Volume 15(4); 2024 Apr 11
Articles from this journal are generally available in PMC after a 12-month delay (embargo); however, the delay may vary at the discretion of the publisher.
Editorials
Empowering
Voices: Inspiring Women in Medicinal Chemistry
Maria-Jesus Blanco, Joanne J. Bronson, Erin F. DiMauro, Carolyn Dzierba, MariJean Eggen, Amanda L. Garner, Gunda Georg, Jeanine Giarolla, Nicole C. Goodwin, Melissa C. Grenier-Davies, Carrie Haskell-Luevano, Ulrike Holzgrabe, Rong Huang, H. Rachel Lagiakos, Katerina Leftheris, Yvonne Martin, Maria João Matos, Tricia L. May-Dracka, Christa E. Müller, Amy H. Newman, Emma Parmee, Jennifer C. Petter, Nuria A. Tamayo, Ruth R. Wexler, Maria Laura Bolognesi, Amy Ripka, Wendy Young
ACS Med Chem Lett. 2024 Apr 11; 15(4): 424–431. Published online 2024 Mar 8. doi: 10.1021/acsmedchemlett.4c00097
Currently embargoed: Free in PMC on Apr 11, 2025
59 Years of MIKIW—A Historical Perspective
Brought Up-to-Date and an Invitation to Collaborate
Douglas Armstrong
ACS Med Chem Lett. 2024 Apr 11; 15(4): 432–433. Published online 2024 Mar 21. doi: 10.1021/acsmedchemlett.4c00108
Currently embargoed: Free in PMC on Apr 11, 2025
In This Issue
In This Issue,
Volume 15, Issue 4
Andrew P. Riley
ACS Med Chem Lett. 2024 Apr 11; 15(4): 434–435. Published online 2024 Apr 11. doi: 10.1021/acsmedchemlett.4c00123
Currently embargoed: Free in PMC on Apr 11, 2025
Innovation
How Shilajit-Based
Nanocarriers Alter Classical Doxorubicin
Delivery to Breast Cancer Cells (MCF-7 and ZR-75-1)
Zahra Asadi, Saba Jalilian, Elham Arkan, Faranak Aghaz
ACS Med Chem Lett. 2024 Apr 11; 15(4): 449–456. Published online 2024 Mar 27. doi: 10.1021/acsmedchemlett.3c00538
Currently embargoed: Free in PMC on Apr 11, 2025
Balanced Permeability Index: A Multiparameter Index
for Improved In Vitro Permeability
Dahlia
R. Weiss, Javier L. Baylon, Ethan D. Evans, Anthony Paiva, Gerry Everlof, Jingfang Cutrone, Fabio Broccatelli
ACS Med Chem Lett. 2024 Apr 11; 15(4): 457–462. Published online 2024 Mar 19. doi: 10.1021/acsmedchemlett.3c00542
Currently embargoed: Free in PMC on Apr 11, 2025
Letters
Dickson Mambwe, Dina Coertzen, Meta Leshabane, Mwila Mulubwa, Mathew Njoroge, Liezl Gibhard, Gareth Girling, Kathryn J. Wicht, Marcus C. S. Lee, Sergio Wittlin, Diogo Rodrigo Magalhães Moreira, Lyn-Marie Birkholtz, Kelly Chibale
ACS Med Chem Lett. 2024 Apr 11; 15(4): 463–469. Published online 2024 Mar 18. doi: 10.1021/acsmedchemlett.3c00496
Discovery
of a New Class of 1-(4-Sulfamoylbenzoyl)piperidine-4-carboxamides
as Human Carbonic Anhydrase Inhibitors
Davide Moi, Serena Vittorio, Andrea Angeli, Claudiu T. Supuran, Valentina Onnis
ACS Med Chem Lett. 2024 Apr 11; 15(4): 470–477. Published online 2024 Mar 13. doi: 10.1021/acsmedchemlett.3c00484
Currently embargoed: Free in PMC on Apr 11, 2025
Discovery of CRN04894: A Novel Potent Selective MC2R
Antagonist
Sun Hee Kim, Sangdon Han, Jian Zhao, Shimiao Wang, Ana Karin Kusnetzow, Greg Reinhart, Melissa A. Fowler, Stacy Markison, Michael Johns, Rosa Luo, R. Scott Struthers, Yunfei Zhu, Stephen F. Betz
