Yeng-Jeng Shaw, PhD, is a Researcher/Scientist at the University of Arizona. His major role in PharmTox is to provide strategic plans to implement early drug discovery projects. During his career, he has worked in pharmaceutical and biotechnology as a medicinal chemist and has coordinated or been part of chemistry efforts on multiple drug-discovery projects across a variety of disease areas, including cardiovascular, neurodegenerative, oncology, pathological pain, rare disease, and autoimmune disease.
BS, Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan
MS, Organic Chemistry, National Taiwan University, Taipei, Taiwan
PhD, Medicinal Chemistry, The Ohio State University, Columbus, OH
Postdoctoral, Medicinal Chemistry, University of Arizona, Tucson, AZ
1. Clinical drug as a molecular template for anticancer agent development
1. J. Zhu, J.-W. Huang, P.-H. Tseng, Y.-T. Yang, J. Fowble, C.-W. Shiau, Y.-J. Shaw, S.K. Kulp, C.-S. Chen*.” From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors”. Cancer Res. 2004, 64(12), 4309-4318.
2. Y.-J. Shaw, Y.-T. Yang, J.B. Garrison, N. Kyprianou, C.-S. Chen*. “Pharmacological exploitation of the alpha1-adrenoreceptor antagonist doxazosin to develop a novel class of antitumor agents that block intracellular protein kinase B/Akt activation.” J. Med. Chem. 2004, 47(18), 4453-4462.
3. C.S. Chen, Y.-J. Shaw “Amino-quinazoline derivatives as antitumor agents.” 2008, WO 2006/002088 A3.
4. J.B. Garrison, Y.-J. Shaw, C.-S. Chen, N. Kyprianou* “Novel quinazoline-based compounds impair prostate tumorigenesis by targeting tumor vascularity.” Cancer Res. 2007, 67(23), 11344-11352.
5. H.-L. Chen, C.-Y. Chang, H.-T. Lee, H.-H. Lin, P.-J. Lu, C.-N. Yang, C.-W. Shiau, A.Y. Shaw* “Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation.” Bioorg. Med. Chem. 2009, 17(20), 7239-7247.
6. A.Y. Shaw *, C.-Y. Chang, M.-Y. Hsu, P.-J. Lu, C.-N, Yang, H.-L. Chen, C.-W. Lo, C.-W. Shiau, M.-K. Chern. “Synthesis and structure-activity relationship study of 8-hydroxyquinoline-derived Mannich bases as anticancer agents.” Eur. J. Med. Chem. 2010, 45(7), 2860-2867.
2. Developed proof-of-concept DYRK1A inhibitors for treating Alzheimer’s disease
1. C. Branca, D. Shaw, R. Belfiore, V. Gokhale, A. Y. Shaw, C. Foley, B. Smith, C. Hulme, T. Dunckley, B. Meechoovet, A. Caccamo, S. Oddo " Dyrk1 inhibition improves Alzheimer's disease-like pathology" Aging Cell 2017,16,1146 - 1154.
2. C. Hulme, T. Dunckley, A. Y. Shaw "Small Molecule Inhibitors of DYRK1A and Uses Thereof". Issued Mar 9, 2017 WO2017/040993A1; PCT/US2016/050198.
3. R. Velazquez, B. Meechoovet, A. Ow, C. Foley, A. Shaw, B. Smith, S. Oddo, C. Hulme, T. Dunckley “Chronic Dyrk1 inhibition delays the onset of AD-like pathology in 3xTg-AD mice.” Mol. Neurobiol. 2019, 56, 8364-8375.
3. Discovery of novel androgen receptor inhibitors
1. A. Y. Shaw, V. Gokhale, S. P. Stratton, C. Hulme. "Promising, early-stage novel androgen receptor antagonists in head–head comparisons with enzalutamide and bicalutamide." Abstract of Papers #2524, AACR Meeting Abstracts, San Diego, CA, April 5-9, 2014.
