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Protein tyrosine phosphatases (PTPs) play a critical role in physiological signaling pathways by controlling the level of tyrosine phosphorylation. The past decade has seen a vast increase in both academic and industrial interest in PTPs and their relevance as potential therapeutic targets, with several PTP inhibitors recently entering clinical trials. Despite these developments, there are numerous examples of failed PTP drug discovery programs, such that PTPs have attained a reputation as ‘undruggable’ targets. This review attempts to illustrate the many obstacles that must be overcome to successfully develop a PTP drug, ranging from validation of PTPs as therapeutic targets to the difficulties of assessing the true inhibitory nature of apparently well-behaved compounds, along with the need to balance the physiocochemical properties required for active site binding with the characteristics needed for in vivo activity. A number of examples of structure-based design are presented, along with cautionary tales of PTP inhibitor programs that have failed due to unexpected shortcomings.

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Benzofuran – Wikipedia,
Benzofuran | C8H1741O – PubChem

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The reusable sulfoximine directing-group-assisted Ru(II)-catalyzed chemo- and regioselective ortho-C-H alkenylation of arenes and heteroarenes with acrylates and alpha,beta-unsaturated ketones/vinyl sulfone is shown. The N-aroyl sulfoximine undergoes annulation with diphenylacetylene, delivering isoquinolinones and methyl phenyl sulfoxide. The present protocol is successfully employed for the synthesis of the EP3 receptor antagonist analogue.

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Benzofuran – Wikipedia,
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Generation of structurally new matrix metalloproteinase inhibitors was successfully carried out using an in silico technique. In order to identify the small fragment interacting with residues in the S1? pocket of MMP-1 through hydrogen bonds, we performed in silico screening using the LUDI program. As a result, acetyl-l-alanyl-(N-methyl)amide (Ac-l-Ala-NHMe) was selected to link with another fragment, hydroxamic acid that interacted with catalytic zinc. By this approach, the l-glutamic acid derivative 2b was discovered to be a new type of matrix metalloproteinase inhibitor. Further transformation to reduce its peptidic nature and improve activity yielded nonpeptidic lead compounds as inhibitors of MMP-1, -2, -3, and -9.

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Benzofuran – Wikipedia,
Benzofuran | C8H1987O – PubChem

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A rhodium(III)-catalyzed redox-neutral coupling of alpha-trifluoromethylacrylic acid with bezamides proceeds smoothly accompanied by amide-directed C?H bond cleavage to produce beta-[2-(aminocarbonyl)phenyl]-alpha-trifluoromethylpropanoic acid derivatives. One of the products can be transformed to a trifluoromethyl substituted heterocyclic compound. In addition, the redox-neutral coupling of alpha-trifluoromethylacrylic acid with related aromatic substrates possessing a nitrogen-containing directing group can also be conducted under similar conditions.

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Benzofuran – Wikipedia,
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Two series of new PAR1 antagonists have been identified. The first incorporates a cinnamoylpiperidine motif and the second a cinnamoylpyridine pattern. The synthesis, biological activity and structure-activity relationship of these compounds are presented. In each series, one analog showed potent in vivo antithrombotic activity in a rat AV shunt model, with up to 53% inhibition at 1.25 mpk iv for compound 30.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1930O – PubChem

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A novel and efficient I2/DMSO mediated metal-free strategy is presented for the direct C-C bond cleavage of aryl-/heteroaryl- or aliphatic alpha-ketoaldehydes by C2-decarbonylation and C1-carbonyl oxidation to give the corresponding carboxylic acids followed by esterification in one pot, offering excellent yields in both the steps. Here, DMSO acts as the oxygen source/oxidant and this reaction works very well under both conventional heating and microwave irradiation. This is a very simple and convenient protocol.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2006O – PubChem

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Novel benzofuran-2-carboxylic acids, exemplified by 29, 38 and 39, have been discovered as potent Pim-1 inhibitors using fragment based screening followed by X-ray structure guided medicinal chemistry optimization. The compounds demonstrate potent inhibition against Pim-1 and Pim-2 in enzyme assays. Compound 29 has been tested in the Ambit 442 kinase panel and demonstrates good selectivity for the Pim kinase family. X-ray structures of the inhibitor/Pim-1 binding complex reveal important salt-bridge and hydrogen bond interactions mediated by the compound’s carboxylic acid and amino groups.

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Benzofuran – Wikipedia,
Benzofuran | C8H2029O – PubChem

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This invention provides novel aryl piperazine derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, D2-like and 5-HT2 receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders incl. schizophrenia

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Benzofuran – Wikipedia,
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A Cu(I)-catalyzed regioselective cross-dehydrogenative coupling of indoline with a variety aryl and alkyl carboxylic acids is described. The divergent process for the oxygenation was achieved in satisfactory yields under additive free conditions, which provides an efficient strategy for the regioselective C7 functionalization of indolines using inexpensive copper catalyst. Oxygen as the sole oxidant is required in this protocol. The method is tolerated by a wide range of functional groups. Preliminary mechanistic study provided support for a reversible C?H bond metallation step. (Figure presented.).

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Benzofuran – Wikipedia,
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A practical solvent-free method for the preparation of 2-furyl-5-aryl-oxyacetylamido-1,3,4-thiadiazoles under microwave irradiation is described.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2013O – PubChem