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Palladium-catalyzed allylic esterifications of secondary homoallyl alcohols with acids via sequential retro-allylation and esterification are demonstrated, affording the corresponding allyl ester in up to 99% yield. The electron effect of the substituent of the secondary alcohol was found to be crucial to the selective C-C bond cleavage.

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A cationic ruthenium(II) complex enabled efficient oxidative alkenylations of anilides in water as a green solvent and proved applicable to double C – H bond functionalizations of (hetero)aromatic amides with ample scope. Detailed studies provided strong support for a change of ruthenation mechanism in the two transformations, with an irreversible metalation as the key step in cross-dehydrogenative alkenylations of benzamides.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1717O – PubChem

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We report a novel class of biaryl polyamides highly selective for G-quadruplex DNA, and with significant cytotoxicity in several cancer cell lines; they form planar U-shaped structures that match the surface area dimensions of a terminal G-quartet in quadruplex structures rather than the grooves of duplex DNA.

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Benzofuran – Wikipedia,
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Several phosphonic diethyl esters were synthesized and their calcium antagonistic activity evaluated in vitro.The diethyl phosphonate group was condensed on substituted , <(2-benzofuranyl)phenylmethyl>, <(4-(diphenylmehyl-1-piperazinyl) methyl>, <4-(4-diphenylmethyl-1-piperazinyl methyl) phenylmethyl>, and <4-(3-phenyl-2-propenyl)-1-piperazinyl methyl> groups.Despite the presence of the diethyl phosphonate moiety and the benzhydrylpiperazinyl group, both present in potent calcium antagonist structures, only 1 of the 19 synthesis compounds exhibited a calcium antagonistic profile. diethyl phosphonate / benzhydryl piperazine / calcium antagonist

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Benzofuran – Wikipedia,
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To find novel non-hydroxamate histone deacetylase (HDAC) inhibitors, a series of compounds modeled after suberoylanilide hydroxamic acid (SAHA) was designed and synthesized. In this series, compound 7, in which the hydroxamic acid of SAHA is replaced by a thiol, was found to be as potent as SAHA, and optimization of this series led to the identification of HDAC inhibitors more potent than SAHA. In cancer cell growth inhibition assay, S-isobutyryl derivative 51 showed strong activity, and its potency was comparable to that of SAHA. The cancer cell growth inhibitory activity was verified to be the result of histone hyperacetylation and subsequent induction of p21WAF1/CIP1 by Western blot analysis. Kinetical enzyme assay and molecular modeling suggest the thiol formed by enzymatic hydrolysis within the cell interacts with the zinc ion in the active site of HDACs.

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A series of novel 2,5-disubstituted-1,3,4-oxadiazole derivatives were synthesized and screened for their antimicrobial and antioxidant activities. The assay indicated that compounds 3c, 3d, and 3i exhibited comparable antibacterial and antioxidant activity with first-line drugs. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.

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Benzofuran – Wikipedia,
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The invention concerns a compound of the formula (I): wherein, for example:R1 is of the formula ?NHC(=O)Rb wherein Rb is, for example, (1-4C)alkyl;R2 and R3 are hydrogen or fluoro;R2 and R3 are hydrogen or fluoro;D is O;R4 and R5 are hydrogen, (1-4C)alkyl or AR-oxymethyl;AR is phenyl or phenyl(1-4C)alkyl;R6 is hydrogen;>A?B? is of the formula >C=C(Ra)?, >CHCHRa?, or >C(OH)CHRa? (> represents two single bonds) wherein Ra is hydrogen or (1-4C)alkyl;and pharmaceutically-acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

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Benzofuran – Wikipedia,
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A series of benzimidazole derivatives with a phenylcyclohexyl acetic acid group as DGAT-1 inhibitors was developed. Among the benzimidazole series, compound 5k showed submicromolar in vitro activity toward human and mouse DGAT-1, good selectivity toward DGAT-2, human liver metabolic stability, and pharmacokinetic (PK) and safety profiles such as hERG, CYP and acute toxicity. Additionally, 5k showed good in vivo efficacy in 4 weeks study with DIO mouse model.

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Ligand efficiency has proven to be a valuable concept for optimization of leads in the early stages of drug design. Taking this one step further, group efficiency (GE) evaluates the binding efficiency of each appendage of a molecule, further fine-tuning the drug design process. Here, GE analysis is used to systematically improve the potency of inhibitors of Mycobacterium tuberculosis pantothenate synthetase, an important target in tuberculosis therapy. Binding efficiencies were found to be distributed unevenly within a lead molecule derived using a fragment-based approach. Substitution of the less efficient parts of the molecule allowed systematic development of more potent compounds. This method of dissecting and analyzing different groups within a molecule offers a rational and general way of carrying out lead optimization, with potential broad application within drug discovery.

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The ruthenium-catalyzed oxidative vinylation of thiophene-2-carboxylic acids with alkenes efficiently proceeds through directed C-H bond cleavage to give the corresponding 3-vinylated products. Similarly, benzothiophene-, benzofuran-, pyrrole-, and indolecarboxylic acids also undergo regioselective vinylation.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H2002O – PubChem