Publications

Diastereoselective Alkylation of Activated Nitrogen Heterocycles with Alkenyl Boronate Complexes.
McGettigan, J. E, Jr.; Ready, Joseph M. Diastereoselective Alkylation of Activated Nitrogen Heterocycles with Alkenyl Boronate Complexes. Angew. Chem. Int. Ed., 2023, 62, e202216961.

Diastereoselective Alkylation of Activated Nitrogen Heterocycles with Alkenyl Boronate Complexes

Small molecule inhibitors of 15-PGDH exploit a physiologic induced-fit closing system.
Huang, W.; Li, H.; Kiselar, J.; Fink, S. P.; Regmi, S.; Day, A.; Yuan, Y.; Chance, M.; Ready, J. M.; Markowitz, S. D.; Taylor, D. J. Nature Commun. 2023, 14, 784.

Small molecule inhibitors of 15-PGDH exploit a physiologic induced-fit closing system

Fast-killing tyrosine amide ((S)-SW228703) with blood- and liver-stage antimalarial activity associated with the cyclic amine resistance locus (PfCARL).
Imlay, L. S.; Lawong, A. K.; Gahalawat, S.; Kumar, A.; Xing, C.; Mittal, N.; Wittlin, S.; Churchyard, A.; Niederstrasser, H.; Crespo-Fernandez, B.; Posner, B. A.; Gamo, F.-J.; Baum, J.; Winzeler, E. A.; Laleu, B.; Ready, J. M.; Phillips, M. A. ACS Infectious Diseases 2023, 9, 527-539.

Fast-killing tyrosine amide ((S)-SW228703) with blood- and liver-stage antimalarial activity associated with the cyclic amine resistance locus (PfCARL).

Mechanistic basis for the Iridium-catalyzed enantioselective allylation of alkenyl boronates.
Davis CR, Fu Y, Liu P, Ready JM. J Am Chem Soc. 2022 Sep 7; 144(35):16118-16130. 

Mechanistic basis for the Iridium-catalyzed enantioselective allylation of alkenyl boronates.

Orally bioavailable quinoxaline inhibitors of 15-prostaglandin dehydrogenase (15-PGDH) promote tissue repair and regeneration.
Hu B, Toda K, Wang X, Antczak MI, Smith J, Geboers S, Nishikawa G, Li H, Dawson D, Fink S, Desai AB, Williams NS, Markowitz SD, Ready JM. J Med Chem. 2022 Nov 24; 65(22):15327-15343.

Orally bioavailable quinoxaline inhibitors of 15-prostaglandin dehydrogenase (15-PGDH) promote tissue repair and regeneration.

A male-derived non-ribosomal peptide pheromone controls female schistosome development.
Chen, R.; Wang, J.; Gradinaru, I.; Vu, H. S.; Geboers, S.; Naidoo, J.; Ready, J.M.; Williams, N.S.; DeBerardinis, R.J.; Ross, E.M.; Collins, J.J. Cell, 2022, 185, 1506-1520.

In vivo CRISPR screening identifies BAZ2 chromatin remodelers as druggable regulators of mammalian liver regeneration.
Jia, Y.; Li, L.; Lin, Y.-H.; Gopal, P.; Shen, S.; Zhou, K.; Yu, X.; Sharma, T.; Zhang, Y.; Siegwart, D. J.; Ready, J. M.; Zhu, H. Cell Stem Cell 2022, 29, 372-385.e8.

Hydroesterification and Difunctionalization of Olefins with N‑Hydroxyphthalimide Esters.
Leng, L.; Ready, J.M. ACS Catalysis, 2021, 11, 13714-13720.

Hydroesterification and Difunctionalization of Olefins with N‑Hydroxyphthalimide Esters.

Aryl sulfonamide inhibits entry and replication of diverse influenza viruses via the hemagglutinin protein.
White, K.; Esparza, M.; Liang, J.; Bhat, P.; Naidoo, J.; McGovern, B. L.; Williams, M. A. P.; Alabi, B. R.; Shay, J.; Niederstrasser, H.; Posner, B.; García-Sastre, A.; Ready, J.; Fontoura, B. M. A. J. Med. Chem. 2021, 64, 10951-10966.

Aryl sulfonamide inhibits entry and replication of diverse influenza viruses via the hemagglutinin protein.

Enantioselective Allylation of Alkenyl Boronates Promotes a 1,2-Metalate Rearrangement with 1,3-Diastereocontrol.
Davis, C. R.; Luvaga, I. K.; Ready, J. M. J. Am. Chem. Soc. 2021, 143, 4921-4927. PMID: 33755457. DOI: 10.1021/jacs.1c01242.

