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An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting Mpro Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-19 Jing Zhang, Lili Zhao, Yuxin Bai, Shanshan Li, Meifang Zhang, Bo Wei, Xianyang Wang, Yan Xue, Li Li, Guiliang Ma, Yu Tang, Xin Wang
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Hydrazyl hydroxycoumarins as new potential conquerors towards Pseudomonas aeruginosa Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-15 Jiang-Sheng Zhao, Nisar Ahmad, Shuo Li, Cheng-He Zhou
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Synthesis, biological evaluation and molecular docking study of pyrimidine linked thiazolidinedione derivatives as potential antimicrobial and antitubercular agents Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-15 M.S. Raghu, C.B. Pradeep Kumar, K Yogesh Kumar, M.K. Prashanth, Fahd Alharethy, Byong-Hun Jeon
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C3-Symmetric ligands in drug design: An overview of the challenges and opportunities ahead Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-13 Maha A. Alshubramy, Faez S. Alotaibi, Hamad M. Alkahtani, Khalid A. Alamry, Mahmoud A. Hussein
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Synthesis and biological evaluation of hydantoin derivatives as potent antiplasmodial agents Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-12 Ee-Zhen Chin, Wei-Jin Chang, Hui-Yin Tan, Sook Yee Liew, Yee-Ling Lau, Yee-Ling Ng, Mohd Azlan Nafiah, Thomas Kurz, Siow-Ping Tan
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Novel ether derivatives of 11-azaartemisinins with high order antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-12 Komal Rathi, Mohammad Hassam, Chandan Singh, Sunil K. Puri, Jawahar L. Jat, Ved Prakash Verma
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Design, synthesis, α-amylase and glucose diffusion inhibition, and molecular docking studies of new indenopyrazolones bearing benzothiazole derivatives Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-05 Ravinder Punia, Satbir Mor, Suchita Sindhu, Deepak Kumar, Priyanku Pradip Das, Deepak Kumar Jindal, Ashwani Kumar, Rajni Mohil, Komal Jakhar
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Synthesis and biological evaluation of radioiodinated benzoxazole and benzothiazole derivatives for imaging myelin in multiple sclerosis Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-05 Hiroyuki Watanabe, Miho Ikawa, Masashi Kakae, Hisashi Shirakawa, Shuji Kaneko, Masahiro Ono
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Identification of two novel chemical classes of Autotaxin (ATX) inhibitors using Enalos Asclepios KNIME nodes Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-05 Elli-Anna Stylianaki, Varnavas D. Mouchlis, Christiana Magkrioti, Konstantinos D. Papavasileiou, Antreas Afantitis, Alexios N. Matralis, Vassilis Aidinis
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Self-assembly of amphiphilic helical-coiled peptide nanofibers and inhibition of fibril formation with curcumin Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-01 Grace Daniel, George Hilan, Lisa Ploeg, David Sabatino
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2-(3-Indolyl)acetamides and their oxazoline analogues: Anticancer SAR study Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-01 Dmitrii A. Aksenov, Jadyn L. Smith, Alexander V. Aksenov, Lidiya A. Prityko, Nicolai A. Aksenov, Iliya K. Kuzminov, Elena V. Aleksandrova, Puppala Sathish, Nakya Mesa-Diaz, Alexandra Vernaza, Angela Zhang, Liqin Du, Alexander Kornienko
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“PROTAC” modified dihydroquinolizinones (DHQs) that cause degradation of PAPD-5 and inhibition of hepatitis A virus and hepatitis B virus, in vitro Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-29 You Li, Nicky Hwang, Andrew Snedeker, Stanley M. Lemon, Daisy Noe, Liren Sun, Jason A. Clement, Tianlun Zhou, Liudi Tang, Timothy Block, Yanming Du
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The discovery of novel and potent indazole NLRP3 inhibitors enabled by DNA-encoded library screening Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-28 George Hartman, Paul Humphries, Robert Hughes, Andrew Ho, Rusty Montgomery, Aditi Deshpande, Maitriyee Mahanta, Sarah Tronnes, Samantha Cowdin, Xu He, Fangchao Liu, Lifang Zhang, Chuan Liu, Dengfeng Dou, Jin Li, Aleksander Spasic, Rebecca Coll, Michael Marleaux, Inga V. Hochheiser, Matthias Geyer, Paul Rubin, Kristen Fortney, Kevin Wilhelmsen
