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Our Research

Medicinal Chemistry
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We specialize in medicinal chemistry which is a key part of the discovery and development of new medicines.  We synthesize small organic molecules with drug-like structural features. Working closely with biological collaborators who evaluate these compounds, we modify their structures to achieve optimal biological properties and pharmaceutical potential with the goal of advancing promising "drug candidates" into clinical trials.  Our research home is the Boris Family Medicinal Chemistry Laboratory

Synthetic Methods 
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We develop new reactions and synthetic strategies that enhance the capacity of chemists to produce valuable speciality compounds from simpler inexpensive building blocks.  We focus mainly on three areas: 1) leveraging organosulfur functionalities like sulfoxides and vinyl sulfides as versatile synthetic intermediates, 2) using environmentally benign heterogeneous reagents to simplify reactions and 3) efficiently synthesizing natural products that are of biomedical interest.


Our Publications

A platform for predicting mechanism of action based on bacterial transcriptional responses identifies an unusual DNA gyrase inhibitor

S. French, A. B. Y. Guo, M.J. Ellis, J.P. Deisinger, J.W. Johnson, K.Rachwalski, Z. A. Piquette, T. Lluka, M. Zary, S. Gamage, J. Magolan, E.D. Brown.

Cell Reports 2024, 43(4), 114053

Magolan Lab members Jarrod Johnson and Zoe Piquette made synthetic chemistry contributions to this collaborative investigation led by the lab of Prof. Eric Brown.

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Allosteric inhibition of tRNA synthetase Gln4 by N-pyrimidinyl-β-thiophenylacrylamides exerts highly selective antifungal activity

E. Puumala, D. Sychantha, E.Lach, S. Reeves, S. Nabeela, M. Fogal, A.K. Nigam, J. W. Johnson, A. Aspuru-Guzik, R.S. Shapiro, P. Uppuluri, S. Kalyaanamoorthy, J.Magolan, L. Whitesell, N. Robbins, G. D. Wright, L. E. Cowen.
Cell Chem. Biol. 2024, 31(4), 760-775.e17

Magolan Lab member Elizabeth Lach and Jarrod Johnson made synthetic chemistry contributions to this collaborative investigation led by the lab of Prof. Leah Cowen at the University of Toronto.

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Bioactivity of the Cannabigerol Cannabinoid and its Analogues – the role of 3-Dimensional Conformation 

M. Salha, H. Adenusi, J. Dupuis, E. Bodo, B. Botta, I. Mckenzie, R. Yada, D. Farrar, J. Magolan, K. V. Tian, G. Chass. 
Org. Biomol. Chem. 2023, 21, 4683-4693.

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Deep learning-guided discovery of an antibiotic targeting Acinetobacter baumannii

G. Liu, D. B. Catacutan, K. Rathod, K. Swanson, W. Jin, J. C. Mohammed, A. Chiappino-Pepe, S. A. Syed, M. Fragis, K. Rachwalski, J. Magolan, M. G. Surette, B. K. Coombes, T. Jaakkola, R. Barzilay, J. J. Collins, J. M. Stokes *

Nat. Chem. Biol. 2023 (ASAP, online May 25, 2023)

Magolan Lab member Meghan Fragis made synthetic chemistry contributions to this collaborative investigation led by the lab of Prof. Jonathan Stokes.

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Genetic and Chemical Screening Reveals Targets and Compounds to Potentiate Gram-Positive Antibiotics against Gram-Negative Bacteria

K. Klobucar, E. Jardine, M. A. Farha, M. R. MacKinnon, M. Fragis, B. Nkonge, T. Bhando, L. Borrillo, C. N. Tsai, J. W. Johnson, B. K. Coombes, J. Magolan, E. D. Brown*

ACS Infect. Dis. 2022 8(10), 2187-2197

Magolan Lab members Marc MacKinnon, Meghan Fragis, Brenda Nkonge, Louis Borrillo, and Jarrod Johnson  made synthetic chemistry contributions to this collaborative investigation led the lab of Prof. Eric Brown.

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QSAR Models Reveal New EPAC-Selective Allosteric Modulators

H. Mohamed, H. Shao, M. Akimoto, P. Darveau, M. R. MacKinnon, J. Magolan, G. Melacini*

RSC Chem. Biol. 2022 ,3, 1230-1239

Magolan Lab members Patrick Darveau and Marc MacKinnon made synthetic chemistry contributions to this collaborative investigation led the lab of Prof. Giuseppe Melacini


Use of Vinyl Sulfides in Fischer Indole Reactions

P. Pal, M. Fragis, S. Dharavath, J. W. Johnson, J. Magolan

Synthesis. 2022, 54, 4917-4931

Highlight on Organic Chemistry Portal.


