ACS Medicinal Chemistry Letters最新文献

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In This Issue, Volume 15, Issue 7 本期,第 15 卷第 7 期
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-11 DOI: 10.1021/acsmedchemlett.4c00282
Andrew P. Riley*, 
{"title":"In This Issue, Volume 15, Issue 7","authors":"Andrew P. Riley*, ","doi":"10.1021/acsmedchemlett.4c00282","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00282","url":null,"abstract":"","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":3.5,"publicationDate":"2024-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141592642","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of Broad-Spectrum Herpes Antiviral Oxazolidinone Amide Derivatives and Their Structure–Activity Relationships 发现广谱抗疱疹病毒的噁唑烷酮酰胺衍生物及其结构-活性关系
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-09 DOI: 10.1021/acsmedchemlett.4c00117
Michael A. Plotkin, Marc Labroli, Jeffrey Schubert, Anthony Shaw, Kelly-Ann S. Schlegel, Richard Berger, Andrew J. Cooke, Robert P. Hayes, Kira A. Armacost, Keith Kinek, Paula Krosky, Christine Burlein, Shi Meng, Edward DiNunzio, Edward M. Murray, Sony Agrawal, Maria Madeira, Amy Flattery, Huifang Yao, Andrew Leithead, William A Rose, II, Christopher Cox, David M. Tellers, Philip M. McKenna, Izzat Raheem
{"title":"Discovery of Broad-Spectrum Herpes Antiviral Oxazolidinone Amide Derivatives and Their Structure–Activity Relationships","authors":"Michael A. Plotkin, Marc Labroli, Jeffrey Schubert, Anthony Shaw, Kelly-Ann S. Schlegel, Richard Berger, Andrew J. Cooke, Robert P. Hayes, Kira A. Armacost, Keith Kinek, Paula Krosky, Christine Burlein, Shi Meng, Edward DiNunzio, Edward M. Murray, Sony Agrawal, Maria Madeira, Amy Flattery, Huifang Yao, Andrew Leithead, William A Rose, II, Christopher Cox, David M. Tellers, Philip M. McKenna, Izzat Raheem","doi":"10.1021/acsmedchemlett.4c00117","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00117","url":null,"abstract":"Herpesvirus infections are ubiquitous, with over 95% of the adult population infected by at least one strain. While most of these infections resolve without treatment in healthy individuals, they can cause significant morbidity and mortality in immunocompromised, stem cell, or organ transplant patients. Current nucleoside standards of care provide meaningful benefit but are limited due to poor tolerability, resistance, and generally narrow spectrum of activity. Herpesviruses share a conserved DNA polymerase, the inhibition of which is validated as an effective strategy to disrupt viral replication. By utilizing a non-nucleoside inhibitor of the viral DNA polymerase, we sought to develop agents covering multiple herpesviruses (e.g., CMV, VZV, HSV1/2, EBV, and HHV6). Herein is described the invention of an oxazolidinone class of broad-spectrum non-nucleoside herpes antiviral inhibitors. A lead compound (<b>42</b>) with potent biochemical and broad-spectrum cellular activity was found to be efficacious in murine models against both HSV-1 and CMV infection.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141573608","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Imidazopyridine and Imidazopyridazine Derivatives as DGAT2 Inhibitors for Treating Multiple Diseases 作为 DGAT2 抑制剂治疗多种疾病的新型咪唑并哒嗪和咪唑并哒嗪衍生物
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-03 DOI: 10.1021/acsmedchemlett.4c00286
Ram W. Sabnis
{"title":"Novel Imidazopyridine and Imidazopyridazine Derivatives as DGAT2 Inhibitors for Treating Multiple Diseases","authors":"Ram W. Sabnis","doi":"10.1021/acsmedchemlett.4c00286","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00286","url":null,"abstract":"Provided herein are novel imidazopyridine and imidazopyridazine derivatives as DGAT2 inhibitors, pharmaceutical compositions, use of such compounds in treating multiple diseases, and processes for preparing such compounds.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141548288","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
AI Based Discovery of a New AKR1C3 Inhibitor for Anticancer Applications 基于人工智能发现新型 AKR1C3 抗癌抑制剂
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-03 DOI: 10.1021/acsmedchemlett.4c00150
