Design, synthesis and biological evaluation of chalcone derivatives as potent and orally active hCYP3A4 inhibitors

Publication date: 15 October 2023

Source: Bioorganic & Medicinal Chemistry Letters, Volume 95

Author(s): Shiwei Lu, Feng Zhang, Jiahao Gong, Jian Huang, Guanghao Zhu, Yitian Zhao, Qi Jia, Yiming Li, Bo Li, Kaixian Chen, Weiliang Zhu, Guangbo Ge

Synthesis and anti-tumor activities in human leukemia-derived cells of polyenylpyrroles with a methyl group at the conjugated polyene terminus

Publication date: 15 October 2023

Source: Bioorganic & Medicinal Chemistry Letters, Volume 95

Author(s): Tomoya Higashi, Chihiro Yoshida, Yoshifumi Hachiro, Chihiro Nakata, Azusa Takechi, Takuya Yagi, Kazuya Miyashita, Nobuo Kitada, Rika Obata, Takashi Hirano, Takahiko Hara, Shojiro A. Maki

Brain-penetrant cyanoindane and cyanotetralin inhibitors of G2019S-LRRK2 kinase activity

Publication date: 15 October 2023

Source: Bioorganic & Medicinal Chemistry Letters, Volume 95

Author(s): Albert W. Garofalo, Jacob Schwarz, Kerry Zobel, Claudia Beato, Silvia Bernardi, Federica Budassi, Laura Caberlotto, Peng Gao, Cristiana Griffante, Xinying Liu, Marco Migliore, Feifei Qiao, Fabio Maria Sabbatini, Anna Sava, Mingliang Zhang, Holly J. Carlisle

Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings

Publication date: 15 October 2023

Source: Bioorganic & Medicinal Chemistry Letters, Volume 95

Author(s): Ahmed Fnaiche, Léa Mélin, Narjara González Suárez, Alexis Paquin, Victoria Vu, Fengling Li, Abdellah Allali-Hassani, Albina Bolotokova, Frédéric Allemand, Muriel Gelin, Philippe Cotelle, Simon Woo, Steven R. LaPlante, Dalia Barsyte-Lovejoy, Vijayaratnam Santhakumar, Masoud Vedadi, Jean-François Guichou, Borhane Annabi, Alexandre Gagnon