Discovery of Novel 5,6-Dihydro‑4H‑pyrido[2,3,4-de]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases (English)
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In:
Journal of Medicinal Chemistry
;
67
, 7
;
5662-5682
;
2024
- Article (Journal) / Electronic Resource
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Title:Discovery of Novel 5,6-Dihydro‑4H‑pyrido[2,3,4-de]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases
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Additional title:J. Med. Chem.
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Contributors:Yang, Leifu ( author ) / Li, Yaxin ( author ) / Du, Yunling ( author ) / Guo, Yan ( author ) / Guo, Zhenke ( author ) / Liu, Baoxiu ( author ) / Liu, Jianglin ( author ) / Liu, Yanfei ( author ) / Niu, Hongdan ( author ) / Sun, Yueming ( author )
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Published in:Journal of Medicinal Chemistry ; 67, 7 ; 5662-5682
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Publisher:
- New search for: American Chemical Society
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Publication date:2024-04-11
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ISSN:
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Coden:
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DOI:
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Type of media:Article (Journal)
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Type of material:Electronic Resource
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Language:English
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Source:
Table of contents – Volume 67, Issue 7
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 5113
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DNA Adducts in Cancer ChemotherapyLi, Yupeng et al. | 2024
- 5144
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Recent Advances on Small-Molecule Inhibitors of Lipocalin-like ProteinsChen, Siliang / Pan, Zhaoping / Liu, Mingxia / Guo, Linghong / Jiang, Xian / He, Gu et al. | 2024
- 5168
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Medicinal Chemistry of Drugs with N‑Oxide FunctionalitiesKobus, Michelle / Friedrich, Timo / Zorn, Eilika / Burmeister, Nils / Maison, Wolfgang et al. | 2024
- 5185
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Recent Discovery and Development of Inhibitors that Target CDK9 and Their Therapeutic IndicationsZhang, Yuming / Shan, Lianhai / Tang, Wentao / Ge, Yating / Li, ChengXian / Zhang, Jifa et al. | 2024
- 5216
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Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-correctorPizzonero, Mathieu / Akkari, Rhalid / Bock, Xavier / Gosmini, Romain / De Lemos, Elsa / Duthion, Béranger / Newsome, Gregory / Mai, Thi-Thu-Trang / Roques, Virginie / Jary, Hélène et al. | 2024
- 5233
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Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory DiseasesPeixoto, Christophe / Joncour, Agnes / Temal-Laib, Taouès / Tirera, Amynata / Dos Santos, Aurélie / Jary, Hélène / Bucher, Denis / Laenen, Wendy / Pereira Fernandes, Anna / Lavazais, Stephanie et al. | 2024
- 5259
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Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase ActivatorThomson, Christopher G. / Aicher, Thomas D. / Cheng, Weiwei / Du, Hongwen / Dudgeon, Crissy / Li, An-Hu / Li, Baozhong / Lightcap, Eric / Luo, Diheng / Mulvihill, Mark et al. | 2024
- 5272
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CBP/p300 Degrader: A Promising Therapeutic Strategy for Treatment of Prostate Cancer and BeyondHu, Jiankang / Xu, Yong et al. | 2024
- 5275
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Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor RegressionChen, Zhixiang / Wang, Mi / Wu, Dimin / Bai, Longchuan / Xu, Tianfeng / Metwally, Hoda / Wang, Yu / McEachern, Donna / Zhao, Lijie / Li, Ruiting et al. | 2024