Agnese C. Pippione, Chiara Vigato, Cristina Tucciarello, Samrina Hussain, Edoardo Salladini, Ha H. Truong, Niel M. Henriksen, Gaia Vanzetti, Giorgia Giordano, Daniele Zonari, Osman Asghar Mirza, Karla Frydenvang, Ymera Pignochino, Simonetta Oliaro-Bosso, Donatella Boschi, Marco L. Lolli
{"title":"AI Based Discovery of a New AKR1C3 Inhibitor for Anticancer Applications","authors":"Agnese C. Pippione, Chiara Vigato, Cristina Tucciarello, Samrina Hussain, Edoardo Salladini, Ha H. Truong, Niel M. Henriksen, Gaia Vanzetti, Giorgia Giordano, Daniele Zonari, Osman Asghar Mirza, Karla Frydenvang, Ymera Pignochino, Simonetta Oliaro-Bosso, Donatella Boschi, Marco L. Lolli","doi":"10.1021/acsmedchemlett.4c00150","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00150","url":null,"abstract":"AKR1C3 is an upregulated enzyme in prostate and other cancers; in addition to regulating hormone synthesis, this enzyme is thought to play a role in the aggressiveness of tumors and in the defense against drugs. We here used an unbiased method to discover new potent AKR1C3 inhibitors: through an AI-based virtual drug screen, compound <b>4</b> was identified as a potent and selective enzymatic inhibitor able to translate this activity into a pronounced antiproliferative effect in the 22RV1 prostate cancer cell model. As other known AKR1C3 inhibitors, compound <b>4</b> determined a significantly increased activity of abiraterone, a drug approved for advanced prostate cancer. Compound <b>4</b> also showed a synergic effect with doxorubicin in osteosarcoma cell lines; specifically, the effect is correlated with AKR1C3 expression. In this research work, therefore, the use of AI allowed the identification of a new structure as an AKR1C3 inhibitor and its potential to enhance the effect of chemotherapeutics.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141573609","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Chemical Probes to Investigate Central Nervous System Disorders: Design, Synthesis and Mechanism of Action of a Potent Human Serine Racemase Inhibitor 研究中枢神经系统疾病的化学探针:一种强效人丝氨酸消旋酶抑制剂的设计、合成及其作用机制
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-03 DOI: 10.1021/acsmedchemlett.4c00174
Francesco Marchesani, Francesca Rebecchi, Marco Pieroni, Serena Faggiano, Giannamaria Annunziato, Chiara Spaggiari, Stefano Bruno, Sofia Rinaldi, Roberta Giaccari, Gabriele Costantino, Barbara Campanini
{"title":"Chemical Probes to Investigate Central Nervous System Disorders: Design, Synthesis and Mechanism of Action of a Potent Human Serine Racemase Inhibitor","authors":"Francesco Marchesani, Francesca Rebecchi, Marco Pieroni, Serena Faggiano, Giannamaria Annunziato, Chiara Spaggiari, Stefano Bruno, Sofia Rinaldi, Roberta Giaccari, Gabriele Costantino, Barbara Campanini","doi":"10.1021/acsmedchemlett.4c00174","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00174","url":null,"abstract":"The intricate signaling network within the central nervous system (CNS) involving <i>N</i>-methyl-<span>d</span>-aspartate receptors (NMDARs) has been recognized as a key player in severe neurodegenerative diseases. The indirect modulation of NMDAR-mediated neurotransmission through inhibition of serine racemase (SR)─the enzyme responsible for the synthesis of the NMDAR coagonist <span>d</span>-serine─has been suggested as a therapeutic strategy to treat these conditions. Despite the inherent challenges posed by SR conformational flexibility, a ligand-based drug design strategy has successfully produced a series of potent covalent inhibitors structurally related to amino acid analogues. Among these inhibitors, O-(2-([1,1′-biphenyl]-4-yl)-1-carboxyethyl)hydroxylammonium chloride (<b>28</b>) has emerged as a valuable candidate with a <i>K</i><sub>d</sub> of about 5 μM, which makes it one of the most potent hSR inhibitors reported to date. This molecule is expected to inspire the identification of selective hSR inhibitors that might find applications as tools in the study and treatment of several CNS pathologies.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141548286","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Correction to “Novel Antiproliferative Chimeric Compounds with Marked Histone Deacetylase Inhibitory Activity” 对 "具有明显组蛋白去乙酰化酶抑制活性的新型抗增殖嵌合化合物 "的更正
