Volume 15(5); 2024 May 9

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.

Editorial

Celebrating the 60th Anniversary of the MIKIW Meeting-in-Miniature: Virtual Special Issue

Terry W. Moore, William C. K. Pomerantz

ACS Med Chem Lett. 2024 May 9; 15(5): 565–566. Published online 2024 Apr 26. doi: 10.1021/acsmedchemlett.4c00139

PMCID:: PMC11089661

Currently embargoed: Free in PMC on May 9, 2025

In This Issue

In This Issue, Volume 15, Issue 5

Chiara Borsari

ACS Med Chem Lett. 2024 May 9; 15(5): 567–568. Published online 2024 May 9. doi: 10.1021/acsmedchemlett.4c00176

PMCID:: PMC11089541

Currently embargoed: Free in PMC on May 9, 2025

Letters

Vinylpyridine as a Tunable Covalent Warhead Targeting C797 in EGFR

Nils Pemberton, Nina Compagne, Argyrides Argyrou, Emma Evertsson, Anders Gunnarsson, Jason G. Kettle, Jonathan P. Orme, Richard A. Ward

ACS Med Chem Lett. 2024 May 9; 15(5): 583–589. Published online 2024 Apr 5. doi: 10.1021/acsmedchemlett.3c00425

PMCID:: PMC11089552

Currently embargoed: Free in PMC on May 9, 2025

Structural Investigations of Phthalazinone Derivatives as Allosteric Inhibitors of Human DNA Methyltransferase 3A

Ivan Hernandez, Ethan Ward, Thomas R. R. Pettus, Norbert O. Reich

ACS Med Chem Lett. 2024 May 9; 15(5): 590–594. Published online 2024 Apr 8. doi: 10.1021/acsmedchemlett.3c00528

PMCID:: PMC11089561

Article PDF–3.0M

Discovery of Sovleplenib, a Selective Inhibitor of Syk in Clinical Development for Autoimmune Diseases and Cancers

Hong Jia, Wei Deng, Baoyu Hao, Min Cai, Dong Guo, Yu Cai, Xiaoming Dai, Zhipeng Wu, Weigang He, Jian Wang, Guanglin Wang, Sumei Xia, Na Li, Weiguo Su, Guangxiu Dai

ACS Med Chem Lett. 2024 May 9; 15(5): 595–601. Published online 2024 Apr 18. doi: 10.1021/acsmedchemlett.3c00553

PMCID:: PMC11089545

Currently embargoed: Free in PMC on May 9, 2025

Identification of Dual Inhibitors Targeting Main Protease (M^pro) and Cathepsin L as Potential Anti-SARS-CoV-2 Agents

Santo Previti, Roberta Ettari, Elsa Calcaterra, Michele Roggia, Benito Natale, Annabelle C. Weldert, Christin Müller-Ruttloff, Florian Salisch, Anna Irto, Rosalia Maria Cigala, John Ziebuhr, Tanja Schirmeister, Sandro Cosconati, Maria Zappalà

ACS Med Chem Lett. 2024 May 9; 15(5): 602–609. Published online 2024 Mar 1. doi: 10.1021/acsmedchemlett.3c00562

PMCID:: PMC11089542

Currently embargoed: Free in PMC on May 9, 2025

Synthesis and Monoamine Oxidase Inhibitory Activity of Halogenated Flavones

Jorge I. Castillo-Arellano, Zachary Stryker, Michael D. Wyatt, Francisco León

ACS Med Chem Lett. 2024 May 9; 15(5): 610–618. Published online 2024 Apr 3. doi: 10.1021/acsmedchemlett.3c00573

PMCID:: PMC11089559

Currently embargoed: Free in PMC on May 9, 2025

Discovery of Disubstituted Carboranes as Inhibitors of Heat Shock Protein 90–Heat Shock Factor 1 Interaction

Yujie Shao, Kazuki Miura, Yasunobu Asawa, Taiki Morita, Guangzhe Li, Hiroyuki Nakamura

ACS Med Chem Lett. 2024 May 9; 15(5): 619–625. Published online 2024 Apr 8. doi: 10.1021/acsmedchemlett.4c00022

PMCID:: PMC11089554

Currently embargoed: Free in PMC on May 9, 2025

Analysis of the Physicochemical Properties of Anti-Schistosomal Compounds to Identify Next-Generation Leads

Diego González Cabrera, Jennifer Keiser, Thomas Spangenberg

ACS Med Chem Lett. 2024 May 9; 15(5): 626–630. Published online 2024 Apr 25. doi: 10.1021/acsmedchemlett.4c00026

PMCID:: PMC11089657

Article PDF–1.9M

Design, Synthesis, and Bioevaluation of Transcriptional Enhanced Assocciated Domain (TEAD) PROTAC Degraders

Huajie Li, Zhiming Ge, Kexin Lin, Wei He, Qinyu Chu, Mingyue Zheng, Sulin Zhang, Tianfeng Xu

ACS Med Chem Lett. 2024 May 9; 15(5): 631–639. Published online 2024 Apr 22. doi: 10.1021/acsmedchemlett.4c00029

