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Crbn-based molecular Glues: Breakthroughs and perspectives Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-18 Juzeng An, Xiaojun Zhang
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Histone deacetylase (HDAC) inhibitor linker specificity determinants are preserved in a class of dual HDAC/non-covalent proteasome inhibitors Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-16 Alexandria M. Chan, Ashley Mitchell, Lena Grogan, Paul Shapiro, Steven Fletcher
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Rational design of prodrug-type apoB-targeted siRNA for nuclease resistance improvement without compromising gene silencing potency Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-15 Junsuke Hayashi, Yosuke Ochi, Kota Senpuku, Shun-ichi Wada, Fumito Wada, Mariko Harada-Shiba, Hidehito Urata
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Cryptic piperazine derivatives activated by knocking out the global regulator LaeA in Aspergillus flavipes Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-15 Yaping Liu, Pengkun Li, Changxing Qi, Ziou Zha, Jie Meng, Chang Liu, Jiapei Han, Qun Zhou, Zengwei Luo, Jianping Wang, Hucheng Zhu, Ying Ye, Chunmei Chen, Yuan Zhou, Yonghui Zhang
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Design, synthesis and biological evaluation of Nrf2 modulators for the treatment of glioblastoma multiforme Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-15 Huihui Yang, Peilu Song, Baohu Li, Shutang Li, Jinfei Yang
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Design, synthesis, and antiviral activity of 1-aryl-4-arylmethylpiperazine derivatives as Zika virus inhibitors with broad antiviral spectrum Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-12 Yingjie Ji, Lidan Wang, Rui Zhou, Xiaotang Yang, Siqi Li, Shan Cen, Yanping Li
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Inhibition of cancer cells by Quinoline-Based compounds: A review with mechanistic insights Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-12 Anjali Saxena, Suman Majee, Devalina Ray, Biswajit Saha
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Caged xanthone derivatives to promote mitochondria-mediated apoptosis in breast cancer cells Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-12 Youyi Wang, Huimin Zheng, Xue Jiang, Huaimo Wu, Yi Ren, Zhichao Xi, Changwu Zheng, Hongxi Xu
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Exploring novel pyrazole-nitroimidazole hybrids: Synthesis and antiprotozoal activity against the human pathogen trichomonas vaginalis Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-07 Rafaela Corrêa Silva, Anna De Freitas, Bruno Vicente, Victor Midlej, Maurício Silva dos Santos
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Discovery of 3-hydroxymethyl-azetidine derivatives as potent polymerase theta inhibitors Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-06 Yazhou Wang, Chao Wang, Jinxin Liu, Deheng Sun, Fanye Meng, Man Zhang, Alex Aliper, Feng Ren, Alex Zhavoronkov, Xiao Ding
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Casitas b cell lymphoma‑B (Cbl-b): A new therapeutic avenue for small-molecule immunotherapy Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-06 Xiuqi Hu, Erdong Li, Yangguo Zhou, Qidong You, Zhengyu Jiang
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Synthesis and biological activity of 11-Oxygenated and heterocyclic estrone analogs in pancreatic cancer monolayers and 3D spheroids Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-05 Khaled Alseud, Trevor Ostlund, Mikhail Durymanov, Joshua Reineke, Fathi Halaweish
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Novel naphthoquinone-1H-1,2,3-triazole hybrids: Design, synthesis and evaluation as inductors of ROS-mediated apoptosis in the MCF-7 cells Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-05 Acácio S. de Souza, Deborah S. Dias, Ruan C.B. Ribeiro, Dora C.S. Costa, Matheus G. de Moraes, David R. Pinho, Maria E.G. Masset, Laís M. Marins, Sandy P. Valle, Cláudio J.C. de Carvalho, Gustavo S.G. de Carvalho, Angélica Lauria N. Mello, Mauro Sola-Penna, Marcos V. Palmeira-Mello, Raissa A. Conceição, Carlos R. Rodrigues, Alessandra M.T. Souza, Luana da S.M. Forezi, Patricia Zancan, Vitor F. Ferreira