ACS Med Chem Lett. 2024 Apr 11; 15(4): 478–485. Published online 2024 Mar 19. doi: 10.1021/acsmedchemlett.3c00514
Currently embargoed: Free in PMC on Apr 11, 2025
Structure-Based
Optimization of Selective and Brain
Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions
Stefan McCarver, Luke Hanna, Andrew Samant, Aaron A. Thompson, Mark Seierstad, Arjun Saha, Dongpei Wu, Brian Lord, Steven W. Sutton, Vishal Shah, Cynthia M. Milligan, Michelle Wennerholm, Jonathan Shelton, Terry P. Lebold, Brock T. Shireman
ACS Med Chem Lett. 2024 Apr 11; 15(4): 486–492. Published online 2024 Mar 7. doi: 10.1021/acsmedchemlett.3c00523
Currently embargoed: Free in PMC on Apr 11, 2025
Exploring
Scaffold Hopping for Novel 2-(Quinolin-4-yloxy)acetamides
with Enhanced Antimycobacterial Activity
Ana Flávia Borsoi, Alessandro Silva Ramos, Nathalia Sperotto, Bruno Lopes Abbadi, Fernanda Souza Macchi Hopf, Adilio da Silva Dadda, Raoní Scheibler Rambo, Mauro Neves Muniz, Josiane Delgado Paz, Estevão Silveira Grams, Fernanda Fries da Silva, Kenia Pissinate, Luiza Galina, Laura Calle González, Lovaine Silva Duarte, Marcia Alberton Perelló, Alexia de Matos Czeczot, Cristiano Valim Bizarro, Luiz Augusto Basso, Pablo Machado
ACS Med Chem Lett. 2024 Apr 11; 15(4): 493–500. Published online 2024 Mar 11. doi: 10.1021/acsmedchemlett.3c00570
Currently embargoed: Free in PMC on Apr 11, 2025
Matthew Allison, Rebecca L. Davie, Adrian J. Mogg, Sally L. Hampton, Jonas Emsley, Michael J. Stocks
ACS Med Chem Lett. 2024 Apr 11; 15(4): 501–509. Published online 2024 Mar 28. doi: 10.1021/acsmedchemlett.3c00572
Imidazole
Bioisostere Activators of Endopeptidase
Neurolysin with Enhanced Potency and Metabolic Stability
Md. Shafikur Rahman, Shiva Hadi Esfahani, Yong Zhang, Aarfa Queen, Manar Aljarrah, Haya Kandil, Andrew Baez, Thomas J. Abbruscato, Vardan T. Karamyan, Paul C. Trippier
ACS Med Chem Lett. 2024 Apr 11; 15(4): 510–517. Published online 2024 Mar 29. doi: 10.1021/acsmedchemlett.4c00009
Currently embargoed: Free in PMC on Apr 11, 2025
Design, Synthesis,
and Evaluation of 8-(o-Tolyl)quinazoline
Derivatives as Small-Molecule
PD-1/PD-L1 Antagonists
Xingye Wu, He Li, Han Liu, Xueyan Ding, Xinting Chen, Chenxi Yin, Yali Gao, Junjie Ma
ACS Med Chem Lett. 2024 Apr 11; 15(4): 518–523. Published online 2024 Mar 15. doi: 10.1021/acsmedchemlett.4c00014
Currently embargoed: Free in PMC on Apr 11, 2025
Lead Optimization
of Small Molecule ENL YEATS Inhibitors
to Enable In Vivo Studies: Discovery of TDI-11055
Mayako Michino, Tanweer A. Khan, Michael W. Miller, Yoshiyuki Fukase, Jeremie Vendome, Carolina Adura, J. Fraser Glickman, Yiman Liu, Liling Wan, C. David Allis, Andrew W. Stamford, Peter T. Meinke, Louis M. Renzetti, Stacia Kargman, Nigel J. Liverton, David J. Huggins
ACS Med Chem Lett. 2024 Apr 11; 15(4): 524–532. Published online 2024 Mar 12. doi: 10.1021/acsmedchemlett.4c00016
Currently embargoed: Free in PMC on Apr 11, 2025
Marion G. Götz, Kacey Godwin, Rachel Price, Robert Dorn, Gabriel Merrill-Steskal, William Klemmer, Hunter Hansen, Gautam Produturi, Megan Rocha, Mathias Palmer, Lea Molacek, Zack Strater, Michael Groll
ACS Med Chem Lett. 2024 Apr 11; 15(4): 533–539. Published online 2024 Mar 27. doi: 10.1021/acsmedchemlett.4c00017
In Retrospect:
Root-Cause Analysis of Structure–Activity
Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833)
Stephen W. Wright, Kathleen A. Farley, Seungil Han, John D. Knafels, Katherine L. Lee
ACS Med Chem Lett. 2024 Apr 11; 15(4): 540–545. Published online 2024 Mar 21. doi: 10.1021/acsmedchemlett.4c00036
Currently embargoed: Free in PMC on Apr 11, 2025
Discovery
of Hepatitis B Virus Surface Antigen Suppressor
GS-8873
Darryl Kato, Regina Wai-Yan Choy, Eda Canales, Ryan A. Dick, April D. Lake, Nathan D. Shapiro, Elbert Chin, Jiayao Li, Jennifer R. Zhang, Qiaoyin Wu, Roland D. Saito, Sammy Metobo, Evangelos Aktoudianakis, Scott D. Schroeder, Zheng-Yu Yang, Dylan M. Glatt, Scott Balsitis, Lindsay Gamelin, Mei Yu, Guofeng Cheng, William E. Delaney, IV, John O. Link
ACS Med Chem Lett. 2024 Apr 11; 15(4): 546–554. Published online 2024 Mar 22. doi: 10.1021/acsmedchemlett.4c00037
Currently embargoed: Free in PMC on Apr 11, 2025
Chemical
Space Profiling of SARS-CoV-2 PLpro Using DNA-Encoded
Focused Libraries
Xudong Wang, Ying Zhu, Qingyi Zhao, Weiwei Lu, Yechun Xu, Hangchen Hu, Xiaojie Lu
ACS Med Chem Lett. 2024 Apr 11; 15(4): 555–564. Published online 2024 Mar 14. doi: 10.1021/acsmedchemlett.4c00069
Currently embargoed: Free in PMC on Apr 11, 2025
Patent Highlight
Novel Phosphorylpurinone
Compounds for Treating Cancer
Ram W. Sabnis
ACS Med Chem Lett. 2024 Apr 11; 15(4): 441–442. Published online 2024 Mar 8. doi: 10.1021/acsmedchemlett.4c00087
Currently embargoed: Free in PMC on Apr 11, 2025
Novel PCSK9 Inhibitors for Treating Cardiovascular
Diseases
Ram W. Sabnis
ACS Med Chem Lett. 2024 Apr 11; 15(4): 443–444. Published online 2024 Mar 8. doi: 10.1021/acsmedchemlett.4c00088
Currently embargoed: Free in PMC on Apr 11, 2025
Novel ACC
Inhibitors for Treating Acne
Ram W. Sabnis
ACS Med Chem Lett. 2024 Apr 11; 15(4): 445–446. Published online 2024 Mar 27. doi: 10.1021/acsmedchemlett.4c00118
Currently embargoed: Free in PMC on Apr 11, 2025
Novel Isoxazolidines
as RIPK1 Inhibitors for Treating
Alzheimer’s Disease, Multiple Sclerosis, and Amyotrophic Lateral
Sclerosis
Ram W. Sabnis
ACS Med Chem Lett. 2024 Apr 11; 15(4): 447–448. Published online 2024 Apr 2. doi: 10.1021/acsmedchemlett.4c00119
Currently embargoed: Free in PMC on Apr 11, 2025
Viewpoint
The Science
and Art of Structure-Based Virtual Screening
Hongtao Zhao
ACS Med Chem Lett. 2024 Apr 11; 15(4): 436–440. Published online 2024 Mar 25. doi: 10.1021/acsmedchemlett.4c00093
Currently embargoed: Free in PMC on Apr 11, 2025
Articles from ACS Medicinal Chemistry Letters are provided here courtesy of American Chemical Society