MIKIW 2019


MIKIW 2019 event logo

April 12 - 14, 2019
The University of Kansas | Lawrence, KS

Keynote Speaker:

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

Details

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

MinnesotaIllinoisKansasIowa
O. GisvoldL. BauerM.P. MertesJ.G. Cannon
P.S. PortogheseD. CovielloE.E. SmissmanD.T. Witiak
T.O. SoineR. DanielsR.A. Wiley 
 J.E. Gearien  

MIKIW 2019 Schedule

Friday, April 12, 2019
TimeAgenda ItemLocation
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 receptionArterra Event Gallery
Saturday, April 13, 2019

* ISB = KU Integrated Science Building

TimeAgenda ItemLocation
8:00 – 8:40 a.m.Breakfast and poster setupISB Atrium
8:40 – 9:00 a.m.Opening remarksISB 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.BreakISB Atrium
11:00 a.m. – noonKeynote 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 setupISB 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 presentISB Atrium
3:45 – 4:45 p.m.Poster session: Even numbered posters presentISB Atrium
4:45 – 5:15 p.m.Faculty meetingISB 1160
6:00 – 7:00 p.m.Faculty mixer (open bar)Van Go inc.
7:00 p.m.Formal banquet dinnerVan Go inc.
Sunday, April 14, 2019

* ISB = KU Integrated Science Building

TimeAgenda ItemLocation
 Check-out of hotel prior to breakfastSpringhill Suites » - Minnesota and Illinois
Quality Inn and Suites » - Iowa
Days Inn » - Wisconsin
8:00 – 8:40 a.m.BreakfastISB 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.BreakISB 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

"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.

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

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

YearHostSpeakerAssociation
2018University of Illinois at ChicagoDr. Michelle ArkinUniversity of California, San Francisco
2017University of MinnesotaDr. Uttam K. TambarUT Southwestern Medical Center
2016The University of IowaDr. Amy Hauck NewmanNIH-NIDA
2015The University of KansasDr. Bruce RothGenentech
2014University of Illinois at ChicagoDr. Paul WenderStanford University
2013University of MinnesotaDr. Marvin J. MillerUniversity of Notre Dame
2012The University of IowaDr. Heidi E. HammVanderbilt University
2011The University of KansasDr. Dennis C. LiottaEmory University
2010University of Illinois at ChicagoDr. Tomáš HudlickýBrock University
2009University of MinnesotaDr. Dale BogerScripps Research Institute
2008The University of IowaDr. Daniel KahneHarvard University
2007The University of KansasDr. Albert PadwaEmory University
2006University of Illinois at ChicagoDr. William FenicalUniversity of California, San Diego
2005University of MinnesotaDr. Christopher LipinskiPfizer, Inc.
2004The University of IowaDr. Kenner RiceNIH
2003The University of KansasDr. C. Dale PoulterUniversity of Utah
2002University of Illinois at ChicagoDr. Richard B. SilvermanNorthwestern University
2001University of MinnesotaDr. Andrew HamiltonYale University
2000The University of IowaDr. Michael MarlettaUniversity of Michigan
1999The University of KansasDr. Roger M. FriedingerMerck Research Laboratories
1998University of Illinois at ChicagoDr. Richard A. LernerScripps Research Institute
1997University of MinnesotaDr. John MontgomeryBiocryst Pharmaceuticals, Inc.
1996The University of IowaDr. David NicholsPurdue University
1995The University of KansasDr. Paul AndersonDupont Merck Pharmaceuticals
1994University of Illinois at ChicagoDr. Arthur PatchettMerck Research Laboratories
1993University of MinnesotaDr. Daniel RichUniversity of Wisconsin, Madison
1992The University of IowaDr. Laurence HurleyUniversity of Texas, Austin
1991The University of KansasDr. Julius RebekMassachusetts Institute of Technology
1990University of Illinois at ChicagoDr. Koji NakanishiColumbia University
1989University of MinnesotaDr. John KatzenellenbogenUniversity of Illinois, Urbana-Champaign
1988The University of IowaDr. Carl DjerrasiStanford University
1987The University of KansasDr. William RoushIndiana University
1986University of Illinois at ChicagoDr. Joseph FriedUniversity of Chicago
1985University of MinnesotaDr. David TriggleSUNY Buffalo
1984The University of IowaDr. Alan KatritzkyUniversity of Florida
1983University of WisconsinDr. Paul BartlettUniversity of California, Berkeley
1982The University of KansasDr. Henry RapoportUniversity of California, Berkeley
1981University of Illinois at ChicagoDr. Harry WassermanYale University
1980University of MinnesotaDr. Eugene JorgensenUniversity of California, San Francisco
1979The University of IowaDr. Alan SartorelliYale University
1978The University of KansasDr. Albert MeyersColorado State University
1977University of Illinois at ChicagoDr. Heinz FlossPurdue University
1976University of MinnesotaDr. Donald JerinaNIH
1975The University of IowaDr. Everett MayNIH
1974The University of KansasDr. Marjorie HorningBaylor University
1973University of Illinois at ChicagoDr. Arnold BrossiHoffman-LaRoche
1972University of MinnesotaDr. Gertrude ElionBurroughs-Wellcome
1971The University of IowaDr. Bernard BelleauUniversity of Ottawa
1970The University of KansasDr. Corwin HanschPomona College
1969University of Illinois at ChicagoDr. Everett MaynertUniversity of Illinois
1968University of MinnesotaDr. Bernard BakerUniversity of California, Santa Barbara
1967The University of IowaDr. Julius AxelrodNIH
1966The University of KansasDr. Richard SchowenThe University of Kansas

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