PMCID:: PMC11089546

Currently embargoed: Free in PMC on May 9, 2025

Simple Fluorescence Labeling Method Enables Detection of Intracellular Distribution and Expression Level of Retinoid X Receptors

Yukina Tanaka, Michiko Fujihara, Yuta Takamura, Mayu Kawasaki, Shogo Nakano, Makoto Makishima, Hiroki Kakuta

ACS Med Chem Lett. 2024 May 9; 15(5): 640–645. Published online 2024 Apr 23. doi: 10.1021/acsmedchemlett.4c00033

PMCID:: PMC11089654

Currently embargoed: Free in PMC on May 9, 2025

Discovery of CVN293, a Brain Permeable KCNK13 (THIK-1) Inhibitor Suitable for Clinical Assessment

Roland W. Bürli, Kevin J. Doyle, Louise Dickson, Anna Rowland, Kim Matthews, Andrew J. Stott, Martin Teall, Bernardino Ossola, Samuel G. Russell, Jenna R. M. Harvey, Yiming Wu, Lakshminarayana Narayana, Nicola L. Brice, Mark Carlton, Lee A. Dawson

ACS Med Chem Lett. 2024 May 9; 15(5): 646–652. Published online 2024 Apr 5. doi: 10.1021/acsmedchemlett.4c00035

PMCID:: PMC11089555

Currently embargoed: Free in PMC on May 9, 2025

Structural Evaluations of a Selective Human STING^A230 Agonist and Its Use in Macrophage Immunotherapies

Zhichao Tang, Junxing Zhao, Ying Li, Shallu Tomer, Manikandan Selvaraju, Nicholas Tien, Diyun Sun, David K. Johnson, Anjie Zhen, Pingwei Li, Jingxin Wang

ACS Med Chem Lett. 2024 May 9; 15(5): 653–658. Published online 2024 Apr 12. doi: 10.1021/acsmedchemlett.4c00048

PMCID:: PMC11089548

Currently embargoed: Free in PMC on May 9, 2025

Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders

Jian Chen, Wentao Zhu, Wenqian Zhang, Yichen Tong, Fang Xu, Jiyan Pang

ACS Med Chem Lett. 2024 May 9; 15(5): 659–666. Published online 2024 Apr 30. doi: 10.1021/acsmedchemlett.4c00065

PMCID:: PMC11089551

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Synthesis of Monofluorinated 7-Hydroxycoumarin-3-Carboxamides as Cell-Permeable Fluorescent Molecular Probes

Digamber Rane, Anver Basha Shaik, Szu Lee, Xiaojun Hu, Blake R. Peterson

ACS Med Chem Lett. 2024 May 9; 15(5): 677–683. Published online 2024 Apr 15. doi: 10.1021/acsmedchemlett.4c00085

PMCID:: PMC11089655

Currently embargoed: Free in PMC on May 9, 2025

Discovery of Novel Bicyclic Pyrazoles as Potent PIP5K1C Inhibitors

Koji Ochiai, Shigeki Seto, Masanobu Yajima, Ryosuke Namie, Noriaki Hashimoto, Motomichi Fujita, Akinobu Yokoyama, Takahiro Suezawa, Hitomi Matsui, Satoshi Tomizawa, Yuji Ishibashi, Yuta Tanaka, Miho Yajima, Michiaki Nagasawa, Naoki Ando

ACS Med Chem Lett. 2024 May 9; 15(5): 684–690. Published online 2024 Apr 3. doi: 10.1021/acsmedchemlett.4c00090

PMCID:: PMC11089562

Currently embargoed: Free in PMC on May 9, 2025

Efficient Radiolabeling of Proteins and Antibodies via Maleamate–Cysteine Bioconjugation

Sajid Mushtaq, Kyo Chul Lee, Ji Ae Park, Jung Young Kim

ACS Med Chem Lett. 2024 May 9; 15(5): 691–695. Published online 2024 Apr 10. doi: 10.1021/acsmedchemlett.4c00092

PMCID:: PMC11089560

Currently embargoed: Free in PMC on May 9, 2025

Structure–Activity Relationship Study of Biselyngbyolide B Reveals Mitochondrial Fission-Induced Cytotoxicity in Cancer

Pratiti Mandal, Debobrata Paul, Himangshu Sharma, Sanu Saha, Partha Chakrabarti, Rajib Kumar Goswami

ACS Med Chem Lett. 2024 May 9; 15(5): 696–705. Published online 2024 Apr 19. doi: 10.1021/acsmedchemlett.4c00094

PMCID:: PMC11089557

Currently embargoed: Free in PMC on May 9, 2025

Synthesis and in Vitro Evaluation of CAPE Derivatives as Ferroptosis Inducers in Triple Negative Breast Cancer

Valeria Consoli, Antonino N. Fallica, Nicola F. Virzì, Loredana Salerno, Sebastiano Intagliata, Valeria Sorrenti, Khaled Greish, Alessandro Giuffrida, Luca Vanella, Valeria Pittalà