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Synthesis, SARS-CoV-2 main protease inhibition, molecular docking and in silico ADME studies of furanochromene-quinoline hydrazone derivatives Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-27 Blake M. Shellenberger, Olivia N. Basile, Joel Cassel, Morgan R. Olsen, Joseph M. Salvino, Luis J. Montaner, Ian Tietjen, Geneive E. Henry
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Fyn, Blk, and Lyn kinase inhibitors: A mini-review on medicinal attributes, research progress, and future insights Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-24 Rupali Kohal, Bhavana, Preety Kumari, Arun Kumar Sharma, Ghanshyam Das Gupta, Sant Kumar Verma
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Development of 1,5-diarylpyrazoles as EGFR/JNK-2 dual inhibitors: design, synthesis, moleecular docking, and bioactivity evaluation Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-24 Osama M. Soltan, Salah A. Abdel-Aziz, Montaser Sh. Shaykoon, Keima Osawa, Atsushi Narumi, Mohamed Abdel-Aziz, Mai E Shoman, Hiroyuki Konno
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Development of STING degrader with double covalent ligands Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-24 Miki Nakamura, Nobumichi Ohoka, Norihito Shibata, Takao Inoue, Genichiro Tsuji, Yosuke Demizu
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Exploration of bromodomain ligand-linker conjugation sites for efficient CBP/p300 heterobifunctional degrader activity Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-24 Praveen Kumar Tiwari, Sai Reddy Doda, Raghu Vannam, Manish Hudlikar, Drew A. Harrison, Samuel Ojeda, Sumit Rai, Ann-Sophie Koglin, Angelique Nguyen Gilbert, Christopher J. Ott
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Synthesis and initial evaluation of radioiodine-labelled deuterated tropane derivatives targeting dopamine transporter Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-24 Jie Liu, Jing Kang, Meihui Qi, Jie Tang, Yi Fang, Chunyi Liu, Jingjing Hong, Jiaojiao Zuo, Zhengping Chen
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Discovery of an ellipticine derivative as TLR3 inhibitor against influenza A virus and SARS-CoV-2 Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-21 Yue Pan, Qiuyue Fu, Yinyan Li, Jie Yang, Kui Cheng
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Re-exploration of tetrahydro-β-carboline scaffold: Discovery of selective histone deacetylase 6 inhibitors with neurite outgrowth-promoting and neuroprotective activities Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-21 Wen Wen, Jiadong Hu, Chenxi Wang, Rui Yang, Yabo Zhang, Baibei Huang, Tingting Qiao, Jiayun Wang, Xin Chen
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Synthesis, antibacterial activity, and 3D-QASR studies of matrine-indole derivatives as potential antibiotics Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-21 Yufang Li, Jamal A.H. Kowah, Meiyan Jiang, Yaqing Wu, Lisheng Wang, Fangfang Yang
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Synthesis and kinetic evaluation of phosphomimetic inhibitors targeting type B ribose-5-phosphate isomerase from Mycobacterium tuberculosis Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-19 Stéphanie Courtiol-Legourd, Sandrine Mariano, Johanna Foret, Annette K. Roos, Sherry L. Mowbray, Laurent Salmon
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Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-18 Pengpeng Niu, Huiqi Xu, Mengyang Fan
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α-Amino bisphosphonate triazoles serve as GGDPS inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-17 Nathaniel R. Gehrke, Dan Feng, Md. Ayub Ali, Mona A. Maalouf, Sarah A. Holstein, David F. Wiemer
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2-Phenylcyclopropylmethylamine (PCPMA) as a privileged scaffold for central nervous system drug design Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-14 Huiqiong Li, Jianjun Cheng
