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Design, synthesis, and biological evaluation of novel benzimidazole derivatives as anti-cervical cancer agents through PI3K/Akt/mTOR pathway and tubulin inhibition Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-16 Si-Si Li, Jun-Jie Chen, Miao-Miao Zhang, Wei-Xu Wang, Wei-Yi Zhang, Cheng Ma
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Development of benzimidazole-based compounds as novel capsid assembly modulators for the treatment of HBV infection Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-16 Kaixin Du, Xianyang Wang, Yuxin Bai, Xue Zhang, Jie Xue, Shanshan Li, Youhua Xie, Zhipei Sang, Yu Tang, Xin Wang
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Data-oriented protein kinase drug discovery Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-15 Elena Xerxa, Jürgen Bajorath
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Novel selective agents for the degradation of AR/AR-V7 to treat advanced prostate cancer Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-15 Yifei Yang, Guangyao Lv, Ruijuan Xiu, Huijie Yang, Wenyan Wang, Pengfei Yu, Jianzhao Zhang, Liang Ye, Hongbo Wang, Jingwei Tian
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Exploration of isoxazole analogs: Synthesis, COX inhibition, anticancer screening, 3D multicellular tumor spheroids, and molecular modeling Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-15 Mohammed Hawash, Samer Abdallah, Mahmoud Abudayyak, Yarob Melhem, Mohammed Abu Shamat, Meera Aghbar, Irfan Çapan, Murad Abualhasan, Anil Kumar, Michał Kamiński, Tomasz Góral, Paulina Maria Dominiak, Shorooq Sobuh
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Discovery of novel amide derivatives as potent quorum sensing inhibitors of Pseudomonas aeruginosa Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-13 Zhe He, Ming-Ming Guan, Lan-Tu Xiong, Xuan Li, Yan Zeng, Xile Deng, Alastair N. Herron, Zi-Ning Cui
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Modulators for palmitoylation of proteins and small molecules Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-12 Zeshuai Fan, Yuchen Hao, Yidan Huo, Fei Cao, Longfei Li, Jianmei Xu, Yali Song, Kan Yang
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Quantum chemistry calculation-aided discovery of potent small-molecule mimics of glutathione peroxidases for the treatment of cisplatin-induced hearing loss Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-12 Wentao Wang, Siyu Qiu, Tianyi Zhang, Zhiwei Zheng, Kongkai Zhu, Xing Gao, Fengping Zhao, Xinyuan Ma, Hongyan Lin, Yingzi He, Canhui Zheng
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Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-12 Yubo Wang, Yulin Liu, Yan Zhang, Zixuan Zhang, Lei Xu, Jiefu Wang, Yijie Yang, Biyu Hu, Yuhong Yao, Mingming Wei, Junfeng Wang, Bencan Tang, Kun Zhang, Shuangwei Liu, Guang Yang
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Design, synthesis, and biological activity of D-bishomo-1α,25-dihydroxyvitamin D3 analogs and their crystal structures with the vitamin D nuclear receptor Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-10 Adrian Fabisiak, Pawel Brzeminski, Rafal R. Sicinski, Natacha Rochel, Ewa Maj, Beata Filip-Psurska, Joanna Wietrzyk, Lori A. Plum, Hector F. DeLuca
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Tetrazole derivatives in the management of neurological disorders: Recent advances on synthesis and pharmacological aspects Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-09 Shivangi Jaiswal, Kanika Verma, Jaya Dwivedi, Swapnil Sharma
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Research progress of fullerenes and their derivatives in the field of PDT Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-07 Xue Bai, Chungeng Dong, Xinle Shao, Faiz-Ur Rahman, Huifang Hao, Yongmin Zhang
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Quinoxaline derivatives: Recent discoveries and development strategies towards anticancer agents Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-07 Vincent Montero, Marc Montana, Manon Carré, Patrice Vanelle
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Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-07 Yue-Gao Hu, Narsaiah Battini, Bo Fang, Cheng-He Zhou
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Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-07 Shuangshuang Xiong, Ke Song, Hua Xiang, Guoshun Luo
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Opportunities and perspectives of small molecular phosphodiesterase inhibitors in neurodegenerative diseases Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-06 Qi Li, Qinghong Liao, Shulei Qi, He Huang, Siyu He, Weiping Lyu, Jinxin Liang, Huan Qin, Zimeng Cheng, Fan Yu, Xue Dong, Ziming Wang, Lingfei Han, Yantao Han
