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2019 MIKIW logo

MIKIW 2019

April 12 - 14, 2019

The University of Kansas | Lawrence, KS

Keynote Speaker:

Nicholas A. Meanwell, Ph.D., FRSC, Executive Director Bristol-Myers Squibb

About MIKIW

The first Medicinal Chemistry Meeting-in-Miniature was organized by faculty from the Departments of Medicinal Chemistry and Pharmacognosy at the Universities of University of MinnesotaUniversity of Illinois at Chicago, The University of Kansas, and The University of Iowa in 1963. Since then, the Departments of Medicinal Chemistry and Pharmacognosy at these universities have alternately hosted the MIKI meeting. MIKI is the longest running and largest regional medicinal chemistry meeting in the U.S., and brings together over 200 graduate students, post-doctoral fellows, and faculty members from the four universities on an annual basis. In 2018, the University of Wisconsin-Madison joined MIKI, giving the conference the new name MIKIW. This year, the graduate students at The University of Kansas are excited to host the 57th Annual MIKIW Meeting and continue this great tradition.

Graduate students from the hosting university have the opportunity to organize and moderate the entire meeting, providing the valuable experience of coordinating a professional event. In addition, participating students receive professional experiences by delivering oral and/or poster presentations, as well as vital networking opportunities. Furthermore, these annual meetings also act as a catalyst for sharing and exchanging ideas among students, postdoctoral researchers, and faculty of the different universities. The meeting features a keynote address from a distinguished scientist in academia, industry, or government, who is a leader in the field of medicinal chemistry.


MIKI Founders

Minnesota Illinois Kansas Iowa
O. Gisvold L. Bauer M.P. Mertes J.G. Cannon
P.S. Portoghese D. Coviello E.E. Smissman D.T. Witiak
T.O. Soine R. Daniels R.A. Wiley  
  J.E. Gearien    

Agenda

MIKIW 2019 Schedule

Friday, April 12, 2019
Time Agenda Item Location
3:00 – 6:00 p.m. • Registration open
• Hotel check-in
Springhill Suites » - Minnesota and Illinois
Quality Inn and Suites » - Iowa
Days Inn » - Wisconsin
7:00 p.m. Welcome reception Arterra Event Gallery
Saturday, April 13, 2019

* ISB = KU Integrated Science Building

Time Agenda Item Location
8:00 – 8:40 a.m. Breakfast and poster setup ISB Atrium
8:40 – 9:00 a.m. Opening remarks ISB Auditorium
  Oral presentation session 1
Moderators: Patrick Ross, Bo Han
ISB Auditorium
9:00 – 9:25 a.m. Yuwen Yin
Blake Peterson lab, KU
Phorbol Carbamates as Novel Tools for Controlling Cellular Signal Transduction
 
9:25 – 9:50 a.m. Arturo L. Aguirre
Robert Kerns lab, UI
Investigating Quinazoline-2,4-dione and Fluoroquinolone Scaffolds for Antibiotic Activity and Metabolic Stability
 
9:50 – 10:15 a.m. Stephanie Blaszczyk
Weiping Tang lab, UW-Madison
S-Adamantyl Group Directed Site-Selective Acylation and Its Applications in the Streamlined Assembly of Oligosaccharides
 
10:15 – 10:40 a.m. Kellan T. Passow
Daniel A. Harki lab, UMN
The Discovery of 4CIN: Indoles as a Platform for Novel Nucleoside Fluorophore Development
 
10:40 – 11:00 a.m. Break ISB Atrium
11:00 a.m. – noon Keynote address
"Inhibitors of HIV-1 Maturation"
Nicholas A. Meanwell, Ph.D., FRSC
Dept. of Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development
ISB Auditorium
12:00 – 1:30 p.m. Lunch and poster setup ISB Atrium
  Oral presentation session 2
Moderators: Sahishna Phaniraj, Bo Han
ISB Auditorium
1:30 – 1:55 p.m. Jacob P. Sorrentino
Ryan Altman lab, KU
Fluorinated Dextromethorphan Analogs to Prevent the Formation of Psychoactive Metabolites
 
1:55 – 2:20 p.m. Brian P. David
Terry W. Moore lab, UIC
Structure-Activity Relationship and Evaluation of Non-electrophilic NRF2 Activators in a Diabetic Mouse Model
 
2:20 – 2:45 p.m. Muhammad M. Khalifa
Jennifer E. Golden lab, UW-Madison
Convergent Annulative Platform for the Synthesis of Ring-Fused Quinolinones
 
2:45 – 3:45 p.m. Poster session: Odd numbered posters present ISB Atrium
3:45 – 4:45 p.m. Poster session: Even numbered posters present ISB Atrium
4:45 – 5:15 p.m. Faculty meeting ISB 1160
6:00 – 7:00 p.m. Faculty mixer (open bar) Van Go inc.
7:00 p.m. Formal banquet dinner Van Go inc.
Sunday, April 14, 2019