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-03 DOI: 10.1021/acsmedchemlett.4c00301
Elisa Giacomini, Angela Nebbioso, Alfonso Ciotta, Cristina Ianni, Federico Falchi, Marinella Roberti, Manlio Tolomeo, Stefania Grimaudo, Antonietta Di Cristina, Rosaria Maria Pipitone, Lucia Altucci, Maurizio Recanatini
{"title":"Correction to “Novel Antiproliferative Chimeric Compounds with Marked Histone Deacetylase Inhibitory Activity”","authors":"Elisa Giacomini, Angela Nebbioso, Alfonso Ciotta, Cristina Ianni, Federico Falchi, Marinella Roberti, Manlio Tolomeo, Stefania Grimaudo, Antonietta Di Cristina, Rosaria Maria Pipitone, Lucia Altucci, Maurizio Recanatini","doi":"10.1021/acsmedchemlett.4c00301","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00301","url":null,"abstract":"Page 976. An error was found in the originally published version of Figure 3. The corrected figure is shown here.<named-content content-type=\"anchor\" r type=\"simple\"></named-content> Figure 3. Western blot analyses carried out for the indicated targets in U937 and MCF-7 cells after 24 h of treatment. ImageJ was used to quantify protein expression. Histone H1, H4 and ERKs indicate equal loading. SAHA and <i><b>trans</b></i><b>-6</b> were used at concentration of 5 μM. This article has not yet been cited by other publications. Figure 3. Western blot analyses carried out for the indicated targets in U937 and MCF-7 cells after 24 h of treatment. ImageJ was used to quantify protein expression. Histone H1, H4 and ERKs indicate equal loading. SAHA and <i><b>trans</b></i><b>-6</b> were used at concentration of 5 μM.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141521853","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Compounds as Orexin Receptor Agonists for Treating Sleep Disorders, Namely, Narcolepsy and Hypersomnia 作为奥列克素受体激动剂治疗睡眠障碍(即嗜睡症和失眠症)的新型化合物
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-03 DOI: 10.1021/acsmedchemlett.4c00285
Ram W. Sabnis
{"title":"Novel Compounds as Orexin Receptor Agonists for Treating Sleep Disorders, Namely, Narcolepsy and Hypersomnia","authors":"Ram W. Sabnis","doi":"10.1021/acsmedchemlett.4c00285","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00285","url":null,"abstract":"Provided herein are novel compounds as orexin receptor agonists, pharmaceutical compositions, use of such compounds in treating sleep disorders, namely, narcolepsy and hypersomnia, and processes for preparing such compounds.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141531684","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2 发现类似于细胞周期蛋白依赖性激酶 2 的化学探针并确定其特性
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-03 DOI: 10.1021/acsmedchemlett.4c00219
Frances M. Bashore, Sophia M. Min, Xiangrong Chen, Stefanie Howell, Caroline H. Rinderle, Gabriel Morel, Josie A. Silvaroli, Carrow I. Wells, Bruce A. Bunnell, David H. Drewry, Navjot S. Pabla, Sila K. Ultanir, Alex N. Bullock, Alison D. Axtman
{"title":"Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2","authors":"Frances M. Bashore, Sophia M. Min, Xiangrong Chen, Stefanie Howell, Caroline H. Rinderle, Gabriel Morel, Josie A. Silvaroli, Carrow I. Wells, Bruce A. Bunnell, David H. Drewry, Navjot S. Pabla, Sila K. Ultanir, Alex N. Bullock, Alison D. Axtman","doi":"10.1021/acsmedchemlett.4c00219","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00219","url":null,"abstract":"Acylaminoindazole-based inhibitors of CDKL2 were identified via analyses of cell-free binding and selectivity data. Compound <b>9</b> was selected as a CDKL2 chemical probe based on its potent inhibition of CDKL2 enzymatic activity, engagement of CDKL2 in cells, and excellent kinome-wide selectivity, especially when used in cells. Compound <b>16</b> was designed as a negative control to be used alongside compound <b>9</b> in experiments to interrogate CDKL2-mediated biology. A solved cocrystal structure of compound <b>9</b> bound to CDKL2 highlighted key interactions it makes within its ATP-binding site. Inhibition of downstream phosphorylation of EB2, a CDKL2 substrate, in rat primary neurons provided evidence that engagement of CDKL2 by compound <b>9</b> in cells resulted in inhibition of its activity. When used at relevant concentrations, compound <b>9</b> does not impact the viability of rat primary neurons or certain breast cancer cells nor elicit consistent changes in the expression of proteins involved in epithelial–mesenchymal transition.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141521971","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of VU6008677: A Structurally Distinct Tricyclic M4 Positive Allosteric Modulator with Improved CYP450 Profile 发现 VU6008677:一种结构独特的三环 M4 阳性异构调节剂,具有更好的 CYP450 特征
