Publications

University of Connecticut

Research Articles

1. Maschinot, C. A. and Hadden, M. K. Synthesis and evaluation of vitamin D3 analogus with C-11 modifications as inhibitors of hedgehog signaling. Bioorg. Med. Chem. Lett. 2017, In Press.

 

2. Sail, V.; Rizzo, A. A.; Chatterjee, N.; Dash, R. C.; Ozen, Z.; Walker, G. C.; Korzhnev, D. M.; Hadden, M. K. Identification of small molecule translesion synthesis inhibitors that target the Rev1-CT/RIR protein-protein interaction. ACS Chem. Biol. 2017, 12, 1903-1912.

 

3. Dash, R. C.; Maschinot, C. M.; Hadden, M. K. A molecular dynamics approach to identify an oxysterol-based hedgehog pathway inhibitor. Biochim. Biophys. Acta 2017, 1861, 168-177.

graphical-abstract

 

4. Pace, J. R.; DeBerardinis, A. M.; Sail, V.; Tacheva-Grigorova, S. K.; Chan, K. A.; Tran, R.; Raccuia, D. S.; Wechsler-Reya, R.; Hadden, M. K. Repurposing the clinically efficacious anti-fungal agent itraconazole as an anti-cancer chemotherapeutic. J. Med. Chem. 2016, 59, 3635-3649.

JP ITZ J Med Chem

 

***5. Maschinot, C. A.; Corman, A. R.; DeBerardinis, A. M.; Hadden, M. K. Synthesis and evaluation of osteogenic oxysterols as hedgehog pathway activators. ChemMedChem 2016, 11, 679-686.TOC Graphical Abstract

Final Cover Image

***Featured article – “The front cover picture shows how the stereochemical orientation of the C-21 methyl group in the oxysterol (OHC) scaffold can determine whether the OHC serves as an agonist of the hedgehog (Hh) signaling pathway (hedgehog image by Marina Maslennikova, iStockphoto). The natural configuration of the C-21 methyl is R, which is shown here in the structure of 23(S)-hydroxycholesterol (4, right), a potent, synthetic agonist of Hh signaling with the ability to promote osteogenic differentiation. Inversion of the C-21 methyl to the S configuration (16, left) completely abolished its ability to activate Hh signaling. These results provide essential structural insight for the future development of small molecule OHCs as Hh pathway agonists.”

 

6. DeBerardinis, A. M.; Raccuia, D. S.; Maschinot, C. A.; Thompson, E.; Hadden, M. K. Vitamin D3 analogues that contain modified A- and seco-B-rings as hedgehog pathway inhibitors. Euro. J. Med. Chem. 2015, 93, 156-171.

Graphical Abstract

 

7. Banerjee, U.; DeBerardinis, A. M.; Hadden, M. K. Design, synthesis, and evaluation of hybrid vitamin D3 side chain analogues as hedgehog pathway inhibitors. Bioorg. Med. Chem. 2015, 23, 548-555.

Graphical Abstract

 

8. DeBerardinis, A. M.; Madden, D. J.; Banerjee, U.; Sail, V.; Raccuia, D. S.; De Carlo, D.; Lemieux, S. M.; Meares, A.; Hadden, M. K. Structure-activity relationships for vitamin D3-based aromatic A-ring analogues as hedgehog pathway inhibitors. J. Med. Chem. 2014, 57, 3724-3736.

Graphical Abstract Aromatic A-Ring JMC

 

9. DeBerardinis, A. M.; Lemieux, S. M.; Hadden, M. K. Analogues of the Inhoffen-Lythgoe diol with anti-proliferative activity. Bioorg. Med. Chem. Lett. 2013, 23, 5367-5370.

Graphical Abstract IL Diol

 

10. DeBerardinis, A. M.; Banerjee, U.; Hadden, M. K. Identification of vitamin D3-based hedgehog pathway inhibitors that incorporate an aromatic A-ring isostere. ACS Med. Chem. Lett. 2013, 4, 590-595.

Graphical Abstract ACSMCL Initial Aromatic A-Ring

 

11. Sail, V.; Hadden, M. K. Identification of small molecule Hes1 modulators as potential anti-cancer chemotherapeutics. Chem. Biol. & Drug Design 2013, 81, 334-342.