* ISB = KU Integrated Science Building

Time Agenda Item Location
  Check-out of hotel prior to breakfast Springhill Suites » - Minnesota and Illinois
Quality Inn and Suites » - Iowa
Days Inn » - Wisconsin
8:00 – 8:40 a.m. Breakfast ISB Atrium
  Oral presentation session 3
Moderators: Patrick Ross, Bo Han
ISB Auditorium
8:40 - 9:05 a.m. Erick J. Carlson
Gunda I. Georg lab, UMN
The Discovery and Characterization of Steroidal Blockers of CatSper
 
9:05 - 9:30 a.m. Alanna Condren
Laura Sanchez lab, UIC
Biofilm Inhibition Alters Specialized Metabolism and Increases Virulence in Pseudomonas Aeruginosa
 
9:30 - 9:55 a.m. Sanjay Bhattarai
Michael S. Wolfe lab, KU
Substrate transmembrane mimetic inhibitors of gamma-secretase: probes for chemical structural biology
 
9:55 - 10:20 a.m. Pratik Rajesh Chheda
Robert J. Kerns lab, UI
Allosteric Inhibitors of Apicoplast DNA Polymerase: New Antimalarials That Bind a Novel Allosteric Binding Site
 
10:20 - 10:40 a.m. Break ISB Atrium
  Oral presentation session 4
Moderators: Tomas Smith, Bo Han
ISB Auditorium
10:40 - 11:05 a.m. Matthew Worth
Jiaoyan Jiang lab, UW-Madison
Covalent Inhibitors Target O-GlcNAc Transferase in Cells
 
11:05 - 11:30 a.m. Ozgun Kilic
Cartson Rick Wagner lab, UMN
Nanorings with Engineered Fibronectins for Cancer Therapeutics
 
11:30 - 11:55 a.m. Katherine E. Zink
Laura M. Sanchez lab, UIC
A Novel Imaging Mass Spectrometry Method for Identifying Preventative Approaches in High Grade Serous Ovarian Cancer
 
12:00 p.m. • Concluding remarks
• Box lunch served
• Buses depart
ISB Atrium

Keynote Presentation

"Inhibitors of HIV-1 Maturation"

Nicholas A. Meanwell, Ph.D., FRSC
Dept. of Chemistry and Molecular Technologies, Bristol-Myers Squibb Research and Development

Abstract: Maturation of the HIV-1 capsid (CA) peptide by HIV-1 protease-mediated cleavage at the CA-SP1 junction is the final step in the formation of infectious virus capsid. A phenotypic screen identified the betulinic acid derivative bevirimat as an inhibitor specific to this step in virion production and this compound demonstrated antiviral effects in Phase 2a clinical trials. However, naturally-occurring polymorphisms proximal to the cleavage site conferred much reduced sensitivity to the effects of bevirimat in vitro which correlated with the clinical response. Guided by assays incorporating the natural polymorphisms, we identified GSK-3532795/BMS-955176 as a second generation HIV-1 maturation inhibitor that exhibits a broader spectrum of antiviral effect in vitro that translated into improved efficacy in clinical trials. In this presentation, we will describe the strategy and tactics adopted by the drug discovery team that led to the discovery of GSK-3532795/BMS-955176, the antiviral and pharmacokinetic profiles of the molecule and the results of early clinical studies.

Sponsors

Acknowledgements

The 57th Annual MIKIW Medicinal Chemistry Meeting would not be possible without the support of the following sponsors. The MIKIW 2019 Organizing Committee and the Department of Medicinal Chemistry at The University of Kansas express our appreciation and sincere gratitude for these generous financial contributions. Thank you to all of the 2019 MIKIW supporters!

Platinum-level Sponsors
  • ACS Medicinal Chemistry Division
  • Pfizer

Gold-level Sponsors
  • KU School of Pharmacy
  • Advion
  • KU Chemical Biology of Infectious Disease

Silver-level Sponsors
  • Waters
  • Teledyne ISCO
  • Deciphera
  • The University of Kansas Cancer Center
  • KU Madison & Lila Self Graduate Fellowship
  • Biotage
  • Vertex
  • Corning
  • KU Higuchi Bioscience Center
  • Journal of Medicinal Chemistry
  • Journal of Natural Products
  • ACS Medicinal Chemistry Letters
  • Abbvie

Bronze-level Sponsors
  • Thincnext
  • Strem Chemicals, Inc.
  • Bristol-Myers Squibb
  • Norell
  • Avanti Polar Lipids, Inc.
  • Orion Bioscience, Inc.
  • Sekisui Xenotech
  • BioTools
  • KU Alumni Association
  • New England Biolabs

Past Keynotes

The previous keynote speakers are among the most accomplished scientists. This group includes Nobel laureates, members of the National Academy of Sciences, leaders in the pharmaceutical industry, and many members of the ACS Medicinal Chemistry Division Hall of Fame. In 2019, we are pleased to have Dr. Nicholas A. Meanwell of Bristol-Myers Squibb deliver the keynote address.