- 5305
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Discovery of Novel 11-Membered Templates as Squalene Synthase InhibitorsHaginoya, Noriyasu / Suzuki, Masanori / Suzuki, Makoto / Ishigai, Yutaka / Terayama, Koji / Kanda, Akira / Sugita, Kazuyuki et al. | 2024
- 5315
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Toward a Template for Synthetic Actin-Targeting Macrolide Analogues That Inhibit Cancer Cell InvasivenessTrofimova, Daria N. / Aeluri, Madhu / Veeranna, Kirana D. / Jiang, Yun / Grange, Rebecca L. / Pipaliya, Bhavin V. / Subaramanian, Murugan / Craig, Andrew W. / Evans, P. Andrew / Allingham, John S. et al. | 2024
- 5333
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Lead Compound Development of SRC‑3 Inhibitors with Improved Pharmacokinetic Properties and Anticancer EfficacyLu, Dong / Chen, Jianwei / Qin, Li / Bijou, Imani / Yi, Ping / Li, Feng / Song, Xianzhou / MacKenzie, Kevin R. / Yu, Xin / Yang, Bin et al. | 2024
- 5351
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Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate CancerChen, Zhixiang / Wang, Mi / Wu, Dimin / Zhao, Lijie / Metwally, Hoda / Jiang, Wei / Wang, Yu / Bai, Longchuan / McEachern, Donna / Luo, Jie et al. | 2024
- 5373
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Chimeric NOD2 Mincle Agonists as Vaccine AdjuvantsDangerfield, Emma M. / Ishizuka, Shigenari / Kodar, Kristel / Yamasaki, Sho / Timmer, Mattie S. M. / Stocker, Bridget L. et al. | 2024
- 5391
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Design, Synthesis, and Activity Evaluation of Fluorine-Containing Scopolamine Analogues as Potential AntidepressantsWang, Le / Zhu, Xushuo / Wang, Bo / Wang, Yijing / Wang, Mengqi / Yang, Shuping / Su, Chenhe / Chang, Junbiao / Zhu, Bo et al. | 2024
- 5421
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5‑Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein–Protein Interaction-Derived FunctionsPätsi, Henri T. / Kilpeläinen, Tommi P. / Jumppanen, Mikael / Uhari-Väänänen, Johanna / Wielendaele, Pieter Van / De Lorenzo, Francesca / Cui, Hengjing / Auno, Samuli / Saharinen, Janne / Seppälä, Erin et al. | 2024
- 5437
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Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of LymphomaYuan, Xinrui / Guan, Dezhong / Chen, Chao / Guo, Shi / Wu, Hanshu / Bu, Hong / Yang, Chao-Yie / Wang, Mian / Zhou, Jinpei / Zhang, Huibin et al. | 2024
- 5458
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Reinvent Aliphatic Arsenicals as Reversible Covalent Warheads toward Targeted Kinase Inhibition and Non-acute Promyelocytic Leukemia Cancer TreatmentZhao, Yang / Zhao, Xinyue / Duan, Lewei / Hou, Ruxue / Gu, Yuxin / Liu, Zhen / Chen, Jianbin / Wu, Feizhen / Yang, Limin / Le, X. Chris et al. | 2024
- 5473
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Combinatorial Ubiquitination REal-time PROteolysis (CURE-PROs): A Modular Platform for Generating Reversible, Self-Assembling Bifunctional Targeted DegradersGiardina, Sarah F. / Valdambrini, Elena / Singh, Pradeep K. / Bacolod, Manny D. / Babu-Karunakaran, Ganesh / Peel, Michael / Warren, J. David / Barany, Francis et al. | 2024
- 5502
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Discovery of 2,3-Dihydro[1,4]dioxino[2,3‑g]benzofuran Derivatives as Protease Activated Receptor 4 (PAR4) Antagonists with Potent Antiplatelet Aggregation Activity and Low Bleeding TendencyChen, Panpan / Chen, Cai / Zheng, Yizheng / Chen, Fangjun / Liu, Zhaojun / Ren, Shenhong / Song, Hangyu / Liu, Tongdan / Lu, Zhipeng / Sun, Hongbin et al. | 2024
- 5538
