Publications

Publications for Medicinal Chemistry Lab

Antczak, M. I.; Zhang, Y.; Wang, C.; Doran, J.; Naidoo, J.; Voruganti, S.; Williams, N, S.; Markowitz, S.D.*; Ready, J.M.* Inhibitors of 15-Prostaglandin Dehydrogenase to Potentiate Tissue Repair. J. Med. Chem. 2017, 60, 3979-4001. PMID: 28398755.

Rujirawanich, J.; Kim, S.; Ma, A.-J.; Butler, JR.; Wang, C.; Rosen, M.; Posner, B.; Nijhawan, D.; Ready, J.M.* Synthesis and Biological Evaluation of Kibdelone C and Its Simplified Derivatives. J. Am. Chem. Soc. 2016, 138, 10561-10570. PMID: 27459345.

Theodoropoulos, P.C.; Gonzales, S.G.; Winterton, S.E.; Rodriguez-Navas, C.; McKnight, J.S.; Morlock, L.K.; Owen, A.E.; Duan, Y.; Moreno, J.R.; Hanson, J.M.; Cross, B.; Lemoff, A.; Mirzaei, H.; Posner, B.A.; Williams, N.S.; Ready*, J.M.; Nijhawan, D.* Discovery of Tumor-Specific Irreversible Inhibitors of Stearoyl CoA Desaturase. Nature Chem Biol, 2016, 12, 218-225. PMID: 26829472.

Zhang, Y.; Desai, A.; Yang, S. Y.; Bae, K. B.; Antczak, M. I.; Fink, S. P;. Tiwari, S.; Willis, J. E.; Williams, N. S.; Dawson, D. M.; Wald, D.; Chen, W.; Wang, Z.; Kasturi, L.; Larusch, G.; He, L.; Cominelli, F.; Di Martino, L.; Cjuric, Z.; Milne, G. L.; Chance, M.; Sanabria, J.; Dealwis, Ch.; Mikkola, D.; Naidoo, J.; Wei, S.; Tai, H.; Gerson, S. L.; Ready, J. M.*; Posner, B.*; Willson, J. K. V.*; Markowitz, S. D.* Inhibition of the prostaglandin- degrading enzyme 15-PGDH potentiates tissue regeneration. Science 2015, 348, aaa2340. PMID: 26068857

Jesus-Cortes, H. D.; Miller, A. D.; Britt, J. K.; DeMarco, A. J.; Jesus-Cortes, M. D.; Stubing, E.; Naidoo, J.; Vazquez-Rosa, E.; Morlock, L; Williams, N. S.; Ready, J. M.; Narayanan, N. S.; Pieper, A. A.* Protective efficacy of P7C3-S243 in the 6-hydroxydopamine model of Parkinson’s disease. NPJ Parkinson’s Disease, 2015, 15010. PMID: 27158662.

Walker, A. K.; Rivera, P. D.; Wang, Q.; Chuang, J.-C.; Tran, S.; Osborne-Lawrence, S.; Estill, S. J.; Starwalt, R.; Huntington, P.; Morlock, L.; Naidoo, J.; Williams, N.; Ready, J. M.; Eisch, A. J.; Piper, A. A.*; Zigman, J. M.* The P7C3-class of neuroprotective compounds exerts antidepressant efficacy in mice by increasing hippocampal neurogenesis. Mol. Psychiatry 2015, 20, 500-8. PMID:24751964.

Kemp, S. W. P.; Szynkaruk, M.; Stanoulis, K. N.; Wood, M. D.; Liu, E. H.; Willand, M. P.; Morlock, L.; Naidoo, J; Williams, N. S.; Ready, J. M.; Namgano, T. J.; Beggs, S.; Salter, M. W.; Gordon, T; Pieper, A. A.*; Borschel, G. H.* Pharmacologic rescue of motor and sensory neurons by the neuroprotective compound P7C3 following neonatal nerve injury. Neuroscience, 2014, 284, 202-16. PMID: 25313000.

Wang, G.; Han, T,; Nijhawan, D.; Theodoropoulos, P.; Naidoo, J.; Yadavalli, S.; Mirzaei, H.; Pieper, A.; Ready, J. M.,* McKnight, S. L.* The P7C3 Class of Neuroprotective Chemicals Function by Activating the Rate-limiting Enzyme in NAD Salvage. Cell 2014, 158, 1324-1334. PMID: 25215490.

Yin, T.C.; Britt, J.K.; De Jesus-Cortes, H.; Lu, Y.; Genova, R.M.; Khan, M.Z.; Voorhees, J.R; Shao, J.; Katzman, A.C.; Huntington, P.J.; Wassink, C.; McDaniel, L.; Newell, E.A.; Dutca, L.M.; Naidoo, J.; Cui, H.; Bassuk, A.G.; Harper, M.M.; McKnight, S.L.; Ready, J.M.; Pieper, A.A. P7C3 Neuroprotective Chemicals Block Axonal Degeneration and Preserve Function after Traumatic Brain Injury. Cell Reports 2014, 8, 1731-1740. PMID: 25220467.

Naidoo, J.; De Jesus-Cortes, H.; Huntington, P.; Estill, S; Morlock, L. K.; Starwalt, R.; Mangano, T. J.; Williams, N. S.; Pieper, A. A.*; Ready, J. M.* Discovery or a Neuroprotective Chemical, (S)-N-(3-(3,6-Dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridine-2-amine [(-)-P7C3-S243], with Improved Druglike Properties. J. Med. Chem. 2014, 57, 3746. PMID: 24697290.