Graphical Abstract Hes1

 

12. Oblak, E. Z.; Bolstad, E. S. D.; Ononye, S. N.; Priestley, N. D.; Hadden, M. K.; Wright, D. L. The furan route to tropolones: probing the antiprolierative effects of β-thujaplicin analogs. Org. Biomol. Chem. 2012, 10, 8597-8604.

GA

 

13. Viswanathan, K.; Ononye, S. N.; Cooper, H. D.; Hadden, M. K.; Anderson, A. C.; Wright, D. L. Viridin analogs derived from steroidal building blocks. Bioorg. Med. Chem. Lett. 2012, 22, 6919-6922.

rsz_kishore_ga_2012

 

14. Corman, A.; DeBerardinis, A.; Hadden, M. K. Structure-activity relationships for side chain oxysterol agonists of hedgehog signaling. ACS Med. Chem. Lett. 2012, 3, 828-833.

AC and AD ACS MCL 2012

 

15. DeBerardinis, A.; Banerjee, U.; Miller, M.; Lemieux, S.; Hadden, M. K. Probing the structural requirements for vitamin D3 inhibition of hedgehog signaling. Bioorg. Med. Chem. Lett. 2012, 22, 4859-4863.

Truncated VD3 BMCL 2012

 

16. Banerjee, U.; Ghosh, M.; Hadden, M. K. Evaluation of vitamin D3 A-ring analogues as hedgehog pathway inhibitors. Bioorg. Med. Chem. Lett. 2012, 22, 1330-1334.

UB VD3 BMCL 2012

 

Reviews and Book Chapters

1. Teske, K. A. and Hadden, M. K. Methyllysine binding domains: Structural insight and small molecule probe development. Euro. J. Med. Chem. 2017, 136, 14-35.

1. Korzhnev, D. M. and Hadden, M. K. Targeting the translesion synthesis pathway for the development of anti-cancer chemotherapeutics. J. Med. Chem. 2016, 59, 9321-9336.

New TOC Graphic

2. Maschinot, C. A.; Pace, J.; Hadden, M. K. Synthetic small molecule inhibitors of Hh signaling as anti-cancer chemotherapeutics. Curr. Med. Chem. 2015, 22, 4033-4057.

3. Hadden, M. K. Targeting GLI proteins in human cancer by small molecules (WO2014116651 A1): a patent evaluation. Exp. Opin. Ther. Patents 2015, 25(5).

4. Banerjee, U.; Hadden, M. K. Recent advances in the design of hedgehog pathway inhibitors for the treatment of malignancies. Exp. Opin. Drug Discov. 2014, 9, 751-771.

5. Hadden, M. K. Hedgehog pathway agonism: Therapeutic potential and small molecule development. ChemMedChem 2014, 9, 27-37.

6. Lemieux, S.; Hadden, M. K. Targeting the fibroblast growth factor receptors for the treatment of cancer. Anti-Cancer Agents Med. Chem. 2013, 13, 748-761.

7. Hadden, M. K. Hedgehog pathway inhibitors: a patent review (2009-present). Exp. Opin. Ther. Patents 2013, 23, 345-361.

8. Sail, V.; Hadden, M. K. Notch pathway modulators as anti-cancer chemotherapeutics. Ann. Rep. Med. Chem. Ed. Manoj Desai. Vol. 47, ARMC, UK: Academic Press, 2012, 267-280.

9. DeCarlo, D.; Hadden, M. K. Oncoepigenomics: Making histone-lysine methylation count. Euro. J. Med. Chem. 2012, 56, 179-194.

 

University of Kansas

1. Blagg, B. S. J.; Hadden, M. K. “Hsp90 Inhibitors.” Burger’s Medicinal Chemistry, Drug Discovery and Development. Eds. Donald Abraham and David Rotella, 7th ed. Vol 6. 2010.

2. Hadden, M. K.; Blagg, B. S. J. Synthesis and evaluation of radamide analogues, a chimera of radicicol and geldanamycin. J. Org. Chem. 2009, 74, 4697-4704.

3. Hadden, M. K.; Hill, S.; Davenport, J.; Matts, R. L.; Blagg, B. S. J. Synthesis and evaluation of Hsp90 inhibitors that contain the 1,4-naphthoquinone scaffold. Bioorg. Med. Chem. 2009, 17, 634-640.

