Some scientific research about Methyl 3-bromobenzofuran-5-carboxylate

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A series of amino acid prodrugs of NVR3-778, a potent anti-HBV candidate currently under phase II clinical trial, were designed and synthesized as new anti-HBV agents. Except for 1e, all of them displayed roughly comparable anti-HBV activity (IC50, 0.28?0.56 muM) to NVR3-778 (IC50, 0.26 muM). Compound 1a, a L-valine ester prodrug of NVR3-778, was found to show significantly improved water solubility (0.7 mg/mL, pH 2) as we expected, and lower cytotoxicity (CC50 > 10 muM) than NVR3-778 (CC50, 4.81 muM). Moreover, 1a also exhibited acceptable PK properties and comparable in vivo efficacy in HBV DNA hydrodynamic mouse model to that of NVR3-778, suggesting it may serve as a promising lead compound for further anti-HBV drug discovery.

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Benzofuran – Wikipedia,
Benzofuran | C8H3968O – PubChem

Discovery of 5-Bromobenzofuran-3(2H)-one

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In this study, the Aldol condensation between benzofuran-3(2H)-ones and ketones or aldehydes mediated by alumina was developed. This simple protocol facilitated the synthesis of various 2-(2-hydroxypropan-2-yl)benzofuran-3(2H)-ones in moderate-to-high yields under mild conditions.

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Benzofuran – Wikipedia,
Benzofuran | C8H3608O – PubChem

Top Picks: new discover of 26238-14-2

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Electric Literature of 26238-14-2, 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.26238-14-2, Name is 5-(Trifluoromethyl)isobenzofuran-1,3-dione, molecular formula is C9H3F3O3. In a article,once mentioned of 26238-14-2

The present invention is directed to N-substituted-5-substituted phthalamic acids which of formula (A). The compounds are considered useful for the treatment of diseases treatment of a neurodegenerative disease, psychiatric disease, motorneuron disease, peripheral neuropathies, pain, neuroinflammation or atherosclerosis such as Alzheimer’s disease and Parkinson’s disease.

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Benzofuran – Wikipedia,
Benzofuran | C8H3661O – PubChem

Some scientific research about 2-Fluoro-5-((3-oxoisobenzofuran-1(3H)-ylidene)methyl)benzonitrile

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763114-25-6, Name is 2-Fluoro-5-((3-oxoisobenzofuran-1(3H)-ylidene)methyl)benzonitrile, belongs to benzofurans compound, is a common compound. SDS of cas: 763114-25-6In an article, once mentioned the new application about 763114-25-6.

Interaction of cyanothioformamides with chalcones gave 3-amino-2-mercaptopyrroles, which have the tautomeric structures (3-aminopyrroline-2-thiones and 3-iminopyrrolidine-2-thiones). The latter was reacted with chloroacetic acid, ethyl chloroacetate, chloroacetamide and 2,3-dichloro-1,4-naphthoquinone to give the corresponding pyrrolothiazines derivatives. On using phenylisocyanate or p-chlorobenzoyl chloride, the corresponding pyrrolothiazole derivatives could be isolated. Replacement of chalcones by maleimides furnished pyrrolopyrrolinediones.

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Benzofuran – Wikipedia,
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Extended knowledge of Methyl 3-bromobenzofuran-5-carboxylate

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The prodrug approach to resolving formulation, delivery, and toxicity limitations on problematic drugs has had its proponents and detractors. Over the last 10 years or so, about 20% of all new small molecule NCEs have been prodrugs-a number that will surprise some. As chemists begin to explore new chemical spaces, larger and more complex molecules present greater drug delivery challenges. Prodrugs provide a means of solving these challenges, but also have their limitations. Prodrugs are becoming an integral part of the drug discovery paradigm in some large pharma companies, and a number of small biotech companies have been built around the design and application of prodrugs to improve drug candidates. Some issues facing the area of prodrug research and the commercialization of prodrugs are discussed.