Marcus A. Tius, PhD, MS

Marcus Antonius Tius, PhD, MS

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Full Member, Cancer Biology Program, University of Hawaiʻi Cancer Center
University of Hawaiʻi Cancer Center Special Liaison to University of Hawaiʻi at Mānoa
Deputy Director (2008-2015), University of Hawaiʻi Cancer Center

Academic Appointment(s):
Professor, Department of Chemistry, College of Natural Sciences, University of Hawaiʻi at Mānoa
Joanna L. Sullivan Chair for Cancer Research, University of Hawaiʻi Cancer Center

1980 - PhD, Chemistry, Harvard University
1977 - MS, Chemistry, Harvard University

2001 - CREST Fellowship (Japan)
1998 - Japan Society for the Promotion of Science Fellowship
1987 - 1991 - Fellow of the Alfred P. Sloan Foundation


11/18/2002 - Roche Distinguished Lecturer, Colorado State University
2000 - Faculty Performance Award
1996 - Honolulu City Council Honoree (research)
1993 - Mortar Board Honoree (teaching)
1991 - Regents' Medal for Excellence in Teaching

Research Focus

My research group works on the development of methodology in organic synthesis and applications of natural products synthesis. The targeted natural products are characterized by structural novelty and pharmacological activity that is relevant to cancer (e.g. aleutianamine, cryptophycins, madindolines, rocaglamide, terpestacin). My group collaborates with the groups of Dr. James Turkson (Cedars-Sinai Medical Center, L.A., STAT3 inhibitors), Hans G. Wendel (Memorial Sloan Kettering, rocaglamide) and Dr. Mark Hamann (Medical University of South Carolina, aleutianamine). My research group also has interests in the synthesis and medicinal chemistry of cannabinoids, primarily classical-nonclassical hybrid structures. I have collaborated with Dr. Alex Makriyannis (Director, Center for Drug Discovery, Northeastern University) on a number of projects. My research group has developed very efficient methods for stereo- and enantioselective synthesis of cannabinoids and we have developed the means to modify all the known pharmacophoric regions of these molecules. This work was initiated before the connection between activation of the endocannabinoid system and cancer had been established, so now all my research has some cancer relevance.

The process team at Eli Lilly Company modified the cryptophycin total synthesis that was developed in my group, and used the method to prepare material for clinical trial. I am a co-inventor on the cryptophycin patent. Although Lilly dropped the compound during Phase II, a research effort wqith Dr. Naoto Ueno's team to develop a ADC based on cryptophycins 1 and 52 is ongoing.

My participation in Dr. Turkson's the STAT3 project goes back approximately eight years when a collaborator with organic synthesis expertise was needed in order to provide materials. We have prepared the first sub-nanomolar specific STAT3 inhibitor.

Selected Publications

Dickinson CF, Yap GPA, Tius MA. (2023). Anion-Accelerated Asymmetric Nazarov Cyclization: Access to Vicinal All-Carbon Quaternary Stereocenters. Org. & Biomol. Chem; 21, 5014 - 5020. DOI: 10.1039/D3OB00735A.

Zhu Y, Yue P, Dickinson C, Yang J, Datanagan K, Zhai N, Zhang Y, Miklossy G, Lopez-Tapia F, Tius M, Turkson J. (2022). Natural product preferentially targets redox and metabolic adaptations and aberrantly-active STAT3 to inhibit breast tumor growth in vivo. J. Cell Death & Disease; 13(12), 1022. https:// DOI:10.1038/s41419-022-05477-2.

Yue P, Zhu Y, Brotherton-Pleiss C, Fu W, Verma N, Chen J, Nakamura K, Chen W, Chen Y, Alonso-Valenteen F, Mikhael S, Medina-Kauwe L, Kershaw KM, Celeridad M, Pan S, Limpert, AS, Sheffler DJ, Cosford NDP, Shiao SL, Tius MA, Lopez-Tapia F, Turkson J. (2022). Novel potent azetidine-based compounds irreversibly inhibit Stat3 activation and induce antitumor response against human breast tumor growth in vivo. Cancer Lett; 534, 215613. https:// DOI:10.1016/j.canlet.2022.215613.

Fu Y, Katsaros D, Biglia N, Wang Z, Pagano I, Tius M, Tiirikainen M, Rosser C, Yang H, Yu H. (2021). Vitamin D receptor upregulates lncRNA TOPORS-AS1 which inhibits the Wnt/β-catenin pathway and associates with favorable prognosis of ovarian cancer. Scientific Reports; 11, 7484.

Brotherton-Pleiss C, Yue P, Zhu Y, Nakamura K, Chen W, Fu W, Kubota C, Chen J, Alonso-Valenteen F, Mikhael S, Medina-Kauwe L, Tius MA, Lopez-Tapia F, Turkson, J. (2021). Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors. J. Med. Chem; 64, 695 – 710. https:// DOI:10.1021/acs.jmedchem.0c01705.

Publication list via PubMed

Active Grants

Mark Hamann, Marcus A. Tius, PI's
"Synthesis and Optimization of the Aleutianamine Class of Alkaloids"
Total synthesis and pharmacological evaluation of aleutianamine, a complex alkaloid isolated from a marine sponge. The natural product is scarce and has high activity against several human tumor cell lines in vitro. Synthesis will provide material for evaluation in mouse models.
07/01/2022 – 06/30/2026