26516-42-7Relevant articles and documents
Substituted Fused Heteroaromatic Tricyclic Compounds as Kinase Inhibitors and The Use Thereof
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Paragraph 0172; 0223, (2021/05/07)
The disclosure relates to substituted fused heteroaromatic tricyclic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1
Design and synthesis of chiral urea-derived iodoarenes and their assessment in the enantioselective dearomatizing cyclization of a naphthyl amide
Tariq, M.Umair,Moran, Wesley J.
, (2020/10/12)
A novel family of urea-derived chiral iodoarenes was designed and synthesized for use in enantioselective iodine(I/III) catalysis. Their preparation required the development of a bidirectional synthetic strategy. These new chiral iodoarenes were assessed as catalysts in the dearomatizing cyclization of a naphthyl amide and provided moderate yields of product in some cases with low enantioselectivities.
Synthesis of 5,9-Diaza[5]helicenes
Wei?, Aaron,Podlech, Joachim
supporting information, p. 6697 - 6701 (2019/11/02)
A new method for the synthesis of 5,9-diaza[5]helicenes is presented using 2,3-bis(acylamino)-substituted ortho-terphenyls as precursors. Activation of the amide groups and electrophilic substitution at the ortho positions of the adjacent phenyl groups leads to the 5,9-diaza[5]helicenes. A stepwise reaction including protection of the first amino group, amide formation at the second amino group with subsequent cyclization, followed by deprotection, amide formation and cyclization at the first amino group ensures that both electrophilic substitutions take place at sufficiently activated arenes and allows for the different substituents at the diaza[5]helicenes brought in with the amide groups. The terphenyl precursors are synthesized by two Suzuki couplings of suitably substituted building blocks. Three different 5,9-diaza[5]helicenes with aliphatic, alkenyl and methoxycarbonylalkyl substituents were prepared; the latter would allow to attach further functionalities by ester or amide linkage.
Synthetic Indolactam V Analogues as Inhibitors of PAR2-Induced Calcium Mobilization in Triple-Negative Breast Cancer Cells
Stein, Jan,Stahn, Sonja,Neud?rfl, J?rg-M.,Sperlich, Julia,Schmalz, Hans-Günther,Teusch, Nicole
supporting information, p. 147 - 154 (2018/02/06)
Human proteinase-activated receptor 2 (PAR2), a transmembrane G-protein-coupled receptor (GPCR), is an attractive target for a novel anticancer therapy, as it plays a critical role in cell migration and invasion. Selective PAR2 inhibitors therefore have potential as anti-metastatic drugs. Knowing that the natural product teleocidin A2 is able to inhibit PAR2 in tumor cells, the goal of the present study was to elaborate structure–activity relationships and to identify potent PAR2 inhibitors with lower activity against the adverse target, protein kinase C (PKC). For this purpose, an efficient gram-scale total synthesis of indolactam V (i.e., the parent structure of all teleocidins) was developed, and a library of derivatives was prepared. Some compounds were indeed found to exhibit high potency as PAR2 inhibitors at low nanomolar concentrations with improved selectivity (relative to teleocidin A2). The pseudopeptidic fragment bridging the C3 and C4 positions of the indole core proved to be essential for target binding, whereas activity and target selectivity depends on the substituents at N1 or C7. This study revealed novel derivatives that show high efficacy in PAR2 antagonism combined with increased selectivity.
Domino Carbopalladation/C-H Activation as a Quick Access to Polycyclic Frameworks
Saha, Nemai,Wang, Haiwen,Zhang, Shengyi,Du, Yongliang,Zhu, Daqian,Hu, Yumin,Huang, Peng,Wen, Shijun
supporting information, p. 712 - 715 (2018/02/09)
A new type of domino reaction for synthesis of heterocycles fusing the important bioactive cores, such as oxindole, indoline, and isoquinoline, is presented. Upon exposure to the very common palladium catalyst, the conceptually designed N-alkenyl iodobiaryls undergo a sequential carbopalladation/C-H activation to build polycyclic frameworks. These novel unique frameworks may provide structure sources in fragment-based drug discovery.
Nucleotides and nucleosides and methods for their use in DNA sequencing
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Page/Page column 69; 70, (2015/12/18)
The present invention relates generally to labeled and unlabled cleavable terminating groups and methods for DNA sequencing and other types of DNA analysis. More particularly, the invention relates in part to nucleotides and nucleosides with chemically cleavable, photocleavable, enzymatically cleavable, or non-photocleavable groups and methods for their use in DNA sequencing and its application in biomedical research.
A Lewis acid-mediated conformational switch
Knipe, Peter C.,Lingard, Hannah,Jones, Ian M.,Thompson, Sam,Hamilton, Andrew D.
supporting information, p. 7937 - 7941 (2015/01/08)
Molecules that change conformation in response to a stimulus have numerous uses, such as artificial chemoreceptors, novel drug delivery strategies and liquid crystal technology. Here we describe the design, synthesis and conformational behaviour of an iso
TOTAL SYNTHESIS OF THAXTOMIN A ANALOGUES AND THEIR INTERMEDIATES
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Paragraph 0032; 0033, (2014/09/30)
Improved synthetic methods for the production of thaxtomin analogues, particularly thaxtomin A, and intermediates therefore such as substituted tryptophans and in particular, 4-nitro-L-tryptophan, and substituted phenyl acrylic acids are disclosed. Bioass
PH-dependent conformational switching in 2,6-benzamidodiphenylacetylenes
Jones, Ian M.,Lingard, Hannah,Hamilton, Andrew D.
supporting information; scheme or table, p. 12569 - 12571 (2012/02/15)
The conformational equilibrium of a pH-dependent switch based on an intramolecularly H-bonded diphenylacetylene can be predictably biased by using electron-donating or -withdrawing groups (see scheme). Furthermore, protonation of the electron-donating dim
Designed molecular switches: Controlling the conformation of benzamido-diphenylacetylenes
Jones, Ian M.,Hamilton, Andrew D.
scheme or table, p. 3651 - 3653 (2010/10/03)
With the goal of creating a molecular switch, the hydrogen-bonded diphenylacetylene structure has been modified such that an equilibrium now exists between two intramolecular H-bonded states. Through X-ray crystallography and 1H NMR analysis it
