750604-86-5Relevant academic research and scientific papers
Synthesis, biological evaluation, 3D-QSAR studies of novel aryl-2H-pyrazole derivatives as telomerase inhibitors
Luo, Yin,Zhang, Shuai,Qiu, Ke-Ming,Liu, Zhi-Jun,Yang, Yu-Shun,Fu, Jie,Zhong, Wei-Qing,Zhu, Hai-Liang
, p. 1091 - 1095 (2013/03/13)
A series of novel aryl-2H-pyrazole derivatives bearing 1,4-benzodioxan or 1,3-benzodioxole moiety were designed as potential telomerase inhibitors to enhance the ability of aryl-2H-pyrazole derivatives to inhibit telomerase, a target of anticancer. The telomerase inhibition tests showed that compound 16A displayed the most potent inhibitory activity with IC50 value of 0.9 μM for telomerase. The antiproliferative tests showed that compound 16A exhibited high activity against human gastric cancer cell SGC-7901 and human melanoma cell B16-F10 with IC50 values of 18.07 and 5.34 μM, respectively. Docking simulation showed that compound 16A could bind well with the telomerase active site and act as telomerase inhibitor. 3D-QSAR model was also built to provide more pharmacophore understanding that could be used to design new agents with more potent telomerase inhibitory activity.
Effect of ring A and ring B substitution on the cytotoxic potential of pyrazole tethered chalcones
Nepali, Kunal,Kadian, Kanika,Ojha, Ritu,Dhiman, Rajni,Garg, Atul,Singh, Gagandip,Buddhiraja, Abhishek,Bedi, Preet Mohinder Singh,Dhar, Kanaya Lal
, p. 2990 - 2997 (2012/10/29)
Chalcone is an aromatic ketone that forms the central core for a variety of important biological compounds, which are collectively known as chalcones. The cytotoxic potential of chalcones which consists of C6-C 3-C6 units gets enhanced by the incorporation of pyrazole ring as proved by our earlier studies. Thus in the present work, pyrazoles of chalcones with ring A substituted by furan, naphthalene and variety of substituted phenyl rings has been prepared and evaluated for in vitro cytotoxic activity against PC-3, OVCAR, IMR-32, HEP-2 human cancer cell lines. Springer Science+Business Media, LLC 2011.
