847609-99-8Relevant academic research and scientific papers
The synthesis and BK channel-opening activity of N-acylaminoalkyloxime derivatives of dehydroabietic acid
Cui, Yong-Mei,Liu, Xin-Lan,Zhang, Wen-Ming,Lin, Hai-Xia,Ohwada, Tomohiko,Ido, Katsutoshi,Sawada, Kohei
, p. 283 - 287 (2016)
A series of N-acylaminoalkyloxime derivatives of dehydroabietic acid were synthesized and evaluated for BK channel-opening activities in an assay system of CHO-K1 cells expressing hBKα channels. The structure-activity relationship study revealed that a non-covalent interaction between the S atom of the 2-thiophene and the carbonyl O atom may contribute to conformation restriction for interaction with the ion channel. This research could guide the design and synthesis of novel abietane-based BK channel opener.
Synthesis of fluorescent molecular probes based on cis-cinnamic acid and molecular imaging of lettuce roots
Fukuda, Hiroshi,Nishikawa, Keisuke,Fukunaga, Yukihiro,Okuda, Katsuhiro,Kodama, Kozue,Matsumoto, Kenji,Kano, Arihiro,Shindo, Mitsuru
, p. 6492 - 6498 (2016/09/23)
We synthesized azo dye- and fluorescence-labeled cis-cinnamic acid analogues possessing inhibitory activity against lettuce root growth and a trans-isomer without bioactivity as a control probe. The radicles incubated with the azo dye-labeled analogue were stained red, with their tips especially deeply dyed. The fluorescent images of the radicles incubated with each of these molecular probes depicted that the root cap was fluorescence-stained. However, images of the control radicles prepared by staining with the trans-isomer fluorescent probe did not show emission at the root cap. These contrasts suggest specific localization of the cis-cinnamate analogue at the columella cells.
Synthesis and biological evaluation of RGD-Conjugated MEK1/2 kinase inhibitors for integrin-targeted cancer therapy
Li, Xiaoxiao,Hou, Jianjun,Wang, Chao,Liu, Xinjie,He, Hongyan,Xu, Ping,Yang, Zhenjun,Chen, Zili,Wu, Yun,Zhang, Lihe
, p. 13957 - 13978 (2014/01/06)
Two novel series of RGD-MEKI conjugates derived from a MEK1/2 kinase inhibitor-PD0325901-have been developed for integrin receptor mediated anticancer therapy. The first series, alkoxylamine analog RGD-MEKI conjugates 9a-g showed anti-proliferation activity in melanoma A375 cells by the same mechanism as that of PD0325901. PEGylation increased the IC50 value of 9f three-fold in the A375 assay, and the multi-cRGD peptide cargo significantly improved the receptor specific anti-proliferation activity of 9g in integrin-overexpressing U87 cells. In the second series, RGD-PD0325901 13 exhibited significantly increased antitumor properties compared to the alkoxylamine analogs by both inhibition of the ERK pathway activity and DNA replication of the cancer cells. Furthermore, 13 displayed more potent anti-proliferation activity in the U87 assay than PD0325901 in a dose-dependent manner. All these data demonstrate that RGD-MEKI conjugates with an ester bond linkage enhanced anticancer efficacy with improved targeting capability toward integrin-overexpressing tumor cells.