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Fluorescent probes and degraders of the sterol transport protein Aster-A Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-02 Nianzhe He, Laura Depta, Sonja Sievers, Luca Laraia
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A chemical magnet: Approaches to guide precise protein localization Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-02 Saurav Kumar, Behnam Nabet
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Discovery of LHF418 as a new potent SOS1 PROTAC degrader Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-02 Huifan Li, Minxue Chai, Yihan Chen, Fengtao Zhou, Xiaomei Ren, Jian Xu, Jian Wang, Zhen Wang, Weixue Huang
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Drug–drug conjugates of MEK and Akt inhibitors for RAS-mutant cancers Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-02 Hikaru Fujita, Sachiko Arai, Hiroshi Arakawa, Kana Hamamoto, Toshiyuki Kato, Tsubasa Arai, Nanaka Nitta, Kazuki Hotta, Natsuko Hosokawa, Takako Ohbayashi, Chiaki Takahashi, Yasuhide Inokuma, Ikumi Tamai, Seiji Yano, Munetaka Kunishima, Yoshihiro Watanabe
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Bioisoteres for carboxylic acids: From ionized isosteres to novel unionized replacements Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-01 Adrian Hall, Maria Chatzopoulou, James Frost
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Development of an oxazole-based cleavable linker for peptides Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-01 Elizabeth L. Taggart, Evan J. Wolff, Pamira Yanar, John P. Blobe, Christopher R. Shugrue
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Design, synthesis and antitumor activity of 2-substituted quinazoline-4-amine derivatives Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-01 Menghan Wang, Jia Yu, Xinyi Huang, Gang Yu, Qi Liang, Sha Cheng, Xueling Meng, Guangcan Xu, Huimin Li, Heng Luo, Bixue Xu
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Design, synthesis and anti-necroptosis activity of fused heterocyclic MLKL inhibitors Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-03-01 Yining Tang, Chunlin Zhuang
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Target fishing reveals PfPYK-1 and PfRab6 as potential targets of an antiplasmodial 4-anilino-2-trichloromethylquinazoline hit compound Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-28 C. Kieffer, N. Primas, S. Hutter, A. Merckx, L. Reininger, S. Bach, S. Ruchaud, F. Gaillard, M. Laget, D. Amrane, L. Hervé, C. Castera-Ducros, J. Renault, A. Dumètre, S. Rault, C. Doerig, P. Rathelot, P. Vanelle, N. Azas, P. Verhaeghe
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AGCM-22, a novel cetuximab-based EGFR-targeting antibody-drug-conjugate with highly selective anti-glioblastoma efficacy Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-27 Dapeng Li, Xianyan Sun, Yiquan Li, Chao Shang, Yuchao Dong, Renshuang Zhao, Hang Zhang, Zihao Wang, Shiyong Fan, Chengyuan Ma, Xiao Li
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Discovery of N-benzylbenzamide-based allosteric inhibitors of Aurora kinase A Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-27 Hyomin Lee, Euijung Kim, Narae Hwang, Jesik Yoo, Yunju Nam, Injeoung Hwang, Jin-Gyeong Park, Sang-Eun Park, Kyung-Sook Chung, Hwan Won Chung, Chiman Song, Mi-Jung Ji, Hyun-Mee Park, In-Kyun Lee, Kyung-Tae Lee, Eun Joo Roh, Wooyoung Hur
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Synthesis and biological evaluation of triazolones/oxadiazolones as novel urease inhibitors Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-25 Yi-Ning Wang, Su-Ya Li, Liang-Chao Yuan, Shu-Fang Bu, Yao Zeng, Zhu-Ping Xiao, Hai-Liang Zhu
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Assessing the rigidity of cubanes and bicyclo(1.1.1)pentanes as benzene bioisosteres Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-23 Graham Pattison
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Dipeptide-catalysed Michael reaction under physiological conditions: Examination of potential bioorthogonality Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-22 Florian Schuster, Benedikt W. Grau, Hong-Gui Xu, Andriy Mokhir, Svetlana B. Tsogoeva
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Research progress of LSD1-based dual-target agents for cancer therapy Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-21 X, i, a, o, j, u, a, n, , Y, a, n, g