Pieper, A. A.; McKnight, S. L.; Ready, J. M.* P7C3 and an unbiased approach to drug discovery for neurodegenerative diseases. Chem. Soc. Rev. 2014, 43, 6716-6726. PMID:24514864.

Brown, C.S.; Lee, M.S.; Leung, D.W.; Wang, T.; Xu, W.; Luthra, P.; Anantpadma, M.; Shabman, R.S.; Melito, L.M.; MacMillan, K.S.; Borek, D.M.; Otwinowski, Z.; Ramanan, P.; Stubbs, A.J.; Peterson, D.S.; Binning, J.M.; Tonelli, M.; Olson, M.A.; Davey, R.; Ready, J.M.; Basler, C.F.; Amarasinghe, G.K.* In silico derived small molecules bind the filovirus VP35 protein and inhibit its polymerase cofactor activity, J. Mol. Biol. 2014, 2045. PMID: 24495995.

Kilgore, J. A.; Du, X.; Melito, L.; Wei, S.; Wang, C.; Chin, H. G.; Posner, B.; Pradhan, S.; Ready, J. M.; Williams, N. S.* Identification of DNMT1 Selective Antagonists Using a Novel Scintillation Proximity Assay. J. Biol. Chem. 2013, 288, 19673. PMID: 23671287.

Naidoo, J.; Bemben, C. J.; Allwein, S. R.; Liang, J.; Pieper, A. A.; Ready, J. M.* Development of a Scalable Synthesis of P7C3-A20, a Potent Neuroprotective Agent. Tetrahedron Lett. 2013, 54, 4429.

De Jesús-Cortés, H.; Xu, P.; Drawbridge, J.; Estill, S. J.; Huntington, P.; Tran, S.; Britt, J.; Tesla, R.; Morlock, L.; Naidoo, J.; Melito, L. M.; Williams, N. S.; Ready, J. M.*; McKnight, S. L.*; Pieper, A. A.* Neuroprotective Efficacy of Aminopropyl Carbazoles in a Mouse Model of Parkinson’s Disease. Proc. Natl. Acad. Sci. USA, 2012, 109, 17010. PMID: 23027934.

Tesla, R.; Wolf, H. P.; Xu, P.; Drawbridge, J.; Estill, S. J.; Huntington, P.; McDaniel, L.; Knobbe, W.; Morlock, L.; Naidoo, J.; Williams, N. S.; Ready, J. M.*; McKnight, S. L.*; Pieper, A. A.* Neuroprotective Efficacy of Aminopropyl Carbazoles in a Mouse Model of Amyotrophic Lateral Sclerosis. Proc. Natl. Acad. Sci. USA, 2012, 109, 17016. PMID: 23027932.

MacMillan, K.S.; Naidoo, J.; Liang, J.; Melito, L.; Williams, N.S.; Morlock, L.; Huntington, P.J.; Estill, S.J.; Longgood, J.;. McKnight, S.L.; Pieper, A.A.; De Brabander, J.K, Ready, J.M.* Development of Proneurogenic, Neuroprotective Small Molecules. J. Am. Chem. Soc. 2011, 133, 1428-1437. PMID: 21210688.

Pieper, A.A.; Xie, S.; Capota, E.; Estill, S.J.; Zhong, J.; Long, J.M.; Becker, G.L.; Huntington.; Goldman, S.E.; Shen, C.H.; Capota, M.; Britt, J.K.; Kotti, T.; Brat, D. J.; Williams, N.S.; MacMillan, K.S.; Naidoo, J.; Melito, L.; Hsieh, J.; De Brabander, J.; Ready, J.M.; McKnight, S.L.* Discovery of a Pro-Neurogenic, Neuroprotective Chemical. Cell 2010, 142, 39-51.

Germanas, J. P.; Wang, S.; Miner, A.; Hao, W.; Ready, J. M.* Discovery of Small-Molecule Inhibitors of Tyrosinase. Bioorg. Med. Chem. Lett. 2007, 6871-6875.

Issued Patents

Ready, J.M.; Nijhawan, D.; Gonzales, S.S.; Theodoropoulos, P. Preparation of benzothiophenes and other compounds and methods and compositions for selective and targeted cancer therapy. 2015. WO 2015/035051 A1.

McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Proneurogenic Compounds. 2015. U.S. Patent No. 9,095,572 B2.

McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Proneurogenic Compounds. 2015. U.S. Patent No. 9,095,571 B2.

McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Methods for Treating Parkinson’s Disease Using Pro-Neurogenic Compounds. 2014, U.S. 8,877,797.

McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Methods of treating traumatic brain injury using pro-neurogenic compounds. 2014, US 8,791,149 B2.

McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Methods of treating post-traumatic stress disorder using pro-neurogenic compounds. 2014, US8,748,473 B2.

McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Methods for treating amyotrophic lateral sclerosis using pro-neurogenic compounds. 2014, US8735440 B2.

Schneider, J.; Hsieh, J.; Frantz, D. E.; McKnight, S. L.; Ready, J. M. Chemical inducers of neurogenesis. 2014, US 8,778,940 B2.

McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Proneurogenic Compounds. 2013. U.S. Patent No. 8,604,074.

McKnight, S.L.; Pieper, A.A.; Ready, J.M.; De Brabander, J. Proneurogenic Compounds. 2013. U.S. Patent No. 8,362,277.

Schneider, J.; Hsieh, J.; Frantz, D. E.; McKnight, S. L.; Ready, J. M. Isoxazole amides, derivatives and methods of chemical induction of neurogenesis. 2012, US 8193225