Enantioselective Allylation of Alkenyl Boronates

Novel antimalarial tetrazoles and amides active against the hemoglobin degradation pathway in Plasmodium falciparum.
Lawong A, Gahalawat S, Okombo J, Striepen J, Yeo T, Mok S, Deni I, Bridgford JL, Niederstrasser H, Zhou A, Posner B, Wittlin S, Gamo FJ, Crespo B, Churchyard A, Baum J, Mittal N, Winzeler E, Laleu B, Palmer MJ, Charman SA, Fidock DA, Ready JM, Phillips MA. J Med Chem. 2021 Mar 11;64(5): 2739-2761.

Novel antimalarial tetrazoles and amides

Photocatalytic α‑Alkylation of Amines with Alkyl Halides.
Leng, L.; Ready, J.M. ACS Catalysis 2020, 10, 13196-13201.

Novel antimalarial tetrazoles and amides

Inhibition of 15-PGDH protects mice from immune-mediated bone marrow failure.
Smith, J. N. P.; Otegbeye, F.; Jogasuria, A. P.; Christo, K. F.; Antczak, M. I.; Ready, J. M.; Gerson, S. L.; Markowitz, S. D.; Desai, A. B. Biol. Blood Marrow Transplantation 2020, 26, 1552-1556. PMID: 32422251.

Regioselective, Photocatalytic a-Functionalization of Amines.
Leng L, Fu Y, Liu P, Ready JM, J. Am. Chem. Soc. 2020, 11972.

Regioselective, Photocatalytic a-Functionalization of Amines

Tumor-Activated Benzothiazole Inhibitors of Stearoyl-CoA Desaturase.
Williams NS, Gonzales S, Naidoo J, Rivera-Cancel G, Voruganti S, Mallipeddi P, Theodoropoulos PC, Geboers S, Chen H, Ortiz F, Posner B, Nijhawan D, Ready JM, J. Med. Chem. 2020, 9773.

Tumor-Activated Benzothiazole Inhibitors

An Antiparasitic Compound from the Medicines for Malaria Venture Pathogen Box Promotes Leishmania Tubulin Polymerization.
Ullah, I.; Gahalawat, S.; Booshehri, L; Niederstrasser, H.; Majumdar, S.; Leija, C.; Bradford, J. M.; Hu, B.; Ready, J. M.; Wetzel, D. M. . ACS Infect. Dis. 2020, 6, 2057-2072. PMID: 32686409.

An Antiparasitic Compound from the Medicines for Malaria

Target discovery of selective non-small-cell lung cancer toxins reveals inhibitors of mitochondrial complex I.
Madhusudhan, N; Hu, B.; Mishra, P.; Calva-Moreno, J. F.; Patel, K.; Boriack, R.; Ready, J. M.; Nijhawan. D. ACS Chem. Bio., 2020, 15, 158-170. PMID: 31874028.

Target discovery of selective non-small-cell lung cancer toxins

Chemical Intervention of Influenza Virus mRNA Nuclear Export.
Esparza, M.; Mor. A.; Niederstrasser, H.; White, L.; White, A.; Zhang, K.; Gao, S.; Wang, J.; Liang, J.; Sho, S.; Sakthivel, R.; Sathe, A.; Xing, C.; Muñoz-Moreno, R.; Shay, J.; García-Sastre, S.; Ready, J.; Posner, B.; Fontoura, B. M. PLoS Pathogens, 2020, in press. PMID: 32240278.

Synthetic Studies on the Kigamicins.
Ma, A.J.; Ready, J.M. Org. Lett., 2019, 21, 1148-1151. PMID: 30714741.

Synthetic Studies on the Kigamicins

Selective Synthesis of (+)-Dysoline. 
Coffin, A,; Ready, J.M. Org. Lett., 2019, 21, 648-651. PMID: 30653329.

Selective Synthesis of (+)-Dysoline

Tandem Allylation/1,2-Boronate Rearrangement for the Asymmetric Synthesis of Indolines with Adjacent Quaternary Stereocenters.
Panda S, Ready JM J. Am. Chem. Soc. 2018, 13242.

Tandem Allylation/1,2-Boronate Rearrangement

Inhibiting pyrimidine biosynthesis impairs Ebola virus replication through depletion of nucleoside pools and activation of innate immune responses.
Luthra P, Naidoo J, Pietzsch CA, De S, Khadka S, Anantpadma M, Williams CG, Edwards MR, Davey RA, Bukreyev A, Ready JM, Basler CF. Antiviral Res. 2018; 158:288-302. doi: 10.1016/j.antiviral.2018.08.012.