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Multi-target potential of newly designed tacrine-derived cholinesterase inhibitors: Synthesis, computational and pharmacological study Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-18 Ivana I. Jevtić, Relja V. Suručić, Gordana Tovilović-Kovačević, Nevena Zogović, Slađana V. Kostić-Rajačić, Deana B. Andrić, Jelena Z. Penjišević
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Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-16 Seyed-Omar Zaraei, Wolfgang Dohle, Hanan S. Anbar, Randa El-Gamal, Bertrand Leblond, Paul A. Foster, Taleb H. Al-Tel, Barry V.L. Potter, Mohammed I. El-Gamal
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3-Amino-5,6,7,8-tetrahydrothieno[2,3-b]quinoline-2-carbonitrile: A fluorescent molecule that induces differentiation in PC12 cells Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-11 Kazuya Asao, Kento Sonoda, Shin-ichi Kawaguchi, Yoshinori Kawazoe
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Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for drug design Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-11 Chunjian Liu, Wei Wang, Jianxin Feng, Brett Beno, Thiruvenkadam Raja, Jacob Swidorski, Raju K.V.L.P. Manepalli, Muthalagu Vetrichelvan, Prasada Rao Jalagam, Satheesh K. Nair, Anuradha Gupta, Manoranjan Panda, Kaushik Ghosh, Jinal Kaushikkumar Shukla, Harinath Sale, Devang Shah, Shashyendra Singh Gautam, Dipal Patel, Arvind Mathur, Bruce A. Ellsworth, Dong Cheng, Alicia Regueiro-Ren
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Iodoetherification as a strategy towards sp3-rich scaffolds for drug discovery Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-10 Lydia Barnes, Timothy N. Birkinshaw, Aaron J. Senior, Oscar Siles Brügge, William Lewis, Stephen P. Argent, Christopher J. Moody, Andrew Nortcliffe
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Cationic lipids from multi-component Passerini reaction for non-viral gene delivery: A structure-activity relationship study Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-07 Jia-Jia Chen, Yu Guo, Rong Wang, Hui-Zhen Yang, Xiao-Qi Yu, Ji Zhang
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1,3-Disubstituted-1,2,4-triazin-6-ones with potent activity against androgen receptor-dependent prostate cancer cells Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-07 Shiting Zhao, Abdelsalam S. Ali, Xiaomin Liu, Zhiwei Yu, Xinyu Kong, Yan Zhang, G. Paul Savage, Yong Xu, Bin Lin, Donghai Wu, Craig L. Francis
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Discovery of novel MAT2A inhibitors by an allosteric site-compatible fragment growing approach Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-06 Feng Gao, Xiaoyu Ding, Zhongying Cao, Wei Zhu, Yaya Fan, Barbara Steurer, Hailong Wang, Xin Cai, Man Zhang, Alex Aliper, Feng Ren, Xiao Ding, Alex Zhavoronkov
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Design, synthesis, and biological evaluation of phenylcyclopropylamine-entinostat conjugates that selectively target cancer cells Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-05 Yosuke Ota, Yukihiro Itoh, Yuri Takada, Yasunobu Yamashita, Chenliang Hu, Mano Horinaka, Yoshihiro Sowa, Mitsuharu Masuda, Toshiyuki Sakai, Takayoshi Suzuki
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Structure-based design and optimization of a new class of small molecule inhibitors targeting the P-stalk binding pocket of ricin Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-05 Michael J. Rudolph, Arkajyoti Dutta, Anastasiia M. Tsymbal, John E. McLaughlin, Yang Chen, Simon A. Davis, Sophia A. Theodorous, Michael Pierce, Benjamin Algava, Xiaoyu Zhang, Zoltan Szekely, Jacques Y. Roberge, Xiao-Ping Li, Nilgun E. Tumer
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Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-01-29 Linda S. Barton, James F. Callahan, Juan Cantizani, Nestor O. Concha, Ignacio Cotillo Torrejon, Nicole C. Goodwin, Amruta Joshi-Pangu, Terry J. Kiesow, Jeff J. McAtee, Mark Mellinger, Christopher J. Nixon, Laura Padrón-Barthe, Jaclyn R. Patterson, Neil D. Pearson, Jeffrey J. Pouliot, Alan R. Rendina, Alexander Buitrago Santanilla, Jessica L. Schneck, Olalla Sanz, Reema K. Thalji, Bryan W. King
