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The synthesis of a novel series of aminoquinoline derivatives 1a-p and their antiproliferative activities against A375 human melanoma cell line were described. Most compounds showed superior antiproliferative activities to Sorafenib as a reference compound. Among them, quinolinyloxymethylphenyl compounds 1k and 1l exhibited potent activities (IC50 = 0.77 and 0.79 muM, respectively) and excellent selectivity against melanoma and fibroblast cell lines.

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A library of spirooxindoles containing varied elements of structural and stereochemical diversity has been constructed via a three step, one pot nitrile hydrozirconation-acylation-cyclization reaction sequence from common acyclic indole intermediates. The resulting library was evaluated for novelty through comparison with MLSMR and Maybridge compound collections.

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Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R4, R5, R8, R10, R11, X1, X2, X3, X9, X12, and Z are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with GPR6.

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Isoxazole – Wikipedia,
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NOVEL TETRAHYDROPYRIDOPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

The present invention provides novel compounds having the general formula (I) wherein R1, R2 and Z are as described herein, compositions including the compounds and methods of using the compounds.

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Isoxazole – Wikipedia,
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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 3405-77-4, name is 5-Methylisoxazole-3-carboxylic acid, introducing its new discovery. category: Isoxazoles

Diacylfuroxans Are Masked Nitrile Oxides That Inhibit GPX4 Covalently

GPX4 represents a promising yet difficult-to-drug therapeutic target for the treatment of, among others, drug-resistant cancers. Although most GPX4 inhibitors rely on a chloroacetamide moiety to modify covalently the protein’s catalytic selenocysteine residue, the discovery and mechanistic elucidation of structurally diverse GPX4-inhibiting molecules have uncovered novel electrophilic warheads that bind and inhibit GPX4. Here, we report our discovery that diacylfuroxans can act as masked nitrile oxide prodrugs that inhibit GPX4 covalently with unique cellular and biochemical reactivity compared to existing classes of GPX4 inhibitors. These observations illuminate a novel molecular mechanism of action for biologically active furoxans and also expand the collection of reactive groups capable of targeting GPX4.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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BENZPYRAZOL DERIVATIVES AS INHIBITORS OF PI3 KINASES

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Chemical oxidation of an anticonvulsant N-(5′-methylisoxazol-3-yl) 2,6- dimethylbenzamide (D2916)

The new anticonvulsant N-(5′-methylisoxazol-3-yl)-2,6-dimethylbeazamide (D2916), which presents two kinds of methyl groups which could be oxidized, was submitted to various chemical oxidizing agents. Several sites and degrees of oxidation were observed. The main oxidized site was the arylmethyl group without cleavage of the isoxazole ring, leading via carboxylic acid and primary alcohol intermediates to phthalimide and lactame derivatives. In no case was the methyl group of the isoxazole moiety hydroxylated.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Synthetic Route of 3405-77-4, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.3405-77-4, Name is 5-Methylisoxazole-3-carboxylic acid, molecular formula is C5H5NO3. In a article,once mentioned of 3405-77-4

2-AMINO-5-SUBSTITUTED PYRIMIDINE INHIBITORS

Compounds having the general structure (A) are provided. The compounds of the invention are capable of inhibiting kinases, such as members of the Src kinase family, Vegfr and various other specific receptor and non-receptor kinases. Formula (I):

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Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line

The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC50 = 0.006 muM) and good selectivity over HS27 fibroblast cell line.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Synthetic Route of 3405-77-4, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 3405-77-4, molcular formula is C5H5NO3, introducing its new discovery.

Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem