10602-04-7Relevant articles and documents
Synthesis of chiral helical poly(hydroxyl-containing phenylacetylene) membranes by in-situ depinanylsilylation and their enantioselective permeabilities
Teraguchi, Masahiro,Mottate, Kazuomi,Kim, Sun-Young,Aoki, Toshiki,Kaneko, Takashi,Hadano, Shingo,Masuda, Toshio
, p. 6367 - 6373 (2005)
Two new chiral helical poly(hydroxyl-containing phenylacetylene) membranes without the coexistence of any other chiral moieties were prepared in the following manner: (1) synthesis and homo-or copolymerization of two new chiral pinanylsiloxy-containing ph
Synthesis of siRNAs incorporated with cationic peptides R8G7 and R8A7 and the effect of the modifications on siRNA properties
Honda, Kenji,Kajino, Ryohei,Kakisawa, Yuri,Maeda, Yusuke,Matsubara, Miho,Ozaki, Koki,Ueno, Yoshihito
, p. 34815 - 34824 (2020)
Small interfering RNA (siRNA) can be used as an innovative next-generation drug. However, there are several challenges in the therapeutic application of siRNAs, including their low cell membrane permeability. In this study, we designed and synthesized siR
Chelation control through the coordination of Lewis acids to an acetylenic π-bond
Asao, Naoki,Asano, Toru,Ohishi, Takeshi,Yamamoto, Yoshinori
, p. 4817 - 4818 (2000)
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Design, synthesis and antitumor evaluations of nucleoside base hydroxamic acid derivatives as DNMT and HDAC dual inhibitors
Sun, Qinsheng,Dai, Qiuzi,Zhang, Cunlong,Chen, Yan,Zhao, Lei,Yuan, Zigao,Jiang, Yuyang
, p. 2479 - 2483 (2021)
DNA methyltransferase (DNMT) and histone deacetylase (HDAC) are well recognized epigenetic targets for discovery of antitumor agents. In this study, we designed and synthesized a series of nucleoside base hydroxamic acid derivatives as DNMT and HDAC dual inhibitors. MTT assays and enzymatic inhibitory activity tests indicated that compound 204 exhibited potent DNMT1 and HDAC1/6 inhibitory potency simultaneously in enzymatic levels and at cellular levels, inducing hypomethylation of p16 and hyperacetylation of histones H3K9 and H4K8. Besides, 204 remarkably inhibited proliferation against cancer cells U937 by prompting G0/G1 cell cycle arrest. Molecular docking models explained the functional mechanism of 204 inhibiting DNMT1 and HDAC. Preliminary studies on metabolic profiles revealed that 204 showed desirable stability in liver microsomes. Our study suggested that 204 inhibiting DNMT and HDAC concurrently can be a potential lead compound for epigenetic cancer therapy.
Creating Dynamic Nanospaces in Solution by Cationic Cages as Multirole Catalytic Platform for Unconventional C(sp)?H Activation Beyond Enzyme Mimics
Li, Kang,Wu, Kai,Lu, Yu-Lin,Guo, Jing,Hu, Peng,Su, Cheng-Yong
supporting information, (2021/12/14)
Herein we demonstrate that, based on the creation of dynamic nanospaces in solution by highly charged positive coordination cage of [Pd6(RuL3)8]28+, multirole and multi-way cage-confined catalysis is accomplisha
ANTIBACTERIAL AND ANTIFUNGAL PLEUROMUTILIN CONJUGATES
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Page/Page column 26; 29, (2021/11/06)
Compounds of formula (1) comprising a pleuromutilin backbone with a triazole based side-group at C22 are provided. The compounds can be used for treatment of bacterial infections and fungal infections. Importantly, infections caused by multidrug-resistant