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Chemoenzymatic synthesis and immunological evaluation of sialyl-Thomsen-Friedenreich (sTF) antigen conjugate to CRM197 Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-03 Weizhao Weng, Sumei Ren, Changcai Teng, Jia Guo, Qiuyu Guo, Wei Zhang, Chengli Zong, Ning Ding
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Design of a novel long-acting dual GLP-1/GIP receptor agonist Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-03 Yuanzhen Dong, Jinhua Zhang, Hongjiang Xu, Hengqiao Shen, Qin Lu, Jun Feng, Zhengyan Cai
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Semisynthesis of segmentally isotope-labeled and site-specifically palmitoylated CD44 cytoplasmic tail Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-01-28 Dominik P. Vogl, Borja Mateos, Mario Migotti, Manuel Felkl, Anne C. Conibear, Robert Konrat, Christian F.W. Becker
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Design and synthesis 1H-Pyrrolo[2,3-b]pyridine derivatives as FLT3 inhibitors for the treatment of Acute myeloid Leukemia Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-02 Tian-Hua Wei, Yun Zhou, Jin Yang, Meng-Yuan Zhang, Jing-Jing Wang, Zhen-Jiang Tong, Jia-Zhen Wu, Yi-Bo Wang, Jiu-Kai Sha, Min Chen, Ning Ding, Yan-Cheng Yu, Wei-Chen Dai, Xue-Jiao Leng, Xin Xue, Shan-Liang Sun, Xiao-Long Wang, Nian-Guang Li, Zhi-Hao Shi
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The prognostic values of plasma desmosines, crosslinking molecules of elastic fibers, in the disease progression of Moyamoya disease Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-01 Ryosuke Tashiro, Riki Anzawa, Tomoo Inoue, Ayame Mikagi, Dan Ozaki, Keita Tominaga, Takashi Inoue, Tomohisa Ishida, Miki Fujimura, Toyonobu Usuki, Hidenori Endo, Kuniyasu Niizuma, Teiji Tominaga
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Colony Stimulating Factor-1 Receptor: An emerging target for neuroinflammation PET imaging and AD therapy Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-01 Anupriya Adhikari, Kanchan Chauhan, Manish Adhikari, Anjani K. Tiwari
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Discovery of novel biaryl benzoxazepinones as dual-mode receptor-interacting protein kinase-1 (RIPK1) inhibitors Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-01 YuFeng Xin, Pengcheng Dai, Hongming Shao, Chunlin Zhuang, Jiao Li
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Synthesis and biological evaluation of 1H-pyrrolo[3,2–g]isoquinolines Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-01 Mathilde Defois, Béatrice Josselin, Pierre Brindeau, Andreas Krämer, Stefan Knapp, Fabrice Anizon, Francis Giraud, Sandrine Ruchaud, Pascale Moreau
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Research progress on small molecule inhibitors targeting KRAS G12C with acrylamide structure and the strategies for solving KRAS inhibitor resistance Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-02-01 Zhiyan Jiang, Yan Li, Xin Zhou, Jie Wen, Pengwu Zheng, Wufu Zhu
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Synthesis of a fluorescent probe for measuring the activity of endo-β-N-acetylglucosaminidases recognizing hybrid-type N-glycans Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-01-27 Nozomi Ishii, Shusei Inoue, Kanae Sano, Satoshi Takahashi, Ichiro Matsuo
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N3-Methyluridine and 2′-O-Alkyl/2′-Fluoro-N3-methyluridine functionalized nucleic acids improve nuclease resistance while maintaining duplex geometry Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-01-28 Avijit Sahoo, Gourav Das, Atanu Ghosh, Siddharam Shivappa Bagale, Nishant Kumar Choudhary, S. Harikrishna, Surajit Sinha, Kiran R. Gore
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Discovery of small molecule benzothiazole and indole derivatives tackling tau 2N4R and a-synuclein fibrils Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-01-28 Ahmed A. Elbatrawy, Taiwo Ademoye, Heba Alnakhala, Arati Tripathi, Ashique Zami, Raluca Ostafe, Ulf Dettmer, Jessica S. Fortin
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Design, synthesis and evaluate of indazolylaminoquinazoline derivatives as potent Tropomyosin receptor kinase (TRK) inhibitors Bioorg. Med. Chem. (IF 3.5) Pub Date : 2024-01-20 Yunsheng Xu, Wei Zhao, Xinyi Zhang, Xihua Yu, Yinbo Chen, Zhenghai Wang, Yong Chu, Xueyan Zhu, Peng Zhang