1575622-50-2Relevant academic research and scientific papers
Novel coumarin-dihydropyrazole thio-ethanone derivatives: Design, synthesis and anticancer activity
Wu, Xiao-Qin,Huang, Cheng,Jia, Ying-Ming,Song, Bao-An,Li, Jun,Liu, Xin-Hua
, p. 717 - 725 (2014)
A series novel 1-(3-substituted-5-phenyl-4,5-dihydropyrazol-1-yl)-2-thio- ethanone derivatives as potential telomerase inhibitors were designed and synthesized. The bioassays demonstrated that compounds 4a, 4f, 4j and 7b, 7d occupied high antiproliferative activity against SGC-7901, MGC-803, Bcap-37 and HEPG-2 cell lines. By a modified TRAP assay, some title compounds were tested against telomerase, and compound 4f showed the most potent inhibitory activity with IC50 value at 0.92 ± 0.09 μM. The mechanism of antitumor action indicated that title compounds 4f and 7b could suppress cell proliferation through inducing cell cycle arrest in G0/G1 phase.
New arylpyrazoline-coumarins: Synthesis and anti-inflammatory activity
Chen, Liu Zeng,Sun, Wei Wei,Bo, Li,Wang, Jie Quan,Xiu, Cheng,Tang, Wen Jian,Shi, Jing Bo,Zhou, Hai Pin,Liu, Xin Hua
, p. 170 - 181 (2017)
To develop new anti-inflammatory agents with improved pharmaceutical profiles, a series of new phenyl-pyrazoline-coumarin derivatives (4a～4m) were designed and synthesized. Compounds 4a and 4b were determined by X-ray crystallography. All of the compounds have been screened for their anti-inflammatory activity characterized by evaluating their inhibition against LPS-induced IL-6 release. Among them, compound 4m showed the highest anti-inflammatory activity with inhibiting IL-6, TNF-α and nitric oxide (NO) production lipopolysaccharide (LPS)-stimulated. The further study showed that title compound 4m could significantly suppress expressions of nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and the productions of IL-6, TNF-α, NO through NF-κB/MAPK signaling pathway. The anti-inflammatory activity of compound 4m was determined by carrageenan induced paw edema. Furthermore in vivo evaluation results indicated that compound 4m could inhibit AA-induced rat ankle joints.