Past Keynote Lectures

Year Host Speaker Association
2018 University of Illinois at Chicago Dr. Michelle Arkin University of California, San Francisco
2017 University of Minnesota Dr. Uttam K. Tambar UT Southwestern Medical Center
2016 The University of Iowa Dr. Amy Hauck Newman NIH-NIDA
2015 The University of Kansas Dr. Bruce Roth Genentech
2014 University of Illinois at Chicago Dr. Paul Wender Stanford University
2013 University of Minnesota Dr. Marvin J. Miller University of Notre Dame
2012 The University of Iowa Dr. Heidi E. Hamm Vanderbilt University
2011 The University of Kansas Dr. Dennis C. Liotta Emory University
2010 University of Illinois at Chicago Dr. Tomáš Hudlický Brock University
2009 University of Minnesota Dr. Dale Boger Scripps Research Institute
2008 The University of Iowa Dr. Daniel Kahne Harvard University
2007 The University of Kansas Dr. Albert Padwa Emory University
2006 University of Illinois at Chicago Dr. William Fenical University of California, San Diego
2005 University of Minnesota Dr. Christopher Lipinski Pfizer, Inc.
2004 The University of Iowa Dr. Kenner Rice NIH
2003 The University of Kansas Dr. C. Dale Poulter University of Utah
2002 University of Illinois at Chicago Dr. Richard B. Silverman Northwestern University
2001 University of Minnesota Dr. Andrew Hamilton Yale University
2000 The University of Iowa Dr. Michael Marletta University of Michigan
1999 The University of Kansas Dr. Roger M. Friedinger Merck Research Laboratories
1998 University of Illinois at Chicago Dr. Richard A. Lerner Scripps Research Institute
1997 University of Minnesota Dr. John Montgomery Biocryst Pharmaceuticals, Inc.
1996 The University of Iowa Dr. David Nichols Purdue University
1995 The University of Kansas Dr. Paul Anderson Dupont Merck Pharmaceuticals
1994 University of Illinois at Chicago Dr. Arthur Patchett Merck Research Laboratories
1993 University of Minnesota Dr. Daniel Rich University of Wisconsin, Madison
1992 The University of Iowa Dr. Laurence Hurley University of Texas, Austin
1991 The University of Kansas Dr. Julius Rebek Massachusetts Institute of Technology
1990 University of Illinois at Chicago Dr. Koji Nakanishi Columbia University
1989 University of Minnesota Dr. John Katzenellenbogen University of Illinois, Urbana-Champaign
1988 The University of Iowa Dr. Carl Djerrasi Stanford University
1987 The University of Kansas Dr. William Roush Indiana University
1986 University of Illinois at Chicago Dr. Joseph Fried University of Chicago
1985 University of Minnesota Dr. David Triggle SUNY Buffalo
1984 The University of Iowa Dr. Alan Katritzky University of Florida
1983 University of Wisconsin Dr. Paul Bartlett University of California, Berkeley
1982 The University of Kansas Dr. Henry Rapoport University of California, Berkeley
1981 University of Illinois at Chicago Dr. Harry Wasserman Yale University
1980 University of Minnesota Dr. Eugene Jorgensen University of California, San Francisco
1979 The University of Iowa Dr. Alan Sartorelli Yale University
1978 The University of Kansas Dr. Albert Meyers Colorado State University
1977 University of Illinois at Chicago Dr. Heinz Floss Purdue University
1976 University of Minnesota Dr. Donald Jerina NIH
1975 The University of Iowa Dr. Everett May NIH
1974 The University of Kansas Dr. Marjorie Horning Baylor University
1973 University of Illinois at Chicago Dr. Arnold Brossi Hoffman-LaRoche
1972 University of Minnesota Dr. Gertrude Elion Burroughs-Wellcome
1971 The University of Iowa Dr. Bernard Belleau University of Ottawa
1970 The University of Kansas Dr. Corwin Hansch Pomona College
1969 University of Illinois at Chicago Dr. Everett Maynert University of Illinois
1968 University of Minnesota Dr. Bernard Baker University of California, Santa Barbara
1967 The University of Iowa Dr. Julius Axelrod NIH
1966 The University of Kansas Dr. Richard Schowen The University of Kansas

Contact

For questions about MIKIW 2019, contact KU Medicinal Chemistry at medchem@ku.edu.


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