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Biological evaluation of sulfonate and sulfate analogues of lithocholic acid: A bioisosterism-guided approach towards the discovery of potential sialyltransferase inhibitors for antimetastatic study Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-17 Ser John Lynon P. Perez, Chia-Ling Chen, Tzu-Ting Chang, Wen-Shan Li
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Identification of a novel histone H2A mono-ubiquitination-inhibiting cell-active small molecule Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-16 Siyao Ni, Yuri Takada, Takaaki Ando, Shengwang Yu, Yasunobu Yamashita, Yukari Takahashi, Miho Sawada, Makoto Oba, Yukihiro Itoh, Takayoshi Suzuki
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In vitro inhibition of α-Synuclein aggregation and disaggregation of preformed fibers by polyphenol hybrids with 2-conjugated benzothiazole Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-15 Ya-Dong Zhao, Wei Zhang, Li-Zi Xing, Ji Xu, Wei-Min Shi, Yun-Xiao Zhang
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Modification of the phenyl ring B of phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates by pyridinyl moiety leads to novel antimitotics targeting the colchicine-binding site Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-11 Vincent Ouellette, Chahrazed Bouzriba, Atziri Corin Chavez Alvarez, Geneviève Hamel-Côté, Sébastien Fortin
A series of 8 novel pyridinyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates (PYRIB-SOs) were designed, prepared and evaluated for their mechanism of action. PYRIB-SOs were found to have antiproliferative activity in the nanomolar to submicromolar range on several breast cancer cell lines. Moreover, subsequent biofunctional assays indicated that the most potent PYRIB-SOs – act as antimitotics binding
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Fluorine-18 labeling PEGylated 6-boronotryptophan for PET scanning of mice for assessing the pharmacokinetics for boron neutron capture therapy of brain tumors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-11 Xiang-Ping Chen, Fu-Chun Hsu, Kwei-Yuan Huang, Teng-San Hsieh, Shiou-Shiow Farn, Rong-Jiun Sheu, Chung-Shan Yu
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Discovery and synthesis of novel benzoylhydrazone neuraminidase inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-11 Shi Kai Fu, Li Ping Cheng
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Retraction notice to “Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities” [Bioorg. Med. Chem. Lett. 22(9) (2012) 3067–3071] Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-10 Minsun Chang, Sung-Hak Lee, Ho Jun Kim, Jong-Sung Koh, Aeri Kim
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Insights into the structure–activity relationship of the anticancer compound ZJ-101: A role played by the amide moiety Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-09 Haibo Qiu, Shan Qian, Sarah A. Head, Phillip R. Sanchez, Jun O. Liu, Zhendong Jin
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Discovery of novel nucleoside derivatives as selective lysine acetyltransferase p300 inhibitors for cancer therapy Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-09 Qiuzi Dai, Zigao Yuan, Qinsheng Sun, Zhuolin Ao, Binsheng He, Yuyang Jiang
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The mechanism of covalent inhibition of LAR phosphatase by illudalic acid Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-09 Daniel T. Hansen, Nicole J. Rueb, Nathan D. Levinzon, Thomas E. Cheatham III, Robert Gaston Jr., Kh Tanvir Ahmed, Sandra Osburn-Staker, James E. Cox, Gregory B. Dudley, Amy M. Barrios
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The discovery of an anti-inflammatory monoterpenoid, neoroseoside from the Zea mays Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-08 Hui Tan, Hyun-jin Lee, Prima F. Hillman, Eun-Young Lee, Chaeyoung Lee, Eun Kyoung Seo, Mi Ja Lee, Sang-Jip Nam
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Structural modification of tanshinone IIA and their α-glucosidase inhibitory activity Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-08 Mutita Kongphet, Hoa Tai Xuan Hang, Thanh The Ngo, Thi-Kim-Dung Le, Warinthorn Chavasiri
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Synthesis and antiproliferative activity of a tetrahydrofuran analog of FR901464 Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-08 Ivanna Pohorilets, Jacob P. Beard, Julia L. Driscoll, John C. Schmitz, Kazunori Koide
