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Indole- and indolizine-glyoxylamides displaying cytotoxicity against multidrug resistant cancer cell lines

We report herein the SAR studies of a series of indole- and indolizine-glyoxylamides that demonstrate substantial in vitro anti-proliferative activities against cancer cell lines, including multidrug resistance (MDR) phenotypes. The in vitro cytotoxic effects have been demonstrated across a wide array of tumor types of various origins (e.g., breast, colon, uterine).

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Properties and Exciting Facts About 3-Methyl-1,2-benzisoxazol-6-ol

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Synthesis of 1,3-bis(heteroaryloxy)-2-hydroxypropanes as symmetrical analogs of DSCG using phase transfer catalyst and their pharmacological activities

1,3-Bis(coumarinoxy)-2-hydroxypropanes (I-III), 1,3-bis(benzisoxazoloxy)-2-hydroxypropanes (IV) and 1,3-bis(benzofuranoxy)-2-hydroxypropanes (V) have been synthesised by treating substituted hydroxycoumarins, benzisoxazoles and benzofurans respectively with epoxide in the presence of a phase transfer catalyst, and found to possess passive cutaneous anaphylaxis and antiallergic activities.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Discovery of isatin and 1H-indazol-3-ol derivatives as D-amino acid oxidase (DAAO) inhibitors

D-Amino acid oxidase (DAAO) is a potential target in the treatment of schizophrenia as its inhibition increases brain D-serine level and thus contributes to NMDA receptor activation. Inhibitors of DAAO were sought testing [6+5] type heterocycles and identified isatin derivatives as micromolar DAAO inhibitors. A pharmacophore and structure-activity relationship analysis of isatins and reported DAAO inhibitors led us to investigate 1H-indazol-3-ol derivatives and nanomolar inhibitors were identified. The series was further characterized by pKa and isothermal titration calorimetry measurements. Representative compounds exhibited beneficial properties in in vitro metabolic stability and PAMPA assays. 6-fluoro-1H-indazol-3-ol (37) significantly increased plasma D-serine level in an in vivo study on mice. These results show that the 1H-indazol-3-ol series represents a novel class of DAAO inhibitors with the potential to develop drug candidates.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Discovery of Benzo[d]isoxazol-3-ol

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Inhibitors of Hepatitis C Virus

Macrocyclic peptides are disclosed having the general formula: wherein R3, R3?, R4, R6, R?, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

A new application about 3,5-Dichlorobenzo[d]isoxazole

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QUINUCLIDINYLOXY-ISOXAZOLE COMPOUNDS AND THEIR THERAPEUTIC USES

Compounds of formula (I): STR1 wherein R 1 is hydrogen, halogen or alkyl; R 2 is hydrogen, alkyl, optionally substituted phenyl or a heterocycle; or R 1 and R 2 together form a group of formula–CR 4 =CR 5–CR 6 =CR 7–, where R. sup. 4, R 5, R 6 and R 7 are hydrogen, halogen, alkyl group, alkoxy, halomethyl, alkylamino, dialkylamino, hydroxy, nitro, aliphatic carboxylic acylamino or amino; and R 3 is piperidyl, substituted piperidyl or quinuclidinyl. The compounds are useful in the treatment and prophylaxis of cognitive disorders, notably senile dementia, including Alzheimer’s disease. Processes for preparing the compounds are also provided.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extended knowledge of Benzo[d]isoxazol-6-ol

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Compositions for dental restoration

A combined chemical-light-polymerization type composition for dental restoration consists of a formulation A composed mainly of a. an ethylenically polymerizable unsaturated compound, b. a photopolymerization initiator and c. a reducing agent, and a formulation B composed mainly of d. a filler and e. an organic perioxide. The formulations A and B are separately packaged and designed to be mixed for use.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extracurricular laboratory:new discovery of 3-Chloro-1,2-benzisoxazole

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Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds

This application relates to compounds of the formula STR1 wherein R1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer’s disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extracurricular laboratory:new discovery of Benzo[d]isoxazol-3-amine

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7-AZASPIRO[3.5]NONANE-7-CARBOXAMIDE COMPOUNDS

Provided herein are 7-azaspiro[3.5]nonane-7-carboxamide compounds and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, cancer and cancer pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Properties and Exciting Facts About 5-Fluorobenzo[d]isoxazol-3(2H)-one

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One Base for Two Shots: Metal-Free Substituent-Controlled Synthesis of Two Kinds of Oxadiazine Derivatives from Alkynylbenziodoxolones and Amidoximes

Different 1,2-migrations and cyclizations of a variety of alkynylbenziodoxolones (EBXs) and amidoximes under one-base conditions are described. This process provides an efficient protocol for the divergent synthesis of two oxadiazine derivatives via switchable selectivity of EBXs controlled by simply varying the substituents of the amidoximes, which feature transition metal-free conditions, simple execution, and high chemoselectivity.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

A new application about Benzo[d]isoxazol-3-amine

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Copper-Catalyzed Asymmetric Arylation of N-Heteroaryl Aldimines: Elementary Step of a 1,4-Insertion

Copper complexes of monodentate phosphoramidites efficiently promote asymmetric arylation of N-azaaryl aldimines with arylboroxines. DFT calculations and experiments support an elementary step of 1,4-insertion in the reaction pathway, a step in which an aryl-copper species adds directly across four atoms of C=N?C=N in the N-azaaryl aldimines.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics