ACS Med Chem Lett
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
- PMCID:
- PMC11017407
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017382
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017383
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
- PMCID:
- PMC11017394
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017404
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017395
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
- PMCID:
- PMC11017293
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017392
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017389
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017393
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017388
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
- PMCID:
- PMC11017387
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017391
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017412
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017298
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
- PMCID:
- PMC11017396
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017420
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017295
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017390
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017386
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017384
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017424
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
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
- PMCID:
- PMC11017385
Currently embargoed: Free in PMC on Apr 11, 2025; PubMed
Articles from ACS Medicinal Chemistry Letters are provided here courtesy of American Chemical Society