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Novel Nonpeptide as Oxytocin Receptor Agonist 新型非肽作为催产素受体激动剂
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-21 DOI: 10.1021/acsmedchemlett.5c0019110.1021/acsmedchemlett.5c00191
Yinlong Li,  and , Steven H. Liang*, 
{"title":"Novel Nonpeptide as Oxytocin Receptor Agonist","authors":"Yinlong Li,&nbsp; and ,&nbsp;Steven H. Liang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0019110.1021/acsmedchemlett.5c00191","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00191https://doi.org/10.1021/acsmedchemlett.5c00191","url":null,"abstract":"<p >This highlight describes a series of novel 1,4-benzodiazepine-based nonpeptides as oxytocin receptor (OT) agonists. The reported compounds demonstrate enhanced potency and selectivity compared to reference compounds, warranting further investigation for potential therapeutic applications in the treatment of OT-related pathologies.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"750–751 750–751"},"PeriodicalIF":3.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917115","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 Sulfonamide Derivatives as Nav1.5 Sodium Channel Blockers for Treating Atrial Fibrillation 新型磺胺衍生物作为Nav1.5钠通道阻滞剂治疗心房颤动
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-21 DOI: 10.1021/acsmedchemlett.5c0019210.1021/acsmedchemlett.5c00192
Siyan Feng,  and , Steven H. Liang*, 
{"title":"Novel Sulfonamide Derivatives as Nav1.5 Sodium Channel Blockers for Treating Atrial Fibrillation","authors":"Siyan Feng,&nbsp; and ,&nbsp;Steven H. Liang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0019210.1021/acsmedchemlett.5c00192","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00192https://doi.org/10.1021/acsmedchemlett.5c00192","url":null,"abstract":"<p >This highlight describes a novel class of sulfonamide-based Nav1.5 sodium channel blockers. These compounds preferentially inhibit Nav1.5 in atrial cardiomyocytes, extending the effective refractory period and preventing arrhythmic, rapid contraction of the atria. The novel Nav1.5 blockers possess the potential to treat Atrial Fibrillation without affecting the function of the rest of the heart.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"748–749 748–749"},"PeriodicalIF":3.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917132","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 Pyrrolidinone Urea as FPR2 Agonists for Treating Atherosclerosis and Heart Failure. 新型吡咯烷酮脲作为FPR2激动剂治疗动脉粥样硬化和心力衰竭。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-21 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00196
Ram W Sabnis
{"title":"Novel Pyrrolidinone Urea as FPR2 Agonists for Treating Atherosclerosis and Heart Failure.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.5c00196","DOIUrl":"10.1021/acsmedchemlett.5c00196","url":null,"abstract":"<p><p>Provided herein are novel pyrrolidinone urea as FPR2 agonists, pharmaceutical compositions, use of such compounds in treating atherosclerosis and heart failure, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"756-757"},"PeriodicalIF":3.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067104/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143952924","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Tetrahydrobenzo[b]pyrazolo[3,4-e][1,4]diazepine Compounds as Oxytocin Receptor Agonists for Treating Autism Spectrum Disorders. 新型四氢苯并[b]吡唑啉[3,4-e][1,4]二氮卓类化合物治疗自闭症谱系障碍的催产素受体激动剂。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-21 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00190
Zhendong Song, Steven H Liang
{"title":"Novel Tetrahydrobenzo[<i>b</i>]pyrazolo[3,4-<i>e</i>][1,4]diazepine Compounds as Oxytocin Receptor Agonists for Treating Autism Spectrum Disorders.","authors":"Zhendong Song, Steven H Liang","doi":"10.1021/acsmedchemlett.5c00190","DOIUrl":"10.1021/acsmedchemlett.5c00190","url":null,"abstract":"<p><p>The present invention reveals a series of novel nonpeptidergic compounds as oxytocin receptor (OT-R) agonists. These agonists, featuring a tetrahydrobenzo[<i>b</i>]pyrazolo[3,4-<i>e</i>][1,4]diazepine scaffold, hold the therapeutic potential for the treatment of autism spectrum disorders.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"752-753"},"PeriodicalIF":3.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067140/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144007243","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Marine-Inspired Multifaceted DNA Damaging Spirooxindoles Combating NSCLC and Associated Bacterial Infection. 抗非小细胞肺癌和相关细菌感染的海洋多面DNA损伤螺菌吲哚的合成。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-18 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00014