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Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional DegradersLucas, Simon C. C. / Ahmed, Afshan / Ashraf, S. Neha / Argyrou, Argyrides / Bauer, Matthias R. / De Donatis, Gian Marco / Demanze, Sylvain / Eisele, Frederik / Fusani, Lucia / Hock, Andreas et al. | 2024
- 5567
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Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate CancerXiao, Maoxu / Ha, Si / Zhu, Jiacheng / Tao, Wenxiang / Fu, Zixuan / Wei, Hanlin / Hou, Qiangqiang / Luo, Guoshun / Xiang, Hua et al. | 2024
- 5591
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Prevention of Metastasis by Suppression of Stemness Genes Using a Combination of microRNAsNevskaya, Kseniya V. / Pershina, Alexandra G. / Hmelevskaya, Ekaterina S. / Efimova, Lina V. / Ibragimova, Marina K. / Dolgasheva, Darya S. / Tsydenova, Irina A. / Ufandeev, Alexander A. / Buyko, Evgeny E. / Perina, Ekaterina A. et al. | 2024
- 5603
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Novel TLR4-Activating Vaccine Adjuvant Enhances the Production of Enterococcus faecium-binding AntibodiesFranco, Ana Rita / Sadones, Océane / Romerio, Alessio / Artusa, Valentina / Shaik, Mohammed Monsoor / Pasco, Samuel T. / Italia, Alice / D’Amato, Simona / Anguita, Juan / Huebner, Johannes et al. | 2024
- 5617
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Design, Synthesis, and Biological Evaluation of a Novel NIK Inhibitor with Anti-Inflammatory and Hepatoprotective Effects for Sepsis TreatmentZhang, Nanxia / Shen, Shige / Yang, Mengyu / He, Sijie / Liu, Chunxiao / Li, Hongmei / Lu, Tao / Liu, Haichun / Hu, Qinghua / Tang, Weifang et al. | 2024
- 5642
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Discovery and Optimization of Novel Nonbile Acid FXR Agonists as Preclinical Candidates for the Treatment of Inflammatory Bowel DiseaseLi, Yuan / Xu, Tingting / Zhao, Yue / Zhang, Hui / Liu, Zesheng / Wang, Hao / Huang, Chaoying / Shu, Zhihao / Gao, Lixin / Xie, Rongrong et al. | 2024
- 5662
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Discovery of Novel 5,6-Dihydro‑4H‑pyrido[2,3,4-de]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 KinasesYang, Leifu / Li, Yaxin / Du, Yunling / Guo, Yan / Guo, Zhenke / Liu, Baoxiu / Liu, Jianglin / Liu, Yanfei / Niu, Hongdan / Sun, Yueming et al. | 2024
- 5683
-
Beyond Rule of Five and PROTACs in Modern Drug Discovery: Polarity Reducers, Chameleonicity, and the Evolving Physicochemical LandscapePrice, Edward / Weinheimer, Manuel / Rivkin, Alexey / Jenkins, Gary / Nijsen, Marjoleen / Cox, Philip B. / DeGoey, David et al. | 2024
- 5699
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Targeting the CSF-1/CSF-1R Axis: Exploring the Potential of CSF1R Inhibitors in Neurodegenerative DiseasesBaek, Jihyun / Jun, Joonhong / Kim, Hyejin / Bae, Hyunah / Park, Haebeen / Cho, Hyunwook / Han, Songhee / Shin, Ho Chul / Hah, Jung-Mi et al. | 2024
- 5721
-
Design, Synthesis, and Biological Evaluation of 2‑Phenoxyalkylhydrazide Benzoxazole Derivatives as Quorum Sensing Inhibitors with Strong Antibiofilm EffectZhang, Panpan / Ma, Yangchun / Wang, Yingmei / Dong, Enhui / Ma, Shutao et al. | 2024
- 5744
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Developing a Copper(II) Isopropyl 2‑Pyridyl Ketone Thiosemicarbazone Compound Based on the IB Subdomain of Human Serum Albumin–Indomethacin Complex: Inhibiting Tumor Growth by Remodeling the Tumor MicroenvironmentMan, Xueyu / Li, Shanhe / Xu, Gang / Li, Wenjuan / Zhu, Minghui / Zhang, Zhenlei / Liang, Hong / Yang, Feng et al. | 2024
- 5758
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Discovery of DNL343: A Potent, Selective, and Brain-Penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative DiseasesCraig, Robert A. / De Vicente, Javier / Estrada, Anthony A. / Feng, Jianwen A. / Lexa, Katrina W. / Canet, Mark J. / Dowdle, William E. / Erickson, Rebecca I. / Flores, Brittany N. / Haddick, Patrick C. G. et al. | 2024