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-03 DOI: 10.1021/acsmedchemlett.4c00249
Rory A. Capstick, Sean R. Bollinger, Julie L. Engers, Madeline F. Long, Sichen Chang, Vincent B. Luscombe, Alice L. Rodriguez, Colleen M. Niswender, Thomas M. Bridges, Olivier Boutaud, P. Jeffrey Conn, Darren W. Engers, Craig W. Lindsley, Kayla J. Temple
{"title":"Discovery of VU6008677: A Structurally Distinct Tricyclic M4 Positive Allosteric Modulator with Improved CYP450 Profile","authors":"Rory A. Capstick, Sean R. Bollinger, Julie L. Engers, Madeline F. Long, Sichen Chang, Vincent B. Luscombe, Alice L. Rodriguez, Colleen M. Niswender, Thomas M. Bridges, Olivier Boutaud, P. Jeffrey Conn, Darren W. Engers, Craig W. Lindsley, Kayla J. Temple","doi":"10.1021/acsmedchemlett.4c00249","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00249","url":null,"abstract":"This Letter details our efforts to develop novel tricyclic muscarinic acetylcholine receptor subtype 4 (M<sub>4</sub>) positive allosteric modulator (PAM) scaffolds with improved pharmacological properties. This endeavor involved a “tie-back” strategy to replace the 3-amino-5-chloro-4,6-dimethylthieno[2,3-<i>b</i>]pyridine-2-carboxamide core, which led to the discovery of two novel tricyclic cores: an 8-chloro-9-methylpyrido[3′,2′:4,5]thieno[3,2-<i>d</i>]pyrimidin-4-amine core and 8-chloro-7,9-dimethylpyrido[3′,2′:4,5]furo[3,2-<i>d</i>]pyrimidin-4-amine core. Both tricyclic cores displayed low nanomolar potency against human M<sub>4</sub> and greatly reduced cytochrome P450 inhibition when compared with parent compound <b>ML253</b>.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141548287","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
TRPA1 Inhibition Effects by 3-Phenylcoumarin Derivatives 3- 苯基香豆素衍生物对 TRPA1 的抑制作用
IF 4.2 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2024-07-02 DOI: 10.1021/acsmedchemlett.4c00072
Carita Sallomy, Paul Awolade, Minna Rahnasto-Rilla, Mari Hämäläinen, Liisa P. Nousiainen, Niklas G. Johansson, Sanna Hiltunen, Petri Turhanen, Eeva Moilanen, Maija Lahtela-Kakkonen, Juri M. Timonen
{"title":"TRPA1 Inhibition Effects by 3-Phenylcoumarin Derivatives","authors":"Carita Sallomy, Paul Awolade, Minna Rahnasto-Rilla, Mari Hämäläinen, Liisa P. Nousiainen, Niklas G. Johansson, Sanna Hiltunen, Petri Turhanen, Eeva Moilanen, Maija Lahtela-Kakkonen, Juri M. Timonen","doi":"10.1021/acsmedchemlett.4c00072","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00072","url":null,"abstract":"Transient receptor potential ankyrin 1 (TRPA1) protein plays an important role in the inflammatory response, and it has been associated with different pain conditions and pain-related diseases, making TRPA1 a valid target for painkillers. In this study, we identified potential TRPA1 inhibitors and located their binding sites utilizing computer-aided drug design (CADD) techniques. The designed 3-phenylcoumarin-based TRPA1 inhibitors were successfully synthesized using a microwave assisted synthetic strategy. 3-(3-Bromophenyl)-7-acetoxycoumarin (<b>5</b>), 7-hydroxy-3-(3-hydroxyphenyl)coumarin (<b>12</b>) and 3-(3-hydroxyphenyl)coumarin (<b>23</b>) all showed inhibitory activity toward TRPA1 <i>in vitro</i>. Compound <b>5</b> also decreased the size and formation of breast cancer cells. Hence, targeting TRPA1 may represent a promising alternative for the treatment of pain and inflammation.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":null,"pages":null},"PeriodicalIF":4.2,"publicationDate":"2024-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141531683","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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