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PSMA-targeted SMART molecules outfitted with SN38 Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-14 Emily A. Savoy, Feyisola P. Olatunji, Nooshin Mesbahi, Ryanne K. Ballard, Christine L. Lovingier, Aaron T. Hendricksen, Melody D. Fulton, Clifford E. Berkman
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A gene-encoded aldehyde tag repurposed from RiPP cyclophane-forming pathway Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-13 Suze Ma, Heng Chen, Shuxun Liu, Xuedong Huang, Tianlu Mo, Wan-Qiu Liu, Wei Zhang, Wei Ding, Qi Zhang
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Discovery of N-(1-(2-hydroxyethyl)quinolin-2-one)-N’-(1-phenyl-1H-pyrazol-5-yl)methyl) urea as Mode-Selective TRPV1 antagonist Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-13 Dongxu Zuo, Mannkyu Hong, Aeran Jung, Sunho Lee, Nayeon Do, Sungwon Jung, Yubum Jeon, Ji Won Jeong, Guocheng Huang, Li-Xuan Li, Peter M. Blumberg, Hongryul Yoon, Yoonji Lee, Jihyae Ann, Jeewoo Lee
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Discovery of a novel series of pyridone amides as NaV1.8 inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-11 Yanfang Wang, Shilong Hu, Yuhao Chen, Meiyuan Chen, Di Zhang, Wencheng Liu, Chunxia Chen, Yu Gan, Menglan Luo, Bowen Ke
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Design, synthesis of new 3H-imidazo[4,5-b]pyridine derivatives and evaluation of their inhibitory properties as mixed lineage kinase 3 inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-10 Hye Ree Yoon, Anand Balupuri, Jinwoo Lee, Chaeeun Lee, Dong-Hyun Son, Re Gin Jeoung, Kyung ah Kim, Sungwook Choi, Nam Sook Kang
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Cytotoxic leuconoxine-type diazaspiroindole alkaloids isolated from Cryptolepis dubia Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-09 Yulin Ren, Elizabeth N. Kaweesa, Joshua M. Henkin, Kongmany Sydara, Mouachanh Xayvue, Pankaj Pandey, Amar G. Chittiboyina, Zulfiqar Ali, Daneel Ferreira, Djaja D. Soejarto, Joanna E. Burdette, A. Douglas Kinghorn
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Rational design, synthesis and biological evaluation of novel HIV-1 protease inhibitors containing 2-phenylacetamide derivatives as P2 ligands with potent activity against DRV-Resistant HIV-1 variants Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-09 Sihan Meng, Yu Gao, Guowei Qiang, Zhiwei Hu, Qi Shan, Juxian Wang, Yucheng Wang, Jie Mou
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Lipid bilayer membrane permeability mechanism of the K-Ras(G12D)-inhibitory bicyclic peptide KS-58 elucidated by molecular dynamics simulations Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-09 Kotaro Sakamoto, Takatsugu Hirokawa
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Design, synthesis and biological evaluation of 2-phenylaminopyrimidine derivatives as EGFR inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-06 Chunlei Tang, Jie Wang, Dong Wang, Huabing Wang, Shengkai Cui, Tianxin Xiao, Weizheng Fan, Yan Zhang
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Potential of several triazene derivatives against DENGUE viruses Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-06 Seynabou Sokhna, Natacha Mérindol, Marc Presset, Insa Seck, Marie-Pierre Girard, Seydou Ka, Samba Fama Ndoye, Aïcha Lalla Ba, Issa Samb, Lionel Berthoux, Erwan Le Gall, Isabel Desgagné-Penix, Matar Seck
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Identification of novel benzothiazole derivatives as inhibitors of NEDDylation pathway to inhibit the progression of gastric cancer Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-05 Xuan Wang, Mei Zhao, Yuanyuan Chang, Sumeng Guan, Mengyu Li, Hua Yang, Moran Sun
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Glycosidase-activated H2S donorsto enhance chemotherapy efficacy Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-03 Zizhen Ye, Jixiang Li, Jiarui Shi, Yuguang Song, Yangping Liu, Jingli Hou
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Design, synthesis and biological evaluation of novel cyclic malonamide derivatives as selective RIPK1 inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-03 József Levente Petró, Gyula Bényei, Péter Bana, Nikolett Linke, Ferenc Horti, Judit Eszter Szabó, Krisztina Katalin Szalai, Gábor Hornyánszky, István Greiner, János Éles