2. C. Hulme, Y.-J. Shaw, V. Gokhale. “Preparation and use of small molecule inhibitors of androgen receptor (AR) activity and /or expression”, 2020, WO 2020123670 A1 20200618.
4. Characterization of oxazole-based antitumor agents targeting pancreatic cancer
1. M.C. Henderson, Y.-J. Shaw, H. Wang, H. Han, L.H. Hurley, G. Flynn, R.T. Dorr, D.D. Von Hoff* “UA62784, a novel inhibitor of centromere protein E kinesin-like protein.” Mol. Cancer Ther. 2009,
2. R. Dorr, G. Flynn, H. Han, L. Hurley, A. Y. Shaw "Compounds, pharmaceutical compositions and methods of use of 2-aryl pyridylazoles" 2015, US8987309.’
3. A.Y. Shaw, M.C. Henderson, G. Flynn, B. Smulitis, H. Han, S.P. Stratton, S. H.-H. Chow, L.H. Hurley, R.T. Dorr* “Characterization of novel diaryl oxazole-based compounds as potential agents to treat pancreatic cancer.” J. Pharmacol. Exp. Ther. 2009, 331(2), 636-647.
5. Applications of multicomponent reactions and development of oxidative amidation
1. Z. Xu, J. Dietrich, A.Y. Shaw, C. Hulme* “Two step syntheses of fused quinoxaline-benzodiazepines and bis-benzodiazepines.” Tetrahedron Lett. 2010, 51(34), 4566-4569.
2. Z. Xu, A.Y. Shaw, J. Dietrich, A.P. Cappelli, G. Nichol, C. Hulme* “Facile, novel two-step syntheses of benzimidazoles, bis-benzimidazoles, and bis-benzimidazole-dihydroquinoxalines.” Mol. Divers. 2012,
3. Z. Xu, A.Y. Shaw, G. Nichol, A.P. Cappelli, C. Hulme* “Applications of ortho-phenylisonitrile and ortho- N-Boc aniline for the two-step preparation of novel bis-heterocyclic chemotypes.” Mol. Divers. 2012,
4. A.Y. Shaw, J. A. McLaren, G. S. Nichol, C. Hulme* “Hydrazine-mediated cyclization of Ugi products to synthesize novel 3-hydroxypyrazoles.” Tetrahedron Lett. 2012, 53, 2592-2594.
5. A.Y. Shaw, Z. Xu, C. Hulme* “Ugi/Robinson–Gabriel reactions directed toward the synthesis of 2,4,5-
trisubstituted oxazoles.” Tetrahedron Lett. 2012, 53, 1998-2000.
6. A.Y. Shaw, F. Medda, C. Hulme* “Facile and rapid route for the synthesis of novel conformationally
constrained norstatine analogs via PADAM-cyclization methodology.” Tetrahedron Lett. 2012, 53,
7. A.Y. Shaw, C. R. Denning, C. Hulme* “Selenium dioxide-mediated synthesis of alpha--ketoamides from
arylglyoxals and secondary amines.” Tetrahedron Lett. 2012, 53, 4151-4153.
8. A.Y. Shaw, C. R. Denning, C. Hulme* “One-pot two-step synthesis of quinoxalinones and diazepinones via a tandem oxidative amidation/deprotection/cyclization”, Synthesis 2013, 45, 459-462.
9. C. Foley, A.Y. Shaw, C. Hulme "Two-step route to diverse N-functionalized peptidomimetic-like isatins
through an oxidation/intramolecular oxidative amidation cascade of Ugi-azide and Ugi three-component reaction products " Org. Lett 2016, 18,4904 - 4907.
10. J. W. Collet, C. Foley, A. Y. Shaw, R. V. A. Orru, E. Ruijter, C. Hulme " Copper(I) catalyzed oxidative
hydrolysis of Ugi 3-component and Ugi-azide reaction products towards α-ketoamides and α- ketotetrazoles" Org. Biol. Chem. 2017,15, 6132 – 6135.
