1376358-90-5Relevant 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 (2014/03/21)
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.
Design and synthesis of novel 5-phenyl-N-piperidine ethanone containing 4,5-dihydropyrazole derivatives as potential antitumor agents
Liu, Xin-Hua,Li, Jun,Shi, Jing Bo,Song, Bao-An,Qi, Xing-Bao
, p. 294 - 299 (2012/07/14)
A series of novel 5-phenyl-N-piperidine ethanone-4,5-dihydropyrazole derivatives as potential telomerase inhibitors were synthesized. The bioassays demonstrated that compounds 4d, 4f, 7a and 7b occupied high antiproliferative activities against SGC-7901, MGC-803 and Bcap-37 cell lines. By a modified TRAP assay, some titled compounds were tested against telomerase, and compound 7b showed the most potent inhibitory activity with IC50 value at 2.00 ± 0.40 μM. The active compound 4d was also docked into the telomerase TERT active site to determine the probable binding model. The results indicated that conserved residues Lys189, Asp254 and Gln308 were important for ligand binding via hydrogen bond interactions.
Novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5-substituted- phenyl-4,5-dihydro-1H-pyrazol-3-yl)-Coumarins: Synthesis and anticancer activity
Lv, Xian-Hai,Zhang, Xiu-Li,Liu, Xin-Hua,Shi, Lei
, p. 199 - 203 (2012/07/17)
Seven novel 3-(1-(2-(2,7a-dihydrobenzo[d]thiazol-2-ylthio)acetyl)-5- substituted-phenyl-4,5-dihydro-1H-pyrazol-3-yl)-2H-chromen-2-one derivatives were synthesized and characterized by 1H NMR and 13 C NMR. All of the compounds have be
