29682-15-3Relevant articles and documents
SYNTHETIC RETINOIDS FOR USE IN RAR ACTIVATION
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Page/Page column 18-19, (2020/09/27)
The present invention relates to compounds of formula I: in which A1-A7 and R1 to R5 are defined herein, for use in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). The invention also relates to pharmaceutical compounds comprising such compounds, and related methods of treatment. In an aspect, the invention relates to a method of screening compounds for therapeutic potential in the treatment of a condition or disease which is alleviated by the activation of retinoic acid receptors (RAR). Aspects of the invention relate to novel compounds of formula I in which at least one of A1 to A3 is N or at least one of A4 is CR12 or A5 is CR13 in which R12/R13 is halogen.
HETEROCYCLIC INTEGRIN AGONISTS
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Paragraph 0246; 0247, (2018/07/29)
The present invention provides polycyclic oxothioxoimidazolidines, dioxoimidazolines, oxothioxooxazolidines, dioxooxazolidines, and related compounds, which are useful as integrin agonists. Methods for the treatment of integrin-mediated diseases such as cancer are also described.
Structure–Activity Relationship of Propargylamine-Based HDAC Inhibitors
Wünsch, Matthias,Senger, Johanna,Schultheisz, Philipp,Schwarzbich, Sabrina,Schmidtkunz, Karin,Michalek, Carmela,Kla?, Michaela,Goskowitz, Stefanie,Borchert, Philipp,Praetorius, Lucas,Sippl, Wolfgang,Jung, Manfred,Sewald, Norbert
supporting information, p. 2044 - 2053 (2017/12/07)
As histone deacetylases (HDACs) play an important role in the treatment of cancer, their selective inhibition has been the subject of various studies. These continuous investigations have given rise to a large collection of pan- and selective HDAC inhibitors, containing diverse US Food and Drug Administration (FDA)-approved representatives. In previous studies, a class of alkyne-based HDAC inhibitors was presented. We modified this scaffold in two previously neglected regions and compared their cytotoxicity and affinity toward HDAC1, HDAC6, and HDAC8. We were able to show that R-configured propargylamines contribute to increased selectivity for HDAC6. Docking studies on available HDAC crystal structures were carried out to rationalize the observed selectivity of the compounds. Substitution of the aromatic portion by a thiophene derivative results in high affinity and low cytotoxicity, indicating an improved drug tolerance.