Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer

Publication date: 15 November 2022Source: European Journal of Medicinal Chemistry, Volume 242Author(s): Limeng Wu, Wenjie Liu, Yaoguang Huang, Chengze Zhu, Qun Ma, Qiong Wu, Liting Tian, Xiangling Feng, Mingyue Liu, Nan Wang, Xiangbo Xu, Xin Liu, Chang…

Development of 3α,7α-dihydroxy-6α-ethyl-24-<em>nor</em>-5β-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites

Publication date: 15 November 2022Source: European Journal of Medicinal Chemistry, Volume 242Author(s): Bruno Cerra, Francesco Venturoni, Maria Souma, Giada Ceccarelli, Anna Maria Lozza, Daniela Passeri, Francesca De Franco, Ian R. Baxendale, Roberto P…

Discovery of azaspirocyclic 1<em>H-</em>3,4,5<em>-</em>Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors

Publication date: 15 November 2022Source: European Journal of Medicinal Chemistry, Volume 242Author(s): Robert K. Leśniak, R. Jeremy Nichols, Marcus Schonemann, Jing Zhao, Chandresh R. Gajera, Grace Lam, Khanh C. Nguyen, J. William Langston, Mark Smith…

Discovery of pimozide derivatives as novel T-type calcium channel inhibitors with little binding affinity to dopamine D<sub>2</sub> receptors for treatment of somatic and visceral pain

Publication date: 5 December 2022Source: European Journal of Medicinal Chemistry, Volume 243Author(s): Yoshihito Kasanami, Chihiro Ishikawa, Takahiro Kino, Momoka Chonan, Naoki Toyooka, Yasuhiro Takashima, Yuriko Iba, Fumiko Sekiguchi, Maho Tsubota, Ts…