11. C. Foley, A.Y. Shaw, C. Hulme "Oxidative deaminations and deisatinylations of Ugi-azide and Ugi-3CR products: A two-step MCR-oxidation protocol toward functionalized α-ketoamides and α-ketotetrazoles" Org. Lett. 2017, 19,2238 - 2241.
12. C. Foley, A.Y. Shaw, C. Hulme "Aza-Riley oxidation of Ugi-azide and Ugi-3CR products toward vicinal tricarbonyl amides: Two-step MCR-oxidation methodology accessing functionalized α,β-diketoamides and α,β-diketotetrazoles" Org. Lett. 2018, 20,1275 - 1278.
13. C.E. Bell, A.Y. Shaw, F. De Moliner, C. Hulme "MCRs reshaped into a switchable microwave-assisted protocol toward 5-aminoimidazoles and dihydrotriazines" Tetrahedron 2014, 70, 54-59.
6. Other synthetic organic and medicinal chemistry research during academic appointment
A.Y. Shaw *, Y.-R. Chen, C.-H. Tsai “Microwave-assisted base-catalyzed cyclization and nucleophilic substitution of O-azidobenzanilides to synthesize 1,2-disubstituted indazol-3-ones.” Synth. Comm. 2009, 39(15), 2647-2663.
A.Y. Shaw *, H.-H. Liau, P.-J. Lu, C.-N. Yang, C.-H. Lee, J.-Y. Chen, Z. Xu, G. Flynn “3,5-Diaryl-1H-pyrazole as a molecular scaffold for the synthesis of apoptosis-inducing agents.” Bioorg. Med. Chem. 2010, 18(9), 3270-3278.
A.Y. Shaw *, C.-Y. Chang, H.-H. Liau, P.-J. Lu, H.-L. C.-N. Chen, H.-Y. Yang “Synthesis of 2-styrylchromones as a novel class of antiproliferative agents targeting carcinoma cells.” Eur. J. Med. Chem. 2009, 44(6), 2552-2562.
C. Lin, P.-J. Lu, C.-N. Yang, C. Hulme, A.Y. Shaw * “Structure-activity relationship study of growth inhibitory 2-styrylchromones against carcinoma cells” Med. Chem. Res. 2013, 22, 2385-2394.
Emily Lee, P.-J. Lu, A.Y. Shaw * "Synthesis and antiproliferative evaluation of 2'-arenesulfonyloxy-5-benzylidene -thiazolidine-2,4-diones". J. Het. Chem. 2012, 49, 792-798.
Y.-H Chen, P.-J. Lu, C. Hulme, A.Y. Shaw * “Synthesis of kojic acid-derived copper-chelating apoptosis inducing agents.” Med. Chem. Res. 2013, 22(2), 995-1003.
Y.-H Chen, P.-J. Lu, C. Hulme, A.Y. Shaw * “Synthesis of (E)‐5‐Methoxy‐2‐styryl‐4‐pyrones as Potent Growth‐Inhibitory Agents Against Hepatocellular Carcinoma Cells” J. Het. Chem. 2014, 51, 56-61.
M.-Y. Hsu, J. Dietrich, C. Hulme, A.Y. Shaw * Synthesis of di- and tri-substituted imidazole-4-carboxylates via PBu3-mediated [3+2] cycloaddition.” Synth. Comm. 2013, 43, 1538-1543.
Y.-S. Lin, A.Y. Shaw, S.-G. Wang, C.-C. Hsu, I.-W. Teng, M.-J. Tseng, T. H.-M. Huang, C.-S. Chen, S.-H. Hsiao, Y.-W. Leu* “Identification of novel DNA methylation inhibitors via a two-component reporter gene system.” J. Biomed. Sci. 2011, 18:3.
C.S. Chen, A.Y. Shaw, Y.-W. Leu, S.-H. Hsiao “Novel DNA methylation inhibitors for cancer treatment and prevention.” 2012, #WO2012087889.