358656-62-9Relevant academic research and scientific papers
A class of novel tubulin polymerization inhibitors exert effective anti-tumor activity via mitotic catastrophe
Zhang, Ya-Liang,Li, Bo-Yan,Yang, Rong,Xia, Lin-Ying,Fan, A-Li,Chu, Yi-Chun,Wang, Lin-Jian,Wang, Zhong-Chang,Jiang, Ai-Qin,Zhu, Hai-Liang
, p. 896 - 910 (2019/01/04)
In current work, a class of novel 4,5-dihydro-1H-pyrazole-1-carboxylate derivatives (E01-E28) were designed, synthesized and evaluated. Among them, the most potent compound E24 exhibited comparable activity against a panel of cancer cells (GI50
Synthesis and Anticancer Activity of 3-(Substituted Aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole Derivatives
Zhan, Xiao-Ping,Lan, Lan,Wang, Shuai,Zhao, Kai,Xin, Yu-Xuan,Qi, Qi,Wang, Yao-Lin,Mao, Zhen-Min
, (2017/02/23)
A series of 3-(substituted aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole derivatives were synthesized and determined for their anticancer activity against eleven cancer cell lines and two normal tissue cell lines using MTT assay. Among the synthesized comp
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives
Congiu, Cenzo,Onnis, Valentina,Vesci, Loredana,Castorina, Massimo,Pisano, Claudio
scheme or table, p. 6238 - 6248 (2010/10/03)
A series of 3,5-diaryl-4,5-dihydropyrazole regioisomers, and their 1-acetylated derivatives, bearing a 3,4,5-trimethoxyphenyl moiety combined with a variety of substituted phenyl rings, was synthesized and evaluated for antitumor activity. Results of the in vitro assay against a non-small cell lung carcinoma cell line (NCI-H460) showed several compounds to be endowed with cytotoxicity in micromolar to sub-micromolar range, depending on substitution pattern and position of aryl rings on 4,5-dihydropyrazole core. Potent and selective activity was also observed in the NCI 60 human cancer cell line panel. 5-(3,4,5-Trimethoxyphenyl)pyrazolines 31 and 39 were found to possess potent antiproliferative activity against SR and MDA-MB-435, with GI50 inhibitory values in nanomolar range. Structure-activity relationships revealed that introduction of a (hydroxy)acetyl group at N-1 of inactive 5-(3,4,5-trimethoxyphenyl)pyrazolines, results in a clear in vitro activating effect. Compound 31 (IC50 = 5.16 μM) showed inhibition of tubulin polymerization comparable to that of CA-4 (IC50 = 4.92 μM).