- 5783
-
Drug Repurposing of ACT001 to Discover Novel Promising Sulfide Prodrugs with Improved Safety and Potent Activity for Neutrophil-Mediated Antifungal ImmunotherapyLu, Xiangran / Wang, Rongrong / Yu, Yao / Wei, Jinlian / Xu, Yixiang / Zhou, Luoyifan / Mao, Fei / Li, Jian / Li, Xiaokang / Jia, Xinming et al. | 2024
- 5800
-
Discovery of Near-Infrared Heptamethine Cyanine Probes for Imaging-Guided Surgery in Solid TumorsLin, Qiao / Li, Changsheng / Wang, Yuhua / Zhu, Yanqing / Gu, Yueqing et al. | 2024
- 5813
-
Copper(II) Complexes with 2,2′:6′,2″-Terpyridine Derivatives Displaying Dimeric Dichloro−μ–Bridged Crystal Structure: Biological Activities from 2D and 3D Tumor Spheroids to In Vivo ModelsChoroba, Katarzyna / Machura, Barbara / Erfurt, Karol / Casimiro, Ana Rita / Cordeiro, Sandra / Baptista, Pedro V. / Fernandes, Alexandra R. et al. | 2024
- 5837
-
Discovery of a Potent, Selective, and Cell-Active SPIN1 InhibitorXiong, Yan / Greschik, Holger / Johansson, Catrine / Seifert, Ludwig / Gamble, Vicki / Park, Kwang-su / Fagan, Vincent / Li, Fengling / Chau, Irene / Vedadi, Masoud et al. | 2024
- 5854
-
Model of P‑Glycoprotein Ligand Binding and Validation with Efflux Substrate Matched PairsConrad, Jay / Paras, Nick A. / Vaz, Roy J. et al. | 2024
- 5866
-
Discovery of Novel Macrocyclic MERTK/AXL Dual InhibitorsKong, Deyu / Tian, Qiang / Chen, Zhilong / Zheng, Hongchao / Stashko, Michael A. / Yan, Dan / Earp, H. Shelton / Frye, Stephen V. / DeRyckere, Deborah / Kireev, Dmitri et al. | 2024
- 5883
-
Design of Novel 2‑Phenylquinazolin-4-amines as Selective CYP1B1 Inhibitors for Overcoming Paclitaxel Resistance in A549 CellsYang, Meixian / Yang, Fengyuan / Huang, Xinyue / Cai, Jiajing / Zhang, Yuxin / Jia, Jianhua / Qiu, Dachuan et al. | 2024
- 5902
-
Inhibition of NF-κB-Mediated Proinflammatory Transcription by Ru(II) Complexes of Anti-Angiogenic Ligands in Triple-Negative Breast CancerChakraborty, Ayan / Ghosh, Shilpendu / Chakraborty, Manas Pratim / Mukherjee, Sujato / Roy, Shantanu Saha / Das, Rahul / Acharya, Moulinath / Mukherjee, Arindam et al. | 2024
- 5924
-
Novel PET Imaging Probe for Quantitative Detection of Senescence In VivoXiang, Xin / Dong, Chuning / Zhou, Lianbo / Liu, Jun / Rabinowitz, Zachary M. / Zhang, Yuzhao / Guo, Honghui / He, Feng / Chen, Xingdou / Wang, Yunhua et al. | 2024
- 5935
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Long-Residence Time Peptide Antagonist for the Vasopressin V2 Receptor to Treat Autosomal Dominant Polycystic Kidney DiseaseXiong, Xiaochun / Wang, Naiyuan / Zhang, Yixiao / Zhao, Wenchao / Pang, Ningning / Fu, Kequan / Zhou, Nan / Zhou, Xueyan / Guo, Dong et al. | 2024
- 5945
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Amphiphilic α‑Peptoid-deoxynojirimycin Conjugate-based Multivalent Glycosidase Inhibitor for Hypoglycemic Effect and Fluorescence ImagingWang, Guang-Yuan / Yan, Dong-Xiao / Rong, Rui-Xue / Shi, Bing-Ye / Lin, Gao-Juan / Yin, Fangqian / Wei, Wen-Tong / Li, Xiao-Liu / Wang, Ke-Rang et al. | 2024
- 5957
-
Correction to “Rational Design of Bioorthogonally Activatable PROTAC for Tumor-Targeted Protein Degradation”Bi, Tao / Liang, Pan / Zhou, Yanan / Wang, Hong / Huang, Rui / Sun, Qin / Shen, Hongping / Yang, Sijin / Ren, Wei / Liu, Zengjin et al. | 2024
- 5958
-
Correction to “A Vancomycin-Templated DNA-Encoded Library for Combating Drug-Resistant Bacteria”Guan, Dongliang / Liu, Jiaxiang / Chen, Feifei / Li, Jian / Wang, Xiaowen / Lu, Weiwei / Suo, Yanrui / Tang, Feng / Lan, Lefu / Lu, Xiaojie et al. | 2024
- 5960
-
Correction to “Discovery of RORγ Allosteric Fluorescent Probes and Their Application: Fluorescence Polarization, Screening, and Bioimaging”Yu, Yan-Cheng / Tong, Zhen-Jiang / Liang, Xiao-Ting / Wu, Jia-Zhen / Xu, Yu-Jing / Wang, Jing-Jing / Zhang, Meng-Yuan / Wei, Tian-Hua / Yang, Jin / Wang, Yi-Bo et al. | 2024