Discovery of Cytochrome P450 4F11 Activated Inhibitors of Stearoyl Coenzyme A Desaturase.
Winterton SE, Capota E, Wang X, Chen H, Mallipeddi PL, Williams NS, Posner BA, Nijhawan D, Ready JM. J Med Chem. 2018; 61:5199-5221. doi: 10.1021/acs.jmedchem.8b00052. 

Tandem Allylation/1,2-Boronate Rearrangement

A second-generation 15-PGDH inhibitor promotes bone marrow transplant recovery independently of age, transplant dose and granulocyte colony-stimulating factor support.
Desai A, Zhang Y, Park Y, Dawson DM, Larusch GA, Kasturi L, Wald D, Ready JM, Gerson SL, Markowitz SD. Haematologica. 2018; 103:1054-1064. doi: 10.3324/haematol.2017.178376.

A high throughput screen identifies benzoquinoline compounds as inhibitors of Ebola virus replication.
Luthra P, Liang J, Pietzsch CA, Khadka S, Edwards MR, Wei S, De S, Posner B, Bukreyev A, Ready JM, Basler CF. Antiviral Res. 2018; 150:193-201. doi: 10.1016/j.antiviral.2017.12.019.

Total synthesis of the dictyodendrins as an arena to highlight emerging synthetic technologies.
Zhang W, Ready JM. Nat Prod Rep. 2017 34:1010-1034. doi: 10.1039/c7np00018a.

Palladium Catalyzed Asymmetric Three-Component Coupling

Rhodium-Catalyzed Enantioselective Radical Addition of CX4 Reagents to Olefins.
Chen B, Fang C, Liu P, Ready JM. Angew Chem Int Ed Engl. 2017; 56:8780-8784. doi: 10.1002/anie.201704074.

Rhodium-Catalyzed Enantioselective

Prostaglandin dehydrogenase is a target for successful induction of cervical ripening.
Kishore AH, Liang H, Kanchwala M, Xing C, Ganesh T, Akgul Y, Posner B, Ready JM, Markowitz SD, Word RA. Proc Natl Acad Sci U S A. 2017 Aug 1;114(31):E6427-E6436. doi: 10.1073/pnas.1704945114.

Total synthesis of the dictyodendrins as an arena to highlight emerging synthetic technologies.
Zhang W, Ready JM. Nat Prod Rep. 2017 34: 1010-1034. doi: 10.1039/c7np00018a.

Total synthesis of the dictyodendrins

Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair.
Antczak MI, Zhang Y, Wang C, Doran J, Naidoo J, Voruganti S, Williams NS, Markowitz SD, Ready JM J. Med. Chem. 2017, 3979.

Inhibitors of 15-Prostaglandin Dehydrogenase

A Concise Total Synthesis of Dictyodendrins F, H, and I Using Aryl Ynol Ethers as Key Building Blocks.
Zhang W, Ready JM J. Am. Chem. Soc. 2016, 10684.

A Concise Total Synthesis of Dictyodendrins F, H, and I

Zirconcene-mediated carbonylative coupling of Grignard reagents.
Moss M, Han X, Ready JM. Angew Chem Int Ed. 2016 Aug 16;55(34):10017-21. doi: 10.1002/anie.201603133

 

Zirconcene-mediated carbonylative coupling of Grignard reagents

[3 + 2]-Cycloadditions of Azomethine Imines and Ynolates.
Winterton SE, Ready JM. Org Lett. 2016 Jun 3;18(11):2608-11

 

[3 + 2]-Cycloadditions of Azomethine Imines

Discovery of tumor-specific irreversible inhibitors of stearoyl CoA desaturase.
Theodoropoulos PC, Gonzales SS, Winterton SE, Rodriguez-Navas C, McKnight JS, Morlock LK, Hanson JM, Cross B, Owen AE, Duan Y, Moreno JR, Lemoff A, Mirzaei H, Posner BA, Williams NS, Ready JM, Nijhawan D Nat. Chem. Biol. 2016, 218.

Discovery of tumor-specific irreversible inhibitors

Synthesis and Utility of Dihydropyridine Boronic Esters.
Panda S, Coffin A, Nguyen QN, Tantillo DJ, Ready JM. Angew Chem Int Ed Engl. 2016 Feb 5;55(6):2205-9. 

