Kanouni, Toufike published the artcileDiscovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1), Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is CC90011 inhibitor lysine specific demethylase 1 LSD1.
Histone demethylase LSDl (KDMlA) belongs to the FAD dependent family of monoamine oxidases and is vital in regulation of mammalian biol. Dysregulation and overexpression of LSD1 are hallmarks of a number of human diseases, particularly cancers that are characterized as morphol. poorly differentiated. As such, inhibitors of LSD1 have potential to be beneficial as a cancer therapy. The most clin. advanced inhibitors of LSDl are covalent inhibitors derived from tranylcypromine (TCP). Herein, we report the discovery of a novel series of reversible and selective LSDl inhibitors. Exploration of structure-activity relationships (SARs) and optimization of ADME properties resulted in the identification of clin. candidate CC-90011. CC-90011 exhibits potent on-target induction of cellular differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cell lines, and antitumor efficacy in patient-derived xenograft (PDX) SCLC models. CC-90011 is currently in phase 2 trials in patients with first line, extensive stage SCLC (ClinicalTrials.gov identifier: NCT03850067).
Journal of Medicinal Chemistry published new progress about Acute myeloid leukemia. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Name: tert-Butyl piperidin-4-ylcarbamate.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem