18926-47-1Relevant academic research and scientific papers
Design, synthesis and evaluation of 3-substituted coumarin derivatives as anti-inflammatory agents
Liu, Shuchen,Peng, Tao,Sun, Yunbo,Wang, Gang,Wang, Lin,Wang, Tao,Wen, Xiaoxue,Zhang, Shouguo
, p. 443 - 446 (2020/09/09)
Coumarin moiety has garnered momentous attention especially in the design of compounds with significant biological activities. In this work, a series of 3-substituted coumarin derivatives 6a-6l were synthesized and fully characterized. Most of the compoun
Discovery of Novel 4-Arylisochromenes as Anticancer Agents Inhibiting Tubulin Polymerization
Li, Wenlong,Shuai, Wen,Xu, Feijie,Sun, Honghao,Xu, Shengtao,Yao, Hong,Liu, Jie,Yao, Hequan,Zhu, Zheying,Xu, Jinyi
supporting information, p. 974 - 979 (2018/10/15)
XJP-L (8), a derivative of the natural product (±)-7,8-dihydroxy-3-methylisochroman-4-one isolated from the peel of Musa sapien tum L., was found to exhibit weak inhibitory activity of tubulin polymerization (IC50 = 10.6 μM) in our previous studies. Thus, a series of 4-arylisochromene derivatives were prepared by incorporating the trimethoxyphenyl moiety into 8, among which compound (±)-19b was identified as the most potent compound with IC50 values ranging from 10 to 25 nM against a panel of cancer cell lines. Further mechanism studies demonstrated that (±)-19b disrupted the intracellular microtubule network, caused G2/M phase arrest, induced cell apoptosis, and depolarized mitochondria of K562 cells. Moreover, (±)-19b exhibited potent in vitro antivascular and in vivo antitumor activities. Notably, the R-configured enantiomer of (±)-19b, which was prepared by chiral separation, was slightly more potent than (±)-19b and was much more potent than the S-configured enantiomer in both antiproliferative and antitubulin assays. Our findings suggest that (±)-19b deserves further research as a potential antitubulin agent for the treatment of cancers.
A Study of Electronic Effects Involving Electron Deficient Nitrogen : Part IV - Schmidt & Beckmann Rearrangements of Isoquinolinones & Isothiachromanone
Venugopal, V. K.,Rao, Nagabhushan,Rahman, M. F.,Bhalerao, U. T.
, p. 156 - 157 (2007/10/02)
Schmidt and Beckmann rearrangements of isoquinolinones (1,2) and isothiachromanone (3) afford exclusively seven-membered lactams (4,5,6) resulting from aryl bond migration.No alkyl bond migration is observed as in chromanones.