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8-Bicycloalkyl-CPFPX derivatives as potent and selective tools for in vivo imaging of the A1 adenosine receptor Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-06 Swen Humpert, Daniela Schneider, Dirk Bier, Annette Schulze, Felix Neumaier, Bernd Neumaier, Marcus Holschbach
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ML162 derivatives incorporating a naphthoquinone unit as ferroptosis/apoptosis inducers: Design, synthesis, anti-cancer activity, and drug-resistance reversal evaluation Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-06 Furong Ma, Yulong Li, Maohua Cai, Wenyan Yang, Zumei Wu, Jinyun Dong, Jiang-Jiang Qin
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Discovery of ganoderic acid A (GAA) PROTACs as MDM2 protein degraders for the treatment of breast cancer Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-06 Yan Li, Guangyu Li, Chenwei Zuo, Xiaolin Wang, Fang Han, Yi Jia, Hai Shang, Yu Tian
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Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-05 Jiamin Zheng, Zhisen Zhang, Xiaoyu Ding, Deheng Sun, Lihua Min, Feng Wang, Sujing Shi, Xin Cai, Man Zhang, Alex Aliper, Feng Ren, Xiao Ding, Alex Zhavoronkov
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Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-04 Giovanni Cervi, Roberto D'Alessio, Simona Bindi, Laura Buffa, Alessia Burocchi, Giulia Canevari, Michele Modugno, Ilaria Motto, Grazia Saturno, Paolo Orsini
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Active site-directed probes targeting dipeptidyl peptidases 8 and 9 Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-03 Margarida Espadinha, Joni De Loose, Sam Corthaut, Sofie Thys, Yentl Van Rymenant, Emile Verhulst, Siham Benramdane, Nicolò Filippi, Koen Augustyns, Pieter Van Wielendaele, Isabel Pintelon, Ingrid De Meester, Pieter Van der Veken
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Discovery of novel Thymol-TPP antibiotics that eradicate MRSA persisters Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-03 Ziyi Tang, Jizhou Feng, Mahesh Challa, Sankara Rao Rowthu, Shuxin Xiong, Cheng Zou, Jianguo Li, Chandra Shekhar Verma, Haibo Peng, Xiaoli He, Chao Huang, Yun He
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Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-02 Christopher R.M. Asquith, Michael P. East, Tuomo Laitinen, Carla Alamillo-Ferrer, Erkka Hartikainen, Carrow I. Wells, Alison D. Axtman, David H. Drewry, Graham J. Tizzard, Antti Poso, Timothy M. Willson, Gary L. Johnson
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Design, synthesis, anti-infective potency and mechanism study of novel Ru-based complexes containing substituted adamantane as antibacterial agents Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-02 Liqiang Wang, Lianghong Liu, Chunyan Zhang, Guangying Yu, Wenjing Lin, Xuemin Duan, Yanshi Xiong, Guijuan Jiang, Jintao Wang, Xiangwen Liao
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Synthesis and biological evaluation of 4-imidazolidinone–containing compounds as potent inhibitors of the MDM2/p53 interaction Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-02 Zhitong Lin, Chen Liu, Ziqin Yan, Jing Cheng, Xiancheng Wang, Feilong Zhou, Xilin Lyu, Shiyan Zhang, Daizhou Zhang, Xiangjing Meng, Yujun Zhao
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Advances in TRPV6 inhibitors for tumors by targeted therapies: Macromolecular proteins, synthetic small molecule compounds, and natural compounds Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-04-01 Weikang Liu, Wenwen Deng, Liqing Hu, Hui Zou
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Mono-quinoxaline-induced DNA structural alteration leads to ZBP1/RIP3/MLKL-driven necroptosis in cancer cells Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-31 Rimita Saha, Ritesh Pal, Bhaskar Ganguly, Bhim Majhi, Sanjay Dutta
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A series of indole-derived γ-hydroxy propiolate esters as potent anti-inflammatory agents: Design, synthesis, in-vitro and in-vivo biological studies Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-30 Maryam Akhtar, Luhao Lai, Ting Tian, Xu Zhang, Hao Cheng, Li Lin
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Schiff bases and their metal complexes to target and overcome (multidrug) resistance in cancer Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-29 Ana Podolski-Renić, Ana Čipak Gašparović, Andreia Valente, Óscar López, Julia H. Bormio Nunes, Christian R. Kowol, Petra Heffeter, Nenad R. Filipović
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Design, synthesis, and biological evaluation of first-in-class FABP1 inhibitors for the treatment of NASH Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-29 Ya Chen, Mingyang Yu, Lianru Chen, Jianming Mao, Wenxin Wang, Zhongcheng Yang, Zhijun Cao, Yuxia Liu, Min Wei, Luyong Zhang, Zheng Li