ACS Med Chem Lett. 2024 May 9; 15(5): 706–713. Published online 2024 Apr 30. doi: 10.1021/acsmedchemlett.4c00099

PMCID:: PMC11089544

Currently embargoed: Free in PMC on May 9, 2025

A Tiny Pocket Packs a Punch: Leveraging Pyridones for the Discovery of CNS-Penetrant Aza-indazole IRAK4 Inhibitors

Philippe N. Bolduc, Magnus Pfaffenbach, Ryan Evans, Zhili Xin, Kate L. Henry, Fang Gao, Terry Fang, John Silbereis, Jorge Vera Rebollar, Pei Li, Jayanth V Chodaparambil, Claire Metrick, Emily A. Peterson

ACS Med Chem Lett. 2024 May 9; 15(5): 714–721. Published online 2024 Apr 26. doi: 10.1021/acsmedchemlett.4c00102

PMCID:: PMC11089553

Currently embargoed: Free in PMC on May 9, 2025

Identification of Selective Imidazopyridine CSF1R Inhibitors

John L. Kane, Jr., Gary Asmussen, Joseph Batchelor, Mandy Cromwell, Malika Fezoui, Maria Fitzgerald, Barret Giese, Tatiana Gladysheva, Stephanie Holley, Kelly Keefe, Michael Kothe, Becky Lam, Sungtaek Lim, Jinyu Liu, Liang Ma, Markus Metz, Andrew A. Scholte, Patrick Shum, LinLi Wei, Lisa Woodworth, Andrea Edling

ACS Med Chem Lett. 2024 May 9; 15(5): 722–730. Published online 2024 Apr 30. doi: 10.1021/acsmedchemlett.4c00110

PMCID:: PMC11089549

Currently embargoed: Free in PMC on May 9, 2025

Note

Intracellular Pharmacokinetics of Activated Drugs in a Prodrug–Enzyme–Ultrasound System: Evaluations on ZD2767P+CPG2+US

Tinghe Yu, Xinya Li, Tianran Yu, Mengjie Chen, Yong Sun, Rui Ran

ACS Med Chem Lett. 2024 May 9; 15(5): 739–745. Published online 2024 Apr 4. doi: 10.1021/acsmedchemlett.4c00071

PMCID:: PMC11089658

Currently embargoed: Free in PMC on May 9, 2025

Patent Highlight

Novel Myeloperoxidase Inhibitors for Treating Multiple Diseases

Ram W. Sabnis

ACS Med Chem Lett. 2024 May 9; 15(5): 569–570. Published online 2024 Apr 11. doi: 10.1021/acsmedchemlett.4c00133

PMCID:: PMC11089653

Currently embargoed: Free in PMC on May 9, 2025

Novel CD73 Inhibitors for Treating Cancer

Ram W. Sabnis

ACS Med Chem Lett. 2024 May 9; 15(5): 571–572. Published online 2024 Apr 9. doi: 10.1021/acsmedchemlett.4c00137

PMCID:: PMC11089543

Currently embargoed: Free in PMC on May 9, 2025

Transforming Therapeutic Approaches with PROTAC Technology: New Targets and Potentials

Robert B. Kargbo

ACS Med Chem Lett. 2024 May 9; 15(5): 573–575. Published online 2024 Apr 26. doi: 10.1021/acsmedchemlett.4c00165

PMCID:: PMC11089660

Currently embargoed: Free in PMC on May 9, 2025

Expanding TPD Horizons: Innovative Strategies Targeting BCL6 and SMARCA2

Robert B. Kargbo

ACS Med Chem Lett. 2024 May 9; 15(5): 576–578. Published online 2024 Apr 26. doi: 10.1021/acsmedchemlett.4c00166

PMCID:: PMC11089547

Currently embargoed: Free in PMC on May 9, 2025

Novel Exatecan-Derived Topoisomerase-1 Inhibitors for Treating Cancer

Ram W. Sabnis

ACS Med Chem Lett. 2024 May 9; 15(5): 579–580. Published online 2024 Apr 26. doi: 10.1021/acsmedchemlett.4c00168

PMCID:: PMC11089550

Currently embargoed: Free in PMC on May 9, 2025

Pyrrolidinone Derivatives as NIK Inhibitors for Treating Autoimmune and Inflammatory Diseases

Ram W. Sabnis

ACS Med Chem Lett. 2024 May 9; 15(5): 581–582. Published online 2024 Apr 23. doi: 10.1021/acsmedchemlett.4c00169

PMCID:: PMC11089656

Currently embargoed: Free in PMC on May 9, 2025

Technical Note

Fitting of k_inact and K_I Values from Endpoint Pre-incubation IC₅₀ Data

Lavleen K. Mader, Jeffrey W. Keillor

ACS Med Chem Lett. 2024 May 9; 15(5): 731–738. Published online 2024 Apr 4. doi: 10.1021/acsmedchemlett.4c00054

PMCID:: PMC11089659

Currently embargoed: Free in PMC on May 9, 2025

Articles from ACS Medicinal Chemistry Letters are provided here courtesy of American Chemical Society