Caffeine blocks SREBP2-induced hepatic PCSK9 expression to enhance LDLR-mediated cholesterol clearance

P. F. Lebeau, J. H. Byun, K. Platko, P. Saliba, M. Sguazzin, M. E. MacDonald, G. Paré, G. R. Steinberg, L. J. Janssen, S. A. Igdoura, M. A. Tarnopolsky, S. R. W. Chen, N. G. Seidah, J. Magolan, R. C. Austin

Nat. Commun. 2022, 13, 770

Magolan Lab members Paul Saliba and Matthew Sguazzin made synthetic chemistry contributions to this collaborative investigation led the lab of Prof. Richard Austin


Hexafluoroisopropyl Sulfamate

J. W. JohnsonM. A. SguazzinJ Magolan

Encyclopedia of Reagents for Organic Synthesis 2022 (online Jan 23, 2022)


Antibacterial Activity of Metergoline Analogues: Revisiting the Ergot Alkaloid Scaffold for Antibiotic Discovery

J. W. Johnson, M. J. Ellis, Z. A. Piquette, C. MacNair, L. Carafrae, T. Bhando, N. E. Ritchie, P. Saliba, E. D. Brown, J. Magolan

ACS Med. Chem. Lett. 2022 (online Jan 21, 2022)


Exploration of BAY 11-7082 as a novel antibiotic

V. E. Coles, P. Darveau, X. Zhang, H. Harvey, B. D. Henriksbo, A. Yang,  J. D. Schertzer, J. Magolan, L. L. Burrows

ACS Infect. Dis. 2022, 8(1), 170-182.
(first published online December 3, 2021)

Magolan Lab members Patrick Darveau and Dr. Xiong Zhang made synthetic chemistry contributions to this collaborative investigation led by Victoria Coles and the lab of Prof. Lori Burrows.


Bibenzyl synthesis in Cannabis sativa L

K. BoddingtonE. SoubeyrandK. Van GelderJ. A. CasarettoC. PerrinT. J.B. ForresterC. ParryM. S.Al-Abdul-WahidN. G. JentschJ. MagolanG. G. BozzoM. S. KimberS. J. RothsteinT. A. Akhtar

The Plant Journal, 2022, 109(3), 693-707
(first published online November 17, 2021)

Magolan Lab member Dr. Nicholas Jentsch made synthetic chemistry contributions to this collaborative investigation led by the lab of Prof. Tariq Akhtar at the University of Guelph.

2021 publications

Aldehyde to Ketone Homologation Enabled by Improved Access to Thioalkyl Phosphonium Salts

M. Fragis, J. L. Deobald, S. Dharavath, J. Scott, J. Magolan

Org. Lett. 2021, 23(12), 4548-4452

This article received an Editor's Choice Award from Organic Letters and was featured in Prof. Taber's Org. Chem. Highlights: "Carbon-Carbon Bond Construction", Jan. 31, 2022 (link)

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Chemical Screen for Vancomycin Antagonism Uncovers Probes of the Gram-Negative Outer Membrane

K. Klobucar, J-P Côté, S. French, L. Borrillo, A.B.Y. Guo, M. H. Serrano-Wu, K.K. Lee, B.K. Hubbard, J.W. Johnson, J.L. Gaulin, J. Magolan, D.T. Hung, E.D. Brown 

ACS Chem. Bio. 2021, 16(5), 929-942

Magolan Lab members Louis Borrillo and Dr. Jarrod Johnson made synthetic chemistry contributions to this collaborative investigation led by the lab of Prof. Eric Brown.

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Targeting SUMOylation dependency in human cancer stem cells through a unique SAE2 motif revealed by chemical genomics

Y.D. Benoit, R.R. Mitchell, W. Wang, L. Orlando, A.L. Boyd, B. Tanasijevic, L. Aslostovar, Z. Shapovalova, M. Doyle, C.J. Bergin, K. Vojnits, F.L. Casado, J.D. Lu, D.P. Porras, J.L. Garcı´a-Rodriguez, J. Russell, A. Zouggar, A.N. Masibag, C. Caba, K. Koteva, L.K. Kinthada, J.S. Patel, S.N. Andres, J. Magolan, T.J. Collins, G.D. Wright, M. Bhatia.

