73948-23-9Relevant academic research and scientific papers
Effects of lipophilicity, protecting group and stereochemistry on the antimalarial activity of carbohydrate-derived thiochromans
Madumo, Gilbert K.,Moshapo, Paseka T.,Kinfe, Henok H.
, p. 817 - 833 (2018/01/10)
A series of novel carbohydrate-derived thiochromans has been successfully synthesized in order to investigate the influence of alkyl substituents on the aromatic ring of the thiophenol moiety in addition to the effect of protecting groups and stereochemistry on the sugar component of the target molecules. Results from the evaluation of the thiochromans for their antimalarial activity against the chloroquine-sensitive (3D7) strain of Plasmodium falciparum suggest that the presence of short chain alkyl substituents, a benzyl ether protecting group and equatorial orientation of the C-4 substituent on the sugar moiety are crucial structural features that impart high antimalarial activity.
Development of sulfonamide AKT PH domain inhibitors
Ahad, Ali Md.,Zuohe, Song,Du-Cuny, Lei,Moses, Sylvestor A.,Zhou, Li Li,Zhang, Shuxing,Powis, Garth,Meuillet, Emmanuelle J.,Mash, Eugene A.
experimental part, p. 2046 - 2054 (2011/05/05)
Disruption of the phosphatidylinositol 3-kinase/AKT signaling pathway can lead to apoptosis in cancer cells. Previously we identified a lead sulfonamide that selectively bound to the pleckstrin homology (PH) domain of AKT and induced apoptosis when present at low micromolar concentrations. To examine the effects of structural modification, a set of sulfonamides related to the lead compound was designed, synthesized, and tested for binding to the expressed PH domain of AKT using a surface plasmon resonance-based competitive binding assay. Cellular activity was determined by means of an assay for pAKT production and a cell killing assay using BxPC-3 cells. The most active compounds in the set are lipophilic and possess an aliphatic chain of the proper length. Results were interpreted with the aid of computational modeling. This paper represents the first structure-activity relationship (SAR) study of a large family of AKT PH domain inhibitors. Information obtained will be used in the design of the next generation of inhibitors of AKT PH domain function.
SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME
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Page/Page column 100-101, (2009/12/02)
Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
Keratinocyte growth inhibitors and hydroxamic acid derivatives
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Page 26, (2010/02/06)
This invention relates to a keratinocyte-proliferation inhibitor comprising as active ingredient a compound having an activity of inhibiting the solubilization of heparin-binding EGF-like growth factor bound to cell membranes and a compound of the formula (I); or pharmaceutically acceptable salt thereof, wherein R1, R2, R3 are hydrogen atom or alkyl and X is substituted benzene or the like.
Photochromism of Hemithioindigo Derivatives. I. Preparation and Photochromic Properties in Organic Solvents
Yamaguchi, Takeo,Seki, Takahiro,Tamaki, Takashi,Ichimura, Kunihiro
, p. 649 - 656 (2007/10/02)
Thirteen hemithioindigo (HT) derivatives bearing alkyl chains are newly synthesized and their photochromism and emission properties are investigated.The Z/E photoisomerisms of these compounds in organic solvents are essentially in agreeement with data reported by Mostoslavskii and Izmail'skii (J.Gen.Chem.USSR, Engl Transl.), 31, 21 (1961), and subsequent papers).At 77 K both the E and Z isomers of HT chromophore emit fluoresscences of comparable intensities, whereas at room temperature very weak fluorescence is observed only from the Z isomer.Examination of repeatable numbers of Z/E photoisomerization reveals that the HT chromophore possesses remarkable inherent photofatigue resistance.
