362665-07-4Relevant articles and documents
Efficient and stable small molecule agonist of v [gamma] 9v delta 2t cells
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Paragraph 0694-0696, (2019/04/30)
The invention relates to a formula (I) compound as an efficient and stable small molecule agonist of v [gamma] 9v delta 2t cells, wherein the groups are defined in the specification and the claims. The present invention also relates to pharmaceutical compositions containing the formula (I) compound and use thereof in the treatment of proliferative diseases.
Structure Property Relationships of Carboxylic Acid Isosteres
Lassalas, Pierrik,Gay, Bryant,Lasfargeas, Caroline,James, Michael J.,Tran, Van,Vijayendran, Krishna G.,Brunden, Kurt R.,Kozlowski, Marisa C.,Thomas, Craig J.,Smith, Amos B.,Huryn, Donna M.,Ballatore, Carlo
, p. 3183 - 3203 (2016/05/19)
The replacement of a carboxylic acid with a surrogate structure, or (bio)-isostere, is a classical strategy in medicinal chemistry. The general underlying principle is that by maintaining the features of the carboxylic acid critical for biological activity, but appropriately modifying the physicochemical properties, improved analogs may result. In this context, a systematic assessment of the physicochemical properties of carboxylic acid isosteres would be desirable to enable more informed decisions of potential replacements to be used for analog design. Herein we report the structure-property relationships (SPR) of 35 phenylpropionic acid derivatives, in which the carboxylic acid moiety is replaced with a series of known isosteres. The data set generated provides an assessment of the relative impact on the physicochemical properties that these replacements may have compared to the carboxylic acid analog. As such, this study presents a framework for how to rationally apply isosteric replacements of the carboxylic acid functional group.
Instantaneous deprotection of tosylamides and esters with Sml 2/amine/water
Ankner, Tobias,Hilmersson, Goeran
supporting information; experimental part, p. 503 - 506 (2009/07/11)
(Chemical Equation Presented) Sml2/amine/water mediates instantaneous cleavage of tosyl amides and tosyl esters. Highly hindered, sensitive and functionalized substrates were successfully deprotected in near quantitative yield.