Electric Literature of 105827-91-6. Let’s face it, organic chemistry can seem difficult to learn. Especially from a beginner’s point of view. Like 105827-91-6, Name is 2-Chloro-5-(chloromethyl)thiazole. In a document type is Article, introducing its new discovery.
Lysine-specific demethylase 1 (LSD1), demethylase against mono- and di – methylated histone3 lysine 4, has emerged as a promising target in oncology. More specifically, it has been demonstrated as a key promoter in acute myeloid leukemia (AML), and several LSD1 inhibitors have already entered into clinical trials for the treatment of AML. In this paper, a series of new indole derivatives were designed and synthesized based on a lead compound obtained by a high-throughput screening with our in-house compound library. Among the synthetic compounds, 9e was characterized as a potent LSD1 inhibitor with an IC50 of 1.230 muM and can inhibit the proliferation of THP-1 cells effectively. And most importantly, this is the first irreversible LSD1 inhibitor that is not derived from monoamine oxidase inhibitors. Hence, the discovery of 9e may serve as a proof of concept work for AML treatment.
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Reference：
Thiazole | C3H2942NS – PubChem,
Thiazole | chemical compound | Britannica