4. Hadden, M. K.; Blagg, B. S. J. Dimeric approaches to anti-cancer chemotherapeutics. Anti-Cancer Agents Med. Chem. 2008, 8, 807-816.

5. Tash, J. S.; Chakrasali, R.; Jakkaraj, S. R.; Hughes, J.; Smith, S. K.; Hornbaker, K.; Heckert, L. L.; Ozturk, S. B.; Hadden, M. K.; Kinzy, T. G.; Blagg, B. S. J.; Georg, G. I. Gamendazole, an orally active indazole carboxylic acid male contraceptive agent, targets HSP-90, eEF1A, and stimulates IL-1 transcription in Sertoli cells. Biol. Reprod. 2008, 78, 1139-1152.

6. Hastings, J. M.; Hadden, M. K.; Blagg, B. S. J. Synthesis and evaluation of derrubone and select analogues. J. Org. Chem. 2008, 73, 369-373.

7. Hadden, M. K.; Galam, L.; Gestwicki, J. E.; Matts, R. L.; Blagg, B. S. J. Derrubone, an inhibitor of the Hsp90 protein folding machinery. J. Nat. Prod. 2007, 70, 2014-2018.

8. Hadden, M. K.; Blagg, B. S. J. Cytotoxic small molecule dimers and their inhibitory activity against human breast cancer cells. Bioorg. Med. Chem. Lett. 2007, 17, 5063-5067.

9. Galam, L.; Hadden, M. K.; Ma, Z.; Ye, Q-Z.; Yun, B-G.; Blagg, B. S. J.; Matts, R. L. High-throughput assay for the identification of Hsp90 inhibitors based on Hsp90-dependent refolding of firefly luciferase. Bioorg. Med. Chem. 2007, 15, 1939-1946.

10. Ansar, S.; Burlison, J. A.; Hadden, M. K.; Yu, X. M.; Desino, K. E.; Bean, J.; Neckers, L.; Audus, K. A.; Michaelis, M. L.; Blagg, B. S. J. A non-toxic Hsp90 inhibitor protects neurons from Aβ-induced toxicity. Bioorg. Med. Chem. Lett. 2007, 17, 1984-1990.

11. Hadden, M. K.; Lubbers, D. J.; Blagg, B. S. J. Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site. Curr. Top. Med. Chem. 2006, 6, 1173-1182.

12. Avila, C.; Hadden, M. K.; Ma, Z.; Kornilayev, B. A.; Ye, Q. Z.; Blagg, B. S. J. High-throughput screening for Hsp90 ATPase inhibitors. Bioorg. Med. Chem. Lett. 2006, 16, 3005-3008.

 

Medical University of South Carolina

1 Orwig, K. S.; Lassetter, M. R.; Hadden, M. K.; Dix, T.A. Comparison of N-terminal modifications of neurotensin (8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy. J. Med. Chem. 2009, 52, 1803-1813.

2. Hadden, M. K.; Orwig, K. S.; Kokko, K. P.; Mazella, J.; Dix, T. A. Design, synthesis, and evaluation of the antipsychotic potential of orally bioavailable neurotensin(8-13) analogues containing non-natural arginine and lysine residues. Neuropharmacology. 2005, 49, 1149-1159.

3. Hadden, M. K.; Kokko, K. P.; Dix, T. A. Asymmetric synthesis of w-bromo-2(S)-methyl acids as precursors for novel arginine, lysine, and mercapto residues. Syn. Comm. 2005, 35, 1675-1680.

4. Hadden, M. K.; Walle, T.; Dix, T. A. Cellular uptake of a radiolabelled analogue of neurotensin in the caco-2 cell model. J. Pharm. and Pharmacol. 2005, 57, 327-333.

5. Kokko, K. P.; Hadden, M. K.; Price, K. L.; Orwig, K. S.; See, R. E.; Dix, T. A. Behavioral effects of stable, receptor-selective neurotensin[8-13] analogues that cross the blood-brain barrier. Neuropharmacology. 2003, 48, 417-425.

6. Kokko, K. P.; Hadden, M. K.; Orwig, K. S., Mazella, J.; Dix, T. A. In vitro analysis of stable, receptor-selective neurotensin[8-13] analogues. J. Med. Chem. 2003, 46, 4141-4148.