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Copper-mediated siRNA activation for conditional control of gene expression Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-07 Kunihiko Morihiro, Yasuhiro Tomida, Honami Ando, Akimitsu Okamoto
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[99mTc]Tc-labeled HYNIC conjugated chlorambucil as a tumor targeting Agent: Synthesis, characterization and ex-vivo evaluation Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-05 Soumi Kolay, Naveen Kumar, Mohini Guleria, Tapas Das
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Systematical mutational analysis of teriparatide on anti-osteoporosis activity by alanine scanning Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-05 Haiyan Liang, Huaxing Shen, Mengjun Zheng, Yejiao Shi, Xiang Li
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A responsive disulfide bond switch aptamer prodrug exhibiting enhanced stability and anticancer efficacy Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-05 Xiao Dong, Zhe Zhang, Tangna Zhao, Zuyi Chen, Jia Wang, Liang Xu, Aiping Zhang
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Antascomicin B stabilizes FKBP51-Akt1 complexes as a molecular glue Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-04 Sabine C. Schäfer, Andreas M. Voll, Andreas Bracher, Steven V. Ley, Felix Hausch
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β-Galactosidase-guided self-assembled 68Ga nanofibers probe for micro-PET tumor imaging Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-04 Kangxia Yu, Peng Zhou, Meimei Wang, Pei Zou, Hongyong Wang, Yaling Liu, Minhao Xie
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Design, synthesis and activity evaluation of quinolinone derivatives as EZH2 inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-04-03 Jin Cai, Haoyuan You, Xintong Qin, Yuhong Wang, Wei Li
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Design, synthesis and biological evaluation of tanshinone IIA derivatives as NLRP3 inflammasome inhibitors Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-29 Hao Chen, Hu Yue, Yuyun Yan, Nannan Wu, Dan Wu, Ping Sun, Wenhui Hu, Zhongjin Yang
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Improved synthesis, molecular modeling and anti-inflammatory activity of new fluorinated dihydrofurano-naphthoquinone compounds Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-22 Ha Thanh Nguyen, Hai Pham-The, Anh Nguyen Tuan, Ha Nguyen Thi Thu, Tuyet Anh Dang Thi, Giang Le-Nhat-Thuy, Phuong Hoang Thi, Quynh Giang Nguyen Thi, Tuyen Van Nguyen
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Antiproliferative activities through accelerating autophagic flux by basidalin and its analogs in human cancer cells Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-22 Tomoe Matagawa, Yukiko Sasazawa, Koki Agui, Motoki Fujimaki, Sayaka Kawano, Akihiro Ogura, Ken-ichi Takao, Masayuki Igarashi, Siro Simizu
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A PSMA-targeted doxorubicin small-molecule drug conjugate Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-21 Hosog Yoon, Emily A. Savoy, Nooshin Mesbahi, Aaron T. Hendricksen, Gabrielle L. March, Melody D. Fulton, Brian S. Backer, Clifford E. Berkman
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Synthesis and antihepatoma activity of guaianolide dimers derived from lavandiolide I Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-21 Xing Wang, Tian-Ze Li, Yun‐Bao Ma, Wen‐Jing Ma, Dong Xue, Ji-Jun Chen
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Targeting ATP-binding site of WRN Helicase: Identification of novel inhibitors through pocket analysis and Molecular Dynamics-Enhanced virtual screening Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-21 Hao Yuan, Run-Duo Liu, Zhuo-Yu Gao, Li-Ting Zhong, Ying-Chen Zhou, Jia-Heng Tan, Zhi-Shu Huang, Zhe Li, Shuo-Bin Chen
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Design, synthesis, and biological evaluation of novel benzo[6,7]indolo[3,4-c]isoquinolines as anticancer agents with topoisomerase I inhibition Bioorg. Med. Chem. Lett. (IF 2.7) Pub Date : 2024-03-20 Kie Sakai, Taisei Soshima, Yuki Hirose, Fumito Ishibashi, Shotaro Hirao
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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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