Michelotti, E.; Cywin, C.; Martin, W.; Pearson, P.; Johnson, G.; Petrukhin, K. “Design, Synthesis, and Evaluation of Non-retinoid Retinol Binding Protein 4 Antagonists for the Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease” J. Med. Chem. 2014, 57, 7731.

Cioffi, C. "Modulation of NMDA Receptor Function for the Potential Treatment of Schizophrenia" Bioorg. Med. Chem. Lett. 2013, 23, 5034.

Cioffi, C.; Liu, S.; Wolf, M.; Mhyre, A.; Guzzo, P.; Sadalapure, K.; Maeng, J-H.; Parthasarathy, V.; Loong, D.; Carulli, E.; Matta, L.; Anandamma, K.; Choo, S.; Xiao, F.; Swaminathan, V.; Sachdev, N. "Design, Synthesis, and SAR of N-((1-4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1" Bioorg. Med. Chem. Lett. 2013, 23, 1257.

Manning, D.; Cioffi, C.; Usyatinsky, A.; Fitzpatrick, K.; Masih, L.; Guo, C.; Zhang, Z.; Sikkander, M-I.; Ryan, K.; Naginskaya, J.; Hassler, C.; Dobritsa, S.; Wierschke, J.; Early, W.; Butler, A.; Brady, C.; Barnes, N.; Cohen, M.; Guzzo, P. "Novel Serotonin Type 3 Receptor Partial Agonists for the Potential Treatment of Irritable Bowel Syndrome" Bioorg. Med. Chem. Lett. 2011, 21, 58.

Cioffi, C.; Lansing, J.; Yuksel, H. "Synthesis of 2-Aminobenzoxazoles Using Tetramethylorthocarbonate or 1, 1-Dichlorodiphenoxymethane" J. Org. Chem. 2010, 75, 7942.

Cioffi, C.; Liu, S.; Wolf, M. "Recent Developments in Glycine Transporter-1 Inhibitors" Annual Reports in Medicinal Chemistry, 2010, 45, chapter 2, 19.

Cioffi, C.; Spencer, W.; Richards, J.; Herr, R. J. "Generation of 3-Pyridyl Biaryl Systems via Palladium-Catalyzed Suzuki Cross-Couplings of Aryl Halides with 3-Pyridylboroxin" J. Org. Chem. 2004, 69, 2210.

Wentland, M.; Ye, Y.; Cioffi, C.; Lou, R.; Zhou, Q.; Xu. G.; Duan, W.; Denhardt, C.; Sun, X.; Cohen, D.; Bidlack, J. "Synthesis and Opioid Receptor Binding Affinities of 8-Amino-2, 6-methano-3-benzazocines" J. Med. Chem. 2003, 46, 838.

SELECTED POSTER PRESENTATIONS

Moore, N.; Cioffi, C.; Liu, S.; Mhyre, A.; Luche, M.; Guzzo, P.; Rassoulpour, A. Preclinical development of a novel class of competitive inhibitors of the Glycine Transporter-1 (GlyT-1) for the treatment of cognitive deficits. 45th Annual Society for Neuroscience Conference, Chicago, IL, October 17-21, 2015.

Cioffi, C.; Liu, S.; Wolf, M.; Guzzo, P.; Sadalapure, K.; Parthasarathy, V.; Maeng, J-H.; Carulli, E.; Loong, D.; Fang, X.; Gupta, P.; Panduga, S.; Kalesh, K.; Matta, M.; Choo, S.; Buckle, R.; Davis, R.; Sakwa, S.; Hu, M.; Dethe, D.; Decornez, H.; Kitchen, D.; Sargent, B.; Moore, N.; Luche, M.; Khmelnitsky, Y.; Ismail, J.; Adolphson, J.; Padilla, G.; Waikins, K.; Tom, S.; Ngo, A.; Chung, M.; Bai, M.; Johal, N.; Swaminathan, S.; Mhyre, A. “Discovery, SAR, and Biological Evaluation of a Novel Series of Piperazine-Based Inhibitors of Glycine Transporter-1” Abstracts of Papers, 249th ACS National Meeting & Exposition, Denver, CO, US, March 22-26, 2015, MEDI-68.

Manning, D.; Cioffi, C.; Wierscke, J.; Barnes, N.; Moore, N.; Guzzo, P. “The 5-HT3 Partial Agonist ALB-137391(a) for the Treatment of IBS-D” 34th National Medicinal Chemistry Symposium, Charleston, SC, May 18-21, 2014.

Moore, N.; Mhyre, A.; Cioffi, C.; Guzzo, P.; Luche, M.; Liu, S.; Swaminathan, S. “A Novel Series of Competitive GlyT-1 Inhibitors for the Treatment of Schizophrenia” Translation CNS Summit, Boston, MA, May 21-23, 2013.

Mantlo, N.; Cao, G.; Fields, T.; Wang, X.; Chen, X.; Cioffi, C.; Dinn, S.; Fernandez, M-C.; Mateo, A.; Escribano, A.; Martin de la Nava, E.; Parthasarathy, S.; Giese, M.; Carson, M.; Beyer, T.; Cockerham, S.; Kovach, K.; Sweetana, S.; Borel, A.; Jones, T.; Cannady, E. "Discovery and SAR of the Benzazepine Based Chloesteryl Ester Transfer Protein Inhibitor, Evacetrapib" Abstracts of Papers, 243rd ACS National Meeting & Exposition, San Diego, CA, US, March 25-29, 2012, MEDI-235.