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Structure-based discovery of small molecule inhibitors of FKBP51-Hsp90 protein-protein interaction Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-28 Lisha Wang, Rajnish Kumar, Bengt Winblad, Pavel F. Pavlov
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An update on antibacterial AlkylGuanidino Ureas: Design of new derivatives, synergism with colistin and data analysis of the whole library Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-28 Claudia Ardino, Filomena Sannio, Giulio Poli, Salvatore Galati, Elena Dreassi, Lorenzo Botta, Jean-Denis Docquier, Ilaria D'Agostino
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Design, synthesis and biological evaluation of matrine contains benzimidazole derivatives as dual TOPOI and PARP inhibitors for cancer therapy Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-27 Gan Qiu, Junwei Xie, Fan Li, Keyan Han, Qingfeng Long, Jamal A.H. Kowah, Ruobing Gao, Lisheng Wang, Xu Liu
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Discovery of a novel homoisoflavonoid derivative 5g for anti-osteoclastic bone loss via targeting FGFR1 Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-27 Zhihao Chen, Alessandra Marie Encarnacion, Robin Prakash Sirvin Rajan, Hongyuan Yao, Sunwoo Lee, Eunae Kim, Tae-Hoon Lee
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Natural products as non-covalent and covalent modulators of the KEAP1/NRF2 pathway exerting antioxidant effects Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-26 Giulia Culletta, Brigitta Buttari, Marzia Arese, Simone Brogi, Anna Maria Almerico, Luciano Saso, Marco Tutone
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Targeting EGFR degradation by autophagosome degraders Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-26 ZhongFeng Zhu, Jiaying Li, Shujun Shen, Hawaa Al-furas, Shengrong Li, Yichen Tong, Yi Li, Yucheng Zeng, Qianyi Feng, Kaiyue Chen, Nan Ma, Fengtao Zhou, Zhang Zhang, Zhengqiu Li, Jiyan Pang, Ke Ding, Fang Xu
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Combining BNCT with carbonic anhydrase inhibition for mesothelioma treatment: Synthesis, in vitro, in vivo studies of ureidosulfamido carboranes Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-26 Alberto Lanfranco, Sahar Rakhshan, Diego Alberti, Polyssena Renzi, Ayda Zarechian, Nicoletta Protti, Saverio Altieri, Simonetta Geninatti Crich, Annamaria Deagostino
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Discovery of a triphenylamine-based ligand that targets mitochondrial DNA G-quadruplexes and activates the cGAS-STING immunomodulatory pathway Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-26 Xiao-Dong Wang, Yong-Si Liu, Meng-Die Chen, Ming-Hao Hu
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Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-25 William Nguyen, Coralie Boulet, Madeline G. Dans, Katie Loi, Kate E. Jarman, Gabrielle M. Watson, Wai-Hong Tham, Kate J. Fairhurst, Tomas Yeo, David A. Fidock, Sergio Wittlin, Mrittika Chowdury, Tania F. de Koning-Ward, Gong Chen, Dandan Yan, Susan A. Charman, Delphine Baud, Stephen Brand, Paul F. Jackson, Alan F. Cowman, Paul R. Gilson, Brad E. Sleebs
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Natural polyphenol: Their pathogenesis-targeting therapeutic potential in Alzheimer's disease Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-25 Chengu Niu, Miaoxian Dong, Yingcai Niu
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13-oxyingenol dodecanoate derivatives induce mitophagy and ferroptosis through targeting TMBIM6 as potential anti-NSCLC agents Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-24 Yaxu Wang, Liwei Gu, Jichong Li, Ruqi Wang, Yuan Zhuang, Xiangyun Li, Xinye Wang, Junzhe Zhang, Qingbo Liu, Jigang Wang, Shao-Jiang Song
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Discovery of pyrido[3,2-d]pyrimidin-6(5H)-one derivatives as checkpoint kinase 1 (CHK1) inhibitors with potent antitumor efficacy Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-24 Shihe Hu, Cuihua Jiang, Qiaomei Jin
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Insights into the development of 99mTc-radioligands for serotonergic receptors imaging: Synthesis, labeling, In vitro, and In vivo studies Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-23 Shahnaz Saednia, Saeed Emami, Masoud Moslehi, Seyed Jalal Hosseinimehr
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Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-23 Xing Zhao, Xuanyu Cao, Hongda Qiu, Weida Liang, Yinli Jiang, Qiang Wang, Weile Wang, Chengxi Li, Yang Li, Bowen Han, Keqi Tang, Lingling Zhao, Xuan Zhang, Xiao Wang, Hongze Liang
