Guanidinium-based derivatives: Searching for new kinase inhibitors
摘要:
Considering the structural similarities between the kinase inhibitor sorafenib and 4,4'-bis-guanidinium derivatives previously prepared by Rozas and co., which display interesting cytotoxicity in cancer cells, we have studied whether this activity could result from kinase inhibition. Five new families have been prepared consisting of unsubstituted and aryl-substituted 3,4'-bis-guanidiniums, 3,4'-bis-2-aminoimidazolinium and 3-acetamide-4'-(4-chloro-3-trifluoromethylphenyl)guanidinium derivatives. Cytotoxicity (measuring the IC50 values) and apoptosis studies in human HL-60 promyelocytic leukemia cells were carried out for these compounds. Additionally, their potential inhibitory effect was explored on a panel of kinases known to be involved in apoptotic pathways. The previously prepared cytotoxic 4,4'-bis-guanidiniums did not inhibit any of these kinases; however, some of the novel 3,4'-substituted derivatives showed a high percentage inhibition of RAF-1/MEK-1, for which the potential mode of binding was evaluated by docking studies. The interesting antitumour properties showed by these compounds open up new exciting lines of investigation for kinase inhibitors as anticancer agents and also highlights the relevance of the guanidinium moiety for protein kinase inhibitors chemical design. (C) 2014 Elsevier Masson SAS. All rights reserved.
FLUORINATED SULFONATE ESTERS OF ARYL KETONES FOR NON-IONIC PHOTO-ACID GENERATORS
申请人:International Business Machines Corporation
公开号:US20180046077A1
公开(公告)日:2018-02-15
Non-ionic photo-acid generating (PAG) compounds were prepared that contain an aryl ketone group having a perfluorinated substituent alpha to the ketone carbonyl. The non-polymeric PAGs release a sulfonic acid when exposed to high energy radiation such as deep UV or extreme UV light. The photo-generated sulfonic acid has a low diffusion rate in an exposed resist layer subjected to a post-exposure bake (PEB) at 100° C. to 150° C., resulting in formation of good line patterns after development. At higher temperatures, the PAGs can also undergo a thermal reaction to form a sulfonic acid. The perfluorinated substituent provides improved thermal stability and hydrolytic/nucleophilic stability.
[EN] PHOTOALIGNING MATERIAL<br/>[FR] MATÉRIAU DE PHOTOALIGNEMENT
申请人:ROLIC AG
公开号:WO2013017467A1
公开(公告)日:2013-02-07
The present invention relates to a copolymer for the photoalignment of liquid crystals comprising a photoreactive group as given below in formula (I), compositions thereof, and its use for optical and electro optical devices, especially liquid crystal devices (LCDs).
The present invention relates to photoreactive compounds that are particularly useful in materials for the alignment of liquid crystals.
本发明涉及光反应性化合物,特别适用于液晶对准材料的制作。
Potential DNA bis-intercalating agents: Synthesis and antitumor activity of novel, conformationally restricted bis(9-aminoacridines)
作者:Gary D. Jaycox、Gordon W. Gribble、Miles P. Hacker
DOI:10.1002/jhet.5570240535
日期:1987.9
A series of bis(9-aminoacridines) bridged by conformationally restricted tethers was synthesized and evaluated against L1210 in vitro. Several of these compounds were found to be highly active in this test system, with ID50 values below 10−7 M. CPK molecular models suggest that this antitumoractivity can be correlated to the ability of these bis(9-aminoacridines) to form bis-intercalative complexes
合成了一系列由构象受限的链桥接的双(9-氨基ac啶),并在体外针对L1210进行了评估。几个这些化合物被认为是在此测试系统高活性的,与ID 50个低于10个值-7 M. CPK分子模型表明,此抗肿瘤活性可以被关联到这些双(9- aminoacridines)以形成双能力-与DNA的插入复合物。
PHOTOALIGNING MATERIAL
申请人:Eckert Jean-Francois
公开号:US20130035446A1
公开(公告)日:2013-02-07
The present invention relates to polymer, homo- or copolymer or oligomer for the photoalignment of liquid crystals comprising a main chain and a side chain, wherein the side chain comprises a difluoromethylene group, compositions thereof, and its use for optical and electro optical devices, especially liquid crystal devices (LCDs).