Mohammad Shahidul Islam, Assem Barakat, Abdul Majeed Abdullah Alayyaf, Matti Haukka, Ved Prakash Verma, Marwa M Abu-Serie, Amira F El-Yazbi, Michael G Shehat, Mustafa Alseqely, Mohamed Teleb
{"title":"Synthesis of Marine-Inspired Multifaceted DNA Damaging Spirooxindoles Combating NSCLC and Associated Bacterial Infection.","authors":"Mohammad Shahidul Islam, Assem Barakat, Abdul Majeed Abdullah Alayyaf, Matti Haukka, Ved Prakash Verma, Marwa M Abu-Serie, Amira F El-Yazbi, Michael G Shehat, Mustafa Alseqely, Mohamed Teleb","doi":"10.1021/acsmedchemlett.5c00014","DOIUrl":"10.1021/acsmedchemlett.5c00014","url":null,"abstract":"<p><p>Targeted therapeutics have gained prominence in combating non-small cell lung carcinoma (NSCLC) and opportunistic bacterial infections like <i>Staphylococcus aureus</i> (<i>S. aureus</i>). This study explores dual-acting marine-inspired spirooxindoles to limit NSCLC and opportunistic bacteria. Pharmacophoric motifs from antitumor and antibacterial marine products were merged into a new series of pyrazole-clubbed spirooxindoles via a stereoselective [3 + 2] cycloaddition reaction. MTT screening identified <b>4e</b>, <b>4i</b>, and <b>4p</b>-<b>4s</b> as potent cytotoxic agents, with <b>4p</b> showing exceptional activity (IC<sub>50</sub> = 0.042 μM) and tumor selectivity (SI = 58.28). <b>4p</b> exhibited antibacterial efficacy against <i>S. aureus</i> (MIC = 25 μg/mL). DNA damage studies using a terbium(III) chloride biosensor revealed <b>4p</b>'s ability to damage both calf thymus and <i>S. aureus</i> DNA at low concentrations. Docking simulations presumed that <b>4p</b> binds between DNA strands, while apoptosis studies indicated it induced G1/S phase cell cycle arrest and increased A549 apoptosis by 33.65%. These findings highlight <b>4p</b> as a promising lead for further studies.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"819-828"},"PeriodicalIF":3.5,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067117/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143953832","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Marine-Inspired Multifaceted DNA Damaging Spirooxindoles Combating NSCLC and Associated Bacterial Infection 抗非小细胞肺癌和相关细菌感染的海洋多面DNA损伤螺菌吲哚的合成
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-18 DOI: 10.1021/acsmedchemlett.5c0001410.1021/acsmedchemlett.5c00014
Mohammad Shahidul Islam, Assem Barakat*, Abdul Majeed Abdullah Alayyaf, Matti Haukka, Ved Prakash Verma, Marwa M. Abu-Serie, Amira F. El-Yazbi, Michael G. Shehat, Mustafa Alseqely and Mohamed Teleb*, 
{"title":"Synthesis of Marine-Inspired Multifaceted DNA Damaging Spirooxindoles Combating NSCLC and Associated Bacterial Infection","authors":"Mohammad Shahidul Islam,&nbsp;Assem Barakat*,&nbsp;Abdul Majeed Abdullah Alayyaf,&nbsp;Matti Haukka,&nbsp;Ved Prakash Verma,&nbsp;Marwa M. Abu-Serie,&nbsp;Amira F. El-Yazbi,&nbsp;Michael G. Shehat,&nbsp;Mustafa Alseqely and Mohamed Teleb*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0001410.1021/acsmedchemlett.5c00014","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00014https://doi.org/10.1021/acsmedchemlett.5c00014","url":null,"abstract":"<p >Targeted therapeutics have gained prominence in combating non-small cell lung carcinoma (NSCLC) and opportunistic bacterial infections like <i>Staphylococcus aureus</i> (<i>S. aureus</i>). This study explores dual-acting marine-inspired spirooxindoles to limit NSCLC and opportunistic bacteria. Pharmacophoric motifs from antitumor and antibacterial marine products were merged into a new series of pyrazole-clubbed spirooxindoles via a stereoselective [3 + 2] cycloaddition reaction. MTT screening identified <b>4e</b>, <b>4i</b>, and <b>4p</b>–<b>4s</b> as potent cytotoxic agents, with <b>4p</b> showing exceptional activity (IC<sub>50</sub> = 0.042 μM) and tumor selectivity (SI = 58.28). <b>4p</b> exhibited antibacterial efficacy against <i>S. aureus</i> (MIC = 25 μg/mL). DNA damage studies using a terbium(III) chloride biosensor revealed <b>4p</b>’s ability to damage both calf thymus and <i>S. aureus</i> DNA at low concentrations. Docking simulations presumed that <b>4p</b> binds between DNA strands, while apoptosis studies indicated it induced G1/S phase cell cycle arrest and increased A549 apoptosis by 33.65%. These findings highlight <b>4p</b> as a promising lead for further studies.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"819–828 819–828"},"PeriodicalIF":3.5,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917101","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 Isoxazolidines Derivatives as RIPK1 Inhibitors for Treating Neurodegenerative Diseases 新型异恶唑烷衍生物作为RIPK1抑制剂治疗神经退行性疾病