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Guanidine-to-piperidine switch affords high affinity small molecule NPFF ligands with preference for NPFF1-R and NPFF2-R subtypes Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-23 Kareem A. Galal, Samuel Obeng, Victoria L.C. Pallares, Alexandria Senetra, Maria A.B.L. Seabra, Ahmed Awad, Christopher R. McCurdy
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Drug development and potential targets for Cushing's syndrome Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-22 Wei Wei, Qianqian Xu, Liuyi Wu, Guangyue Gong, Yucheng Tian, Huidan Huang, Zhiyu Li
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Cajaninstilbene acid derivatives conjugated with siderophores of 3-hydroxypyridin-4(1H)-ones as novel antibacterial agents against Gram-negative bacteria based on the Trojan horse strategy Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-22 Yong-Jun Huang, Yi-Peng Zang, Li-Jun Peng, Ming-Han Yang, Jing Lin, Wei-Min Chen
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Synthesis and biological activity of thiophene bioisosteres of natural styryl lactone goniofufurone and related compounds Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-21 Mirjana Popsavin, Sanja Djokić, Ivana Kovačević, Slađana M. Stanisavljević, Vesna Kojić, Marko V. Rodić, Lidija Aleksić, Jelena Kesić, Bojana Srećo Zelenović, Velimir Popsavin, Dimitar S. Jakimov
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New strategies to hit hematological cancers Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-20 Marilia Barreca, Francesco Bertoni, Paola Barraja
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Novel 6-alkyl-bridged 4-arylalkylpiperazin-1-yl derivatives of azepino[4,3-b]indol-1(2H)-one as potent BChE-selective inhibitors showing protective effects against neurodegenerative insults Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-20 Francesco Samarelli, Rosa Purgatorio, Gianfranco Lopopolo, Caterina Deruvo, Marco Catto, Michael Andresini, Antonio Carrieri, Orazio Nicolotti, Annalisa De Palma, Daniela Valeria Miniero, Modesto de Candia, Cosimo D. Altomare
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Synthesis, kinase inhibition and anti-leukemic activities of diversely substituted indolopyrazolocarbazoles Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-20 Théo Frazier, Elisabeth Pereira, Reidun Aesoy, Lionel Nauton, Francis Giraud, Lars Herfindal, Fabrice Anizon, Pascale Moreau
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Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-20 Gang Sun, Zhiqi Feng, Yufan Kuang, Zhuoxin Fu, Yanyan Wang, Xing Zhao, Fengqin Wang, Hongbin Sun, Haoliang Yuan, Liang Dai
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Structure-based discovery of potent myosin inhibitors to guide antiparasite drug development Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-20 Xiaoping Tan, Shenye Qu, Guangshuo Wang, Gengrong Zhang, Tianqiang Liu, Fei Ling, Gaoxue Wang
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Radioprotective effectiveness of a novel delta-tocotrienol prodrug on mouse hematopoietic system against 60Co gamma-ray irradiation through inducing granulocyte-colony stimulating factor production Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-19 Zongchao Zuo, Limei Wang, Shaozheng Wang, Xinyu Liu, Dandan Wu, Zhangyi Ouyang, Ruoxi Meng, Yajun Shan, Shouguo Zhang, Tao Peng, Lin Wang, Zhongtang Li, Yuwen Cong
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Synthesis and biological evaluation of 1-phenyl-tetrahydro-β-carboline-based first dual PRMT5/EGFR inhibitors as potential anticancer agents Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-18 Juan Zhang, Xuliang Liu, Na Sa, Jin-He Zhang, Yong-Si Cai, Kai-Ming Wang, Wei Xu, Cheng-Shi Jiang, Kong-Kai Zhu
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Novel triterpenoid pyrones, phthalimides and phthalates are selectively cytotoxic in CCRF-CEM cancer cells – Synthesis, potency, and mitochondrial mechanism of action Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-18 Anna Kazakova, Ivo Frydrych, Nikola Jakubcová, Jan Pokorný, Barbora Lišková, Soňa Gurská, Petr Džubák, Marián Hajdúch, Milan Urban
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Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-18 Xiaodong Dou, Tongyu Huo, Yameng Liu, Zichen Pang, Lingyu Su, Xinyi Zhao, Xing Peng, Zhenming Liu, Liangren Zhang, Ning Jiao
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Synthetic approaches and clinical application of small-molecule inhibitors of sodium-dependent glucose transporters 2 for the treatment of type 2 diabetes mellitus Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-18 Tong Xie, Li-Jie Zhao
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Glucagon-like peptide-1 analogs: Miracle drugs are blooming? Eur. J. Med. Chem. (IF 6.7) Pub Date : 2024-03-17 Binbin Gong, Zhihong Yao, Chenxu Zhou, Wenxi Wang, Lidan Sun, Jing Han