Mhyre, A.; Cioffi, C.; Beebe, A.; Moore, N.; Guzzo, P.; Luche, M.; Sargent, B.; Liu, S. "A Novel Series of GlyT-1 Inhibitors for the Treatment of Schizophrenia: Is Binding Competitively with Glycine Important?" Society for Neuroscience, Washington, DC, November 12-16, 2011.

Cioffi, C.; Liu, S.; Moore, N.; Guzzo, P.; Wolf, M.; Mhyre, A. "AMR-GLY-3, A Novel GLYT-1 Inhibitor for the Treatment of Schizophrenia" NYAS Advancing Drug for Schizoprenia, New York, NY, March 11-12, 2011.

Manning, D.; Cioffi, C.; Usyantinsky, A.; Fitzpatrick, K.; Masih, L.; Guo, C.; Zhang, Z.; Choo, S.; Sikkander, M-I.; Ryan, K.; Naginskaya, J.; Hassler, C.; Dobritsa, S.; Wierschke, J.; Early, W.; Butler, A.; Brady, C.; Barnes, N.; Cohen, M.; Guzzo. P. “The Discovery of Novel 5-HT3 Receptor Partial Agonists for the Potential Tratment of Irritable Bowel Syndrome“ EFMC-ISMC 2010, 21st International Symposium on Medicinal Chemistry, Brussels, Belgium, September 5-9, 2010.

PATENTS

ARF6 Inhibitors and Methods of Synthesis and Use Thereof, Ostanin, K.; Shenderovich, M.; Bajji, A.; Cioffi, C.; Moss, N.; Vankayalapati, H.; Li, D. PCT Patent Application No. WO 2015183989.

4-Phenyl Piperidines, Their Preparation and Use, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L. PCT Patent Application No. WO 2015168286 A1.

4-Phenyl Piperidines, Their Preparation and Use, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L. PCT Patent Application No. WO 2014152013 A1.

Octahydropyrrolopyrroles, Their Preparation and Use, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Cywin, C.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L. PCT Patent Application No. WO 2014151936 A1.

N-Alkyl-2-phenoxyethanamines, Their Preparation and Use, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L. PCT Patent Application No. WO 2014151959 A1.

Octahydrocyclopentapyrroles, Their Preparation and Use, Petrukhin, K.; Cioffi, C.; Johnson, G.; Allikmets, R.; Dobri, N.; Freeman, E.; Conlon, M.; Chen, P.; Zhu, L. PCT Patent Application No. WO 2014152018 A1.

RBP4 Antagonists for the Treatment of Age-Related Macular Degeneration and Stargardt Disease, Petrukhin, K.; Cioffi, C.; Allikmets, R. US Provisional Application No. 61/785,227.

5-HT3 Receptor Modulators, Methods of Making and Use Thereof, Manning, D.; Cioffi, C., US Patent No. 8710047 B2.

5-HT3 Receptor Modulators, Methods of Making and Use Thereof, Manning, D.; Cioffi, C., US Patent No. 8501729 B2.

5-HT3 Receptor Modulators, Methods of Making and Use Thereof, Manning, D.; Cioffi, C., US Patent No. 8124600 B2.

N-[(Sulfonylpiperazinyl)cycloalkyl]methyl Carboxamide Derivatives as Glycine Transporter-1 Inhibitors and their Preparation, Cioffi, C., Wolf, M.; Guzzo, P.; Sadalapure, K., US Patent No. 9045445 B2.

Synthesis of 2-Aminobenzoxazole Compounds Starting from 2-Aminophenols and Amines, Cioffi, C., US Patent No. 8178666 B2.

Compounds and Methods for Treating Dyslipidemia, Cao, G.; A.; Escribano, A.; Fernandez, M-C.; Fields, T.; Gernert, D.; Cioffi, C.; Herr, R.; Mantlo, N.; Martin de la Nava, E-M.; Mateo-Herranz, A.; Mayhugh, D.; Wang, X. US Patent No. 7749992 B2.

Preparation of Ben[b]azepines and Related Compounds as Inhibitors of Cholesterol Ester Transfer Protein for Treating Dyslipidemia, Chen, X.; Dinn, S.; Cioffi, C.; Escribano, Fernandez, M-C.; Carmen, M.; Fields, T.; Herr, R.; Mantlo, N.; Martin de la Nava, E-M.; Isabel, A.; Partsarathy, S.; Wang, X. US Patent No. 7786108 B2.

CONFERENCES AND PRESENTATIONS

Cioffi CL. Design, Synthesis, and Evaluation 0f Non-Retinoid Retinol Binding Protein 4 Antagonists for the Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease. Abstracts of Papers, 256th ACS National Meeting & Exposition, Boston MA, August 19-24, 2018, MEDI-9.

EXTRAMURAL GRANTS

Role: Co-Principal Investigator (with Konstantin Petrukhin)
Project Title: Pharmacological treatment for atrophic age-related macular degeneration compounded by common forms of age-related amyloid disease
Grantor: National Institutes of Health – National Eye Institute 
Amount: $1,452,045 
Grant Number: 1R01EY028549-01
Term: 2/01/2018 – 1/31/2021