Monthly Archives: October 2023

Non-peptidic immunoproteasome β5i-selective inhibitor as potential treatment for idiopathic pulmonary fibrosis: Virtual screening, hit evolution and lead identification

Posted on by

Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Yunxuan Li, Guanglei Nan, Xianxin Hou, Yechao Yan, Yajun Yang, Ying Yang, Ke Li, Zhiyan Xiao

Exploring the structural-activity relationship of hexahydropyrazino[1,2-d]pyrido[3,2-b][1,4]oxazine derivatives as potent and orally-bioavailable PARP7 inhibitors

Posted on by

Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Silong Zhang, Yu Zhang, Ziwei Wang, Luolong Qing, Shaojuan Fu, Juan Xu, Yuanyuan Li, Huaxiang Fang, Huan He

Indirubin derivatives as bifunctional molecules inducing DNA damage and targeting PARP for the treatment of cancer

Posted on by

Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Siyuan Wan, Xinye Chen, Fucheng Yin, Shang Li, Yonglei Zhang, Heng Luo, Zhongwen Luo, Ningjie Cui, Yifan Chen, Xinxin Li, Lingyi Kong, Xiaobing Wang

Design, synthesis, and biological evaluation of novel 4,4′-bipyridine derivatives acting as CDK9-Cyclin T1 protein-protein interaction inhibitors against triple-negative breast cancer

Posted on by

Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Guiping Gao, Jiayi Li, Yin Cao, Xudan Li, Yuqing Qian, Xiumei Wang, Mengyu Li, Yingkun Qiu, Tong Wu, Liqiang Wang, Meijuan Fang

PITB: A high affinity transthyretin aggregation inhibitor with optimal pharmacokinetic properties

Posted on by

Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Francisca Pinheiro, Nathalia Varejão, Adrià Sánchez-Morales, Filipa Bezerra, Susanna Navarro, Adrián Velázquez-Campoy, Félix Busqué, Maria Rosário Almeida, Ramon Alibés, David Reverter, Irantzu Pallarès, Salvador Ventura

Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer’s disease

Posted on by

Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Paula Zaręba, Kamil Łątka, Gabriela Mazur, Beata Gryzło, Anna Pasieka, Justyna Godyń, Dawid Panek, Anna Skrzypczak-Wiercioch, Georg C. Höfner, Gniewomir Latacz, Maciej Maj, Alba Espargaró, Raimon Sabaté, Krzysztof Jóźwiak, Klaus T. Wanner, Kinga Sałat, Barbara Malawska, Katarzyna Kulig, Marek Bajda

Design, synthesis, and biological evaluation of quinoline-piperazine/pyrrolidine derivatives as possible antileishmanial agents

Posted on by

Publication date: 5 December 2023

Source: European Journal of Medicinal Chemistry, Volume 261

Author(s): Sarita Katiyar, Karthik Ramalingam, Abhishek Kumar, Alisha Ansari, Amol Chhatrapati Bisen, Garvita Mishra, Sachin Nashik Sanap, Rabi Sankar Bhatta, Bidyut Purkait, Neena Goyal, Koneni V. Sashidhara