1620753-65-2Relevant academic research and scientific papers
Identification of human telomerase inhibitors having the core of N-acyl-4,5-dihydropyrazole with anticancer effects
Xiao, Xuan,Ni, Yong,Jia, Ying-Ming,Zheng, Min,Xu, Han-Fei,Xu, Jun,Liao, Chenzhong
, p. 1508 - 1511 (2016/07/27)
Eight human telomerase inhibitors (5a–5h) having the core of N-acyl-4,5-dihydropyrazole with anticancer effects were identified in this study. Biological results revealed that a few compounds had potent anticancer activities against three common tumor cell lines (SGC-7901, HepG2 and MGC-803). Among them, compound 5c, with a molecular weight of only 272.2?Da, had antiproliferative activities against SGC-7901 and MGC-803 with EC50values of 2.06?±?0.17 and 2.89?±?0.62?μM, respectively, better than 5-Fluorouracil. Compound 5c inhibited the enzyme of telomerase with an IC50value of 1.86?±?0.51?μM, surpassing the control compound, ethidium bromide. Modeling study showed that this compound can reside in the binding pocket of the telomerase/TNA:DNA hairpin complex. When the moiety of N-acyl was changed to N-sulfonyl, the gotten compounds (8a–8i) had deteriorative activities against both these three cancer cell lines and the enzyme of telomerase.
Novel 4-bromo-2-(3-methyl-1-(substituted-phenylsulfonyl)-4,5-dihydro-1-H- pyrazol-5-yl)phenol derivatives: Synthesis and antibacterial activity
Cheng, Qing,Jia, Ying-Ming,Cheng, Fei-Hu,Liu, Xin-Hua
, p. 572 - 577 (2014/05/20)
A series of novel 4-bromo-2-(3-methyl-1-(substituted-phenylsulfonyl)-4,5- dihydro-1H-pyrazol-5-yl) phenol derivatives were synthesized and characterized by NMR, ESI-MS. Compound 3c was determined by X-ray. Biological activity tests results show that compound 3h displayed activity with MIC of 0.39, 0.78, 1.562 μg/mL against B. subtilis ATCC 6633, S. aureus ATCC 6538, P. fluorescens ATCC 13525 and could strongly inhibit S. aureus DNA gyrase and B. subtilis DNA gyrase with IC50s of 0.25 and 0.18 μg/mL respectively.