Cell Chem. Biol. 2021 28, 1-13

Magolan Lab member Dr. Lakshmana Kinthada made synthetic chemistry contributions to this collaborative investigation led by the lab of Prof. Mick Bhatia.

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Hexafluoroisopropyl Sulfamate: A Useful Reagent for the Synthesis of Sulfamates and Sulfamides

M. Sguazzin, J. Johnson, J. Magolan

Org. Lett  2021, 23(9), 3373-3378

DOI: 10.1021/acs.orglett.1c00855

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2020 Publications

Efficient Synthesis of Cannabigerol, Grifolin, and Piperogalin via Alumina-Promoted Allylation

N. G. Jentsch, X. Zhang, J. Magolan

J. Nat. Prod.  2020, 83(9), 2587-2591

DOI: 10.1021/acs.jnatprod.0c00131

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Genetic and chemical screening in human blood serum reveals unique antibacterial targets and compounds against Klebsiella pneumoniae

B. S. Weber, A. M. De Jong, A. B. Y. Guo, S. Dharavath, S. French, A. A. Fiebig-Comyn, B. K. Coombes, J. Magolan, E. D. Brown

Cell Reports 2020, 32(3), 107927

DOI: 10.1016/j.celrep.2020.107927

Magolan Lab member Dr. Srinivas Dharavath made synthetic chemistry contributions to this collaborative investigation led by the lab of Prof. Eric Brown.

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Targeting two-component systems uncovers a small molecule inhibitor of Salmonella virulence.

C. N. Tsai, C. R. MacNair, M. P. T. Cao, J. N. Perry, J. Magolan, E. D. Brown, B. K. Coombes

Cell Chem. Bio. 2020, 27(7), 793-805

DOI: 10.1016/j.chembiol.2020.04.005

Magolan Lab member Dr. My Cao made synthetic chemistry contributions to this collaborative investigation led by the lab of Prof. Brian Coombes.  


Mechanism of Action of an EPAC1-Selective Competitive Partial Agonist

H. Shao, H. Mohamed, S. Boulton, J. Huang, P. Wang, H. Chen, J. Zhou, U. Luchowska-Stańska, N. Jentsch, A. Armstrong, J. Magolan, Y. Stephen, G. Melacini

J. Med. Chem. 2020, 63(9), 4762-4775

DOI: 10.1021/acs.jmedchem.9b02151

Magolan Lab members Dr. Nick Jentsch and Alison Armstrong made synthetic chemistry contributions to this collaborative protein NMR-based investigation led by the lab of Prof. Giuseppe Melacini.  

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Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge Verongida rigida

A. J. Kochanowska-Karamyan, H. C. Araujo, X. Zhang, A. El-Alfy, P. Carvalho, M. A. Avery, S. Holmbo, J. Magolan, M. T. Hamann

J. Nat. Prod. 202083(4), 1902-1098

DOI: 10.1021/acs.jnatprod.9b01107

Magolan Lab members Hugo Araujo, Xiong Zhang, and Steven Holmbo completed the first gram scale total synthesis of veranamine as part of this international collaboration co-led by Dr. Magolan and Dr. Hamann.  

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Uncovering the hidden antibiotic potential of Cannabis 

M. A. Farha, O. M. El-Halfawy, R.T. Gale, C. R. MacNair, L. A. Carfrae, X. Zhang, N. G. Jentsch, J. Magolan, E. D. Brown

ACS Infec. Dis. 2020, 6(3), 338-346

DOI: 10.1021/acsinfecdis.9b00419

Magolan Lab members Xiong Zhang and Dr. Nick Jentsch made synthetic chemistry contributions to this collaborative investigation led by Prof. Eric Brown's lab.  

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2019 and earlier - Pubications

Alkylation of indoles with α,β-unsaturated ketones using alumina in hexanes

Zhang, X., Jones-Mensah, E., Deobald J., Magolan J.

Advanced Synthesis and Catalysis 2019, 361, 5548-5551.

DOI 10.1002/adsc.201901037


A macrophage-based screen identifies antibacterial compounds selective for intracellular Salmonella Typhimurium

Ellis, M.J., Tsai, C.N., Johnson, J.W., French, S., Elhenawy, W., Porwollik, S., Andrews-Polymenis, H., McClelland, M., Magolan, J., Coombes, B.K., Brown, E.D

Nature Communications 2019, 10(1), 197
DOI 10.1038/s41467-018-08190-x

Magolan Lab member Dr. Jarrod Johnson made synthetic chemistry contributions to this collaborative investigation led by the labs of Prof. Eric Brown and Prof. Brian Coombes. 