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-17 DOI: 10.1021/acsmedchemlett.5c0019710.1021/acsmedchemlett.5c00197
Ram W. Sabnis*, 
{"title":"Novel Isoxazolidines Derivatives as RIPK1 Inhibitors for Treating Neurodegenerative Diseases","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0019710.1021/acsmedchemlett.5c00197","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00197https://doi.org/10.1021/acsmedchemlett.5c00197","url":null,"abstract":"<p >Provided herein are novel isoxazolidines derivatives as RIPK1 inhibitors, pharmaceutical compositions, use of such compounds in treating neurodegenerative diseases, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"754–755 754–755"},"PeriodicalIF":3.5,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143916992","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 Isoxazolidines Derivatives as RIPK1 Inhibitors for Treating Neurodegenerative Diseases. 新型异恶唑烷衍生物作为RIPK1抑制剂治疗神经退行性疾病。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-17 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00197
Ram W Sabnis
{"title":"Novel Isoxazolidines Derivatives as RIPK1 Inhibitors for Treating Neurodegenerative Diseases.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.5c00197","DOIUrl":"10.1021/acsmedchemlett.5c00197","url":null,"abstract":"<p><p>Provided herein are novel isoxazolidines derivatives as RIPK1 inhibitors, pharmaceutical compositions, use of such compounds in treating neurodegenerative diseases, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"754-755"},"PeriodicalIF":3.5,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067113/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143951715","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
PDE7 as a Precision Target: Bridging Disease Modulation and Potential PET Imaging for Translational Medicine PDE7作为精确靶点：连接疾病调节和潜在的转化医学PET成像
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-15 DOI: 10.1021/acsmedchemlett.5c0016010.1021/acsmedchemlett.5c00160
Taoqian Zhao,  and , Steven H. Liang*, 
{"title":"PDE7 as a Precision Target: Bridging Disease Modulation and Potential PET Imaging for Translational Medicine","authors":"Taoqian Zhao,&nbsp; and ,&nbsp;Steven H. Liang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0016010.1021/acsmedchemlett.5c00160","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00160https://doi.org/10.1021/acsmedchemlett.5c00160","url":null,"abstract":"<p >Phosphodiesterase 7 (PDE7) regulates cAMP-PKA signaling and plays a crucial role in immune function, neuroprotection, and inflammation. Dysregulated PDE7 activity is linked to neurodegenerative, autoimmune, and metabolic disorders, making it a promising therapeutic target. Recent advancements in PDE7 inhibitors, particularly pyrimidinone-based compounds, have shown high selectivity and potent biological effects. Beyond therapeutics, radiolabeled PDE7 inhibitors offer potential for PET imaging, enabling noninvasive disease monitoring and treatment assessment.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"711–714 711–714"},"PeriodicalIF":3.5,"publicationDate":"2025-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/epdf/10.1021/acsmedchemlett.5c00160","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917055","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
PDE7 as a Precision Target: Bridging Disease Modulation and Potential PET Imaging for Translational Medicine. PDE7作为精确靶点：连接疾病调节和潜在的转化医学PET成像。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-15 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00160
Taoqian Zhao, Steven H Liang
{"title":"PDE7 as a Precision Target: Bridging Disease Modulation and Potential PET Imaging for Translational Medicine.","authors":"Taoqian Zhao, Steven H Liang","doi":"10.1021/acsmedchemlett.5c00160","DOIUrl":"10.1021/acsmedchemlett.5c00160","url":null,"abstract":"<p><p>Phosphodiesterase 7 (PDE7) regulates cAMP-PKA signaling and plays a crucial role in immune function, neuroprotection, and inflammation. Dysregulated PDE7 activity is linked to neurodegenerative, autoimmune, and metabolic disorders, making it a promising therapeutic target. Recent advancements in PDE7 inhibitors, particularly pyrimidinone-based compounds, have shown high selectivity and potent biological effects. Beyond therapeutics, radiolabeled PDE7 inhibitors offer potential for PET imaging, enabling noninvasive disease monitoring and treatment assessment.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"711-714"},"PeriodicalIF":3.5,"publicationDate":"2025-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067116/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143951220","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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