 

Synthesis and Utility of Dihydropyridine Boronic Esters

Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration.
Zhang Y, Desai A, Yang SY, Bae KB, Antczak MI, Fink SP, Tiwari S, Willis JE, Williams NS, Dawson DM, Wald D, Chen WD, Wang Z, Kasturi L, Larusch GA, He L, Cominelli F, Di Martino L, Djuric Z, Milne GL, Chance M, Sanabria J, Dealwis C, Mikkola D, Naidoo J, Wei S, Tai HH, Gerson SL, Ready JM, Posner B, Willson JK, Markowitz SD Science 2015 Jun, 348 6240 aaa2340

TISSUE REGENERATION

Structure Elucidation of Nigricanoside A Through Enantioselective Total Synthesis.
Chen J, Koswatta P, DeBergh JR, Fu P, Pan E, MacMillan JB, Ready JM. Chem Sci. 2015 May 1;6(5):2932-2937. 

 

Structure Elucidation of Nigricanoside A

The P7C3 class of neuroprotective compounds exerts antidepressant efficacy in mice by increasing hippocampal neurogenesis.
Walker AK, Rivera PD, Wang Q, Chuang JC, Tran S, Osborne-Lawrence S, Estill SJ, Starwalt R, Huntington P, Morlock L, Naidoo J, Williams NS, Ready JM, Eisch AJ, Pieper AA, Zigman JM. Mol Psychiatry. 2015 Apr;20(4):500-8.

Protective efficacy of P7C3-S243 in the 6-hydroxydopamine model of Parkinson's disease.
De Jesús-Cortés H, Miller AD, Britt JK, DeMarco AJ, De Jesús-Cortés M, Stuebing E, Naidoo J, Vázquez-Rosa E, Morlock L, Williams NS, Ready JM, Narayanan NS, Pieper AA.
NPJ Parkinsons Dis. 2015;1. pii: 15010.

P7C3 Neuroprotective Chemicals Function by Activating the Rate-Limiting Enzyme in NAD Salvage.
Wang G, Han T, Nijhawan D, Theodoropoulos P, Naidoo J, Yadavalli S, Mirzaei H, Pieper AA, Ready JM, McKnight SL Cell2014 Sep 158 6 1324-34

 

P7C3 Neuroprotective Chemicals

Pharmacologic Rescue of Motor and Sensory Function by the Neuroprotective Compound P7C3 Following Neonatal Nerve Injury.
Kemp SW, Szynkaruk M, Stanoulis KN, Wood MD, Liu EH, Willand MP, Morlock L, Naidoo J, Williams NS, Ready JM, Mangano TJ, Beggs S, Salter MW, Gordon T, Pieper AA, H Borschel G Neuroscience 2014 Oct

P7C3 Neuroprotective Chemicals Block Axonal Degeneration and Preserve Function after Traumatic Brain Injury.
Yin TC, Britt JK, De Jesús-Cortés H, Lu Y, Genova RM, Khan MZ, Voorhees JR, Shao J, Katzman AC, Huntington PJ, Wassink C, McDaniel L, Newell EA, Dutca LM, Naidoo J, Cui H, Bassuk AG, Harper MM, McKnight SL, Ready JM, Pieper AACell Rep 2014 Sep 8 6 1731-40

The Ketene-Surrogate Coupling: Catalytic Conversion of Aryl Iodides into Aryl Ketenes through Ynol Ethers.
Zhang W, Ready JM Angew. Chem. Int. Ed. Engl. 2014 Jun

 

The Ketene-Surrogate Coupling

Discovery of a Neuroprotective Chemical, (S)-N-(3-(3,6-Dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(-)-P7C3-S243], with Improved Druglike Properties.
Naidoo J, De Jesus-Cortes H, Huntington P, Estill S, Morlock LK, Starwalt R, Mangano TJ, Williams NS, Pieper AA, Ready JM J. Med. Chem. 2014 Apr

 

Discovery of a Neuroprotective Chemical

The P7C3 class of neuroprotective compounds exerts antidepressant efficacy in mice by increasing hippocampal neurogenesis.
Walker AK, Rivera PD, Wang Q, Chuang JC, Tran S, Osborne-Lawrence S, Estill SJ, Starwalt R, Huntington P, Morlock L, Naidoo J, Williams NS, Ready JM, Eisch AJ, Pieper AA, Zigman JM Mol. Psychiatry 2014 Apr

In silico derived small molecules bind the filovirus VP35 protein and inhibit its polymerase cofactor activity.
Brown CS, Lee MS, Leung DW, Wang T, Xu W, Luthra P, Anantpadma M, Shabman RS, Melito LM, MacMillan KS, Borek DM, Otwinowski Z, Ramanan P, Stubbs AJ, Peterson DS, Binning JM, Tonelli M, Olson MA, Davey RA, Ready JM, Basler CF, Amarasinghe GK J Mol Biol 2014 May 426 2045-58. 

 

n silico derived small molecules bind the filovirus VP35 protein

Dehydrogenative coupling to enable the enantioselective total synthesis of (-)-simaomicin α.
Wang Y, Wang C, Butler JR, Ready JM. Angew Chem Int Ed Engl. 2013 Oct 52 10796-9

 

Dehydrogenative coupling to enable the enantioselective total synthesis of (-)-simaomicin α.

On the rapid oxidation of allene-containing phosphines.
Cai F, Thangada ND, Pan E, Ready JM. Organometallics 2013 32 5619-22.

 

On the rapid oxidation of allene-containing phosphines

Identification of DNMT1 selective antagonists using a novel scintillation proximity assay.
Kilgore JA, Du X, Melito L, Wei S, Wang C, Chin HG, Posner B, Pradhan S, Ready JM, Williams NS J. Biol. Chem. 2013 May 288 19673-84.

Development of scalable synthesis of P7C3-A20, a potent neuroprotective agent.
Naidoo J, Bemben CJ, Allwin SR, Lian J, Pieper AA, Ready JM. Tetrahedron Lett 2013 54 4429-4432.

 

Development of scalable synthesis of P7C3-A20

Neuroprotective efficacy of aminopropyl carbazoles in a mouse model of Parkinson disease.
De Jesús-Cortés H, Xu P, Drawbridge J, Estill SJ, Huntington P, Tran S, Britt J, Tesla R, Morlock L, Naidoo J, Melito LM, Wang G, Williams NS, Ready JM, McKnight SL, Pieper AA Proc. Natl. Acad. Sci. U.S.A. 2012 Oct 109 42 17010-5

 

Neuroprotective efficacy of aminopropyl carbazoles

Neuroprotective efficacy of aminopropyl carbazoles in a mouse model of amyotrophic lateral sclerosis.
Tesla R, Wolf HP, Xu P, Drawbridge J, Estill SJ, Huntington P, McDaniel L, Knobbe W, Burket A, Tran S, Starwalt R, Morlock L, Naidoo J, Williams NS, Ready JM, McKnight SL, Pieper AA Proc. Natl. Acad. Sci. U.S.A. 2012 Oct 109 42 17016-21

 

Neuroprotective efficacy of aminopropyl carbazoles

Cyclocondensation of amino-propargyl silanes.
Wang Y, Ready JM Org. Lett. 2012 May 14 9 2308-11

 

Cyclocondensation of amino-propargyl silanes

Two-, three-, and four-component coupling to form isoquinolones based on directed metalation.
Antczak M, Ready JM. Chem Sci 2012 3 1450-1454.

 

Two-, three-, and four-component coupling to form isoquinolones

Chiral allene-containing phosphines in asymmetric catalysis.
Cai F, Pu X, Qi X, Lynch V, Radha A, Ready JM. J Am Chem Soc. 2011 Nov 133 18066-9.

 

Chiral allene-containing phosphines in asymmetric catalysis

Enantioselective total synthesis of (-)-kibdelone C.
Butler JR, Wang C, Bian J, Ready JM. J Am Chem Soc 2011 Jul 133 9956-9.

 

Enantioselective total synthesis of (-)-kibdelone C

Titanium-mediated oxidative arylation of homoallylic alcohols.
Lee KS, Ready JM. Angew Chem Int Ed Engl. 2011 Feb 50 2111-4

 

Titanium-mediated oxidative arylation of homoallylic alcohols

Development of proneurogenic, neuroprotective small molecules.
MacMillan KS, Naidoo J, Liang J, Melito L, Williams NS, Morlock L, Huntington PJ, Estill SJ, Longgood J, Becker GL, McKnight SL, Pieper AA, De Brabander JK, Ready JM. J Am Chem Soc. 2011 Feb 133 1428-37

 

Development of proneurogenic, neuroprotective small molecules

Asymmetric synthesis of tertiary benzylic alcohols.
Antczak MI, Cai F, Ready JM. Org Lett. 2011 Jan 13 84-7.

Asymmetric synthesis of tertiary benzylic alcohols