Since a novel coronavirus was discovered from a cluster of patients with emerging pneumonia of unknown etiology in Wuhan, China, it has spread rapidly through droplet and contact transmission. Recently, the novel coronavirus pneumonia which was named COVID-19 by the World Health Organization (WHO) has been raised as a worldwide problem. Radiological examinations were confirmed as effective methods for the screening and diagnosis of COVID-19. It is reported that some radiologists and radiological technologists were infected when giving examinations to the patients with COVID-19. In order to reduce the infection risk of medical staff in radiology department, we summarized the experience on prevention and control measures in radiology department for COVID-19, aiming to guide the prevention and practical work for radiologists and radiological technologists. Key Points • The novel coronavirus spreads rapidly through droplet and contact transmission.• Radiologists and radiological technologists were possibly infected by patients.• Prevention and control measures in radiology department for COVID-19 are important.

Histone lysine specific demethylase 1 (LSD1) has been recognized as an important modulator in post-translational process in epigenetics. Dysregulation of LSD1 has been implicated in the development of various cancers. Herein, we report the discovery of the hit compound 8a (IC 50 = 3.93 μmol/L) and further medicinal chemistry efforts, leading to the generation of compound 15u (IC 50 = 49 nmol/L, and K i = 16 nmol/L), which inhibited LSD1 reversibly and competitively with H3K4me2, and was selective to LSD1 over MAO-A/B. Docking studies were performed to rationalize the potency of compound 15u . Compound 15u also showed strong antiproliferative activity against four leukemia cell lines (OCL-AML3, K562, THP-1 and U937) as well as the lymphoma cell line Raji with the IC 50 values of 1.79, 1.30, 0.45, 1.22 and 1.40 μmol/L, respectively. In THP-1 cell line, 15u significantly inhibited colony formation and caused remarkable morphological changes. Compound 15u induced expression of CD86 and CD11b in THP-1 cells, confirming its cellular activity and ability of inducing differentiation. The findings further indicate that targeting LSD1 is a promising strategy for AML treatment, the triazole-fused pyrimidine derivatives are new scaffolds for the development of LSD1/KDM1A inhibitors.

Lysine specific demethylase 1 (LSD1) plays a pivotal role in regulating the lysine methylation. The aberrant overexpression of LSD1 has been reported to be involved in the progression of certain human malignant tumors. Abrogation of LSD1 with RNAi or small molecule inhibitors may lead to the inhibition of cancer proliferation and migration. Herein, a series of [1,2,3]triazolo[4,5-]pyrimidine derivatives were synthesized and evaluated for their LSD1 inhibitory effects. The structure-activity relationship studies (SARs) were conducted by exploring three regions of this scaffold, leading to the discovery of compound as potent LSD1 inhibitor (IC = 0.564 μM). Compound was identified as a reversible LSD1 inhibitor and showed certain selectivity to LSD1 over monoamine oxidase A/B (MAO-A/B). When MGC-803 cells were treated with compound, the activity of LSD1 can be significantly inhibited, and the cell migration ability was also suppressed. Docking studies indicated that the hydrogen interaction between the nitrogen atom in the pyridine ring and Met332 could be responsible for the improved activity of 2-thiopyridine series. The [1,2,3]triazolo[4,5-]pyrimidine scaffold can be used as the template for designing new LSD1 inhibitors.