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One-pot carbonyl reduction and carbonate formation using sodium borohydride in dialkyl carbonate solvents 

Osumah, A., Magolan J., Waynant, K.

Tetrahedron Letters. 2019, 60(44), 151203

DOI 10.1016/j.tetlet.2019.151203

Magolan Lab research done at the University of Idaho (2010-2017)

Biaryl Ketones via Suzuki-Miyaura Cross-Coupling of Organotrifluoroborates and Acid Chlorides. 

Frobes, A. M.; Meier, G. P.; Jones-Mensah, E.; Magolan J.  

Eur. J. Org. Chem. 2016, 17, 2983-2987.

DOI: 10.1002/ejoc.201600199


Dimethylsulfoxide as a Synthon in Organic Chemistry.  

Jones-Mensah, E.; Karki, M.; Magolan, J.

Synthesis 2016, 48(10), 1421-1436.

DOI: 10.1055/s-0035-1560429


Cerium-Free Luche Reduction Directed by Rehydrated Alumina. 

Jones-Mensah, E.; Nickerson, L. A.; Deobald, J. L.; Ertel, A. B.; Knox, H. L.; Magolan. J.

Tetrahedron 2016, 72(26) 3748-3753.


Evaluation of Synthetic Coumarins for Antiausterity Cytotoxicity against Pancreatic Cancers.  

Farley, C. M.; Dibwe, D.F.; Ueda, J.; Hall, E.A.; Awale, S. Magolan, J.

Bioorg. Chem. Med. Lett. 2016, 26(5), 1471-1474.


Bromination of Olefins with HBr and DMSO. 

Karki, M.; Magolan, J.

J. Org. Chem. 2015, 80(7) 3701-3707.
DOI: 10.1021/acs.joc.5b00211


Aryl methyl sulfides via SNAr using DMSO as the source of the thiomethyl moiety. 

Jones-Mensah, E.; Magolan, J.  

Tetrahedron Lett. 2014, 55(38), 5323-5326.
DOI: 10.1016/j.tetlet.2014.07.058


Dehydroaromatization with V2O5. 

Karki, M.; Araujo, H. C.; Magolan, J.

Synlett 2013, 24(13), 1675-1678.
DOI: 10.1055/s-0033-133927


Combined Pd/C and Montmorillonite Catalysis for Efficient One-Pot Synthesis of Benzimidazoles. 

Weires, N.A.; Boster, J.; Magolan, J. 

Eur. J. Org. Chem. 201233, 6508-6512
DOI: 10.1002/ejoc.201201101

highlighted: Snieckus V.; Singh S.P. SYNFACTS 2013, 9(3), 254

Publications from Dr. Magolan's graduate and postdoctoral research

Tilly, D.; Magolan, J.; Mortier, J.

Directed Remote Aromatic Metalations: Mechanisms and Driving Forces.  

Chemistry a European Journal 2012, 18(13), 3804-3820. (link)

Magolan, J.; Adams, N.B.P.; Onozuka, H.; Esumi, H.; Hugerford, N.L.; Coster, M.J.  

Synthesis and biological evaluation of analogues of the natural product angelmarin for anti-pancreatic cancer activity. 

ChemMedChem 2012, 7(5), 766-770. (link)

Magolan, J.; Coster, M.J.

Targeting the resistance of pancreatic cancer cells to nutrient deprivation: anti-austerity compounds. 

Current Drug Delivery 2010, 7(5), 355-369. (link)

Magolan, J.; Coster M.J.

Total Synthesis of (+)-Angelmarin. 

Journal of Organic Chemistry 2009, 74(14), 5083–5086. (link)

Magolan, J.; Carson, C.; Kerr, M.A.

Total Synthesis of (±)-Mersicarpine. 

Organic Letters 2008, 10(7), 1437-1440. (link)

Li, L.; Jones, C.D.; Magolan, J.;  Lemieux, R.P.

Siloxane-terminated phenylpyrimidine liquid hosts.

Journal of Materials Chemistry 2007, 17, 2313-2319. (link)

Magolan, J.; Kerr, M.A.  

Expanding the Scope of Mn(OAc)3-Mediated Cyclizations: Synthesis of the Tetracyclic Core of Tronocarpine. 

Organic Letters 2006, 8(17), 3777-3779. (Link)

England, D.B.; Magolan, J.; Kerr, M.A.

Synthesis of the Western Half of the Lolicines and the Lolitrems. 

Organic Letters 2006, 8(11), 2209-2212. (link)

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