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Identification of 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one scaffolds as potent Lck inhibitors as anti-cancer agents Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-03 Su Hyun Ji, Han Byeol Kim, Yeonju Song, Hwan Won Chung, Duck-Hyung Lee, Cheulhee Jung, Yeonjin Ko, Seo-Jung Han
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Exploring 2-methyl–substituted vitamin K3 derivatives with potent inhibitory activity against the 3CL protease of SARS-CoV-2 Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-02 Ryohto Koharazawa, Mayu Hayakawa, Kazuki Takeda, Kotone Miyazaki, Chisato Tode, Yoshihisa Hirota, Yoshitomo Suhara
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Discovery of a novel series of selective macrocyclic PKCTheta inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-01 Stefano Crosignani, Sebastien Campos, Claire Bouix-Peter, Craig Harris, Eric Talbot, Haiyang Hu, Shun Wang, John Maclean, Ugo Zanelli, Simon Taylor, Kevin Foote, Feriel Hacini-Rachinel, Edwige Nicodeme, Valerie Julia
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Identification of (4-chlorophenyl)(5-hydroxynaphtho[1,2-b]furan-3-yl)methanone as novel COX-2 inhibitor with analgesic profile Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-02-01 Shilong Hu, Wencheng Liu, Yu Gan, Xi Yang, Yanfang Wang, Xing Wei, Meiyuan Chen, Di Zhang, Bowen Ke
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Discovery and first-time disclosure of CVN766, an exquisitely selective orexin 1 receptor antagonist Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-30 Angela Glen, Roland W. Bürli, David Livermore, William Buffham, Stephanie Merison, Anna E. Rowland, Robert Newman, Charlotte Fieldhouse, David J. Miller, Lee A. Dawson, Kim Matthews, Mark B. Carlton, Nicola L. Brice
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Novel orexin receptor agonists based on arene- or pyridine-fused 1,3-dihydro-2H-imidazole-2-imines Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-23 Wentian Wang, Alok Ranjan, Wei Zhang, Qiren Liang, Karen S. MacMillan, Karen Chapman, Xiaoyu Wang, Preethi Chandrasekaran, Noelle S. Williams, Daniel M. Rosenbaum, Jef K. De Brabander
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Further structural optimization and SAR study of sungsanpin derivatives as cell-invasion inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-23 Shuai Chen, Kai Zhang, Jihua Zou, Zhou Yu, Conghao Gai, Xiaoyun Chai, Qingjie Zhao, Yan Zou
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Novel xanthone derivatives as potent sirtuin 2 inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-26 Gabriela Mazur, Katarzyna Pańczyk-Straszak, Karolina Krysińska, Karolina Niemiec, Anna Waszkielewicz
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Synthesis and biological evaluation of novel 18F-labeled 2,4-diaminopyrimidine derivatives for detection of ghrelin receptor in the brain Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-20 Haruka Saito, Hiroyuki Watanabe, Masahiro Ono
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Cytotoxic effects of kinetin riboside and its selected analogues on cancer cell lines Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-25 Ewa Totoń, Natalia Lisiak, Aleksandra Romaniuk-Drapała, Grzegorz Framski, Eliza Wyszko, Tomasz Ostrowski
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Structure-based design and synthesis of sulfonylureas as novel NLRP3 inhibitors for Alzheimer’s disease Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-19 Eun Young Kim, Jae Hong Im, Jinhe Han, Won-Jea Cho
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Direct-to-biology platform: From synthesis to biological evaluation of SHP2 allosteric inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-23 Simona Ponzi, Federica Ferrigno, Monica Bisbocci, Cristina Alli, Jesus M. Ontoria, Alessia Petrocchi, Carlo Toniatti, Esther Torrente
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Design, synthesis and bioactivity evaluation of the combination of evodiamine and erlotinib linked by indolequinone Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-01-18 Binbin Wei, Jingjing Ma, Hui Guo, Yuwei Wang, Dongyan Guo, Yuping Tang