Design, Synthesis, and Biological Evaluation of 2-Hydroxy-4-phenylthiophene-3-carbonitrile as PD-L1 Antagonist and Its Comparison to Available Small Molecular PD-L1 Inhibitors

Author:

Ważyńska Marta A.1ORCID,Butera Roberto2,Requesens Marta1,Plat Annechien1,Zarganes-Tzitzikas Tryfon3,Neochoritis Constantinos G.4ORCID,Plewka Jacek5ORCID,Skalniak Lukasz5,Kocik-Krol Justyna56,Musielak Bogdan5,Magiera-Mularz Katarzyna5ORCID,Rodriguez Ismael56ORCID,Blok Simon N.7ORCID,de Bruyn Marco1,Nijman Hans W.1,Elsinga Philip H.7ORCID,Holak Tad A.5ORCID,Dömling Alexander28ORCID

Affiliation:

1. Department of Obstetrics and Gynecology, University Medical Center Groningen, University of Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands

2. Department of Drug Design, University of Groningen, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands

3. Centre for Medicines Discovery, Nuffield Department of Medicine, Alzheimer’s Research UK Oxford Drug Discovery Institute, NDM Research Building, Roosevelt Drive, OX3 7FZ Oxford, U.K.

4. Department of Chemistry, University of Crete, Voutes, 70013 Heraklion, Greece

5. Department of Organic Chemistry, Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387 Krakow, Poland

6. Doctoral School of Exact and Natural Sciences, Jagiellonian University, Prof. St. Łojasiewicz St 11, 30-348 Krakow, Poland

7. Department of Nuclear Medicine and MolecularImaging, University Medical Center Groningen, University of Groningen, Hanzeplein 1, 9713 GZ Groningen, The Netherlands

8. Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry and Czech Advanced Technology and Research Institute, Palacky University in Olomouc, Olomouc 77900, Czech Republic

Funder

HORIZON EUROPE Widening participation and spreading excellence

European Regional Development Fund

Fundacja na rzecz Nauki Polskiej

KWF Kankerbestrijding

H2020 Spreading Excellence and Widening Participation

Narodowe Centrum Badan i Rozwoju

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference42 articles.

1. The blockade of immune checkpoints in cancer immunotherapy

2. Immune-related adverse events with immune checkpoint blockade: a comprehensive review

3. European Medicines Agency. EMEA/H/C/003985─EPAR Product Information 2022. https://www.ema.europa.eu/en/documents/product-information/opdivo-epar-product-information_en.pdf (accessed Sept 01, 2022).

4. Opdivo (nivolumab) price, Farmacotherapeutisch Kompas. https://www.farmacotherapeutischkompas.nl/bladeren/preparaatteksten/n/nivolumab#kosten (accessed Sept 01, 2022).

5. Queva, C.; Morrow, M.; Hammond, S.; Alimzhanov, M.; Babcock, J.; Foltz, I.; Kang, J. S.; Sekirov, L.; Boyle, M.; Chodorge, M. Targeted binding agents against b7-h1. WO 2011066389 A1, 2011.

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