92858-63-4Relevant academic research and scientific papers
Novel diphenylpropene derivative, preparation method thereof and pharmaceutical composition
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Paragraph 0115; 0116; 0117, (2018/07/30)
The invention provides a novel diphenylpropene derivative and a preparation method thereof, and a pharmaceutical composition. The novel diphenylpropene derivative is a compound with the following general formula I, or the novel diphenylpropene derivative is an acceptable salt formed by a compound with the general formula I and an inorganic acid or an organic acid, wherein B is E-1-allyl group or E-2-allyl group; R1 and R3 are methoxy groups and R2 is hydrogen, or R2 and R3 form a methylenedioxy group, and R1 is hydrogen; the general formula I specifically comprises a general formula II, a general formula III, a general formula IV and a general formula V. Based on the setting of a specific substituent R, the novel diphenylpropene derivative has the effect of promoting the activity of the body nerves and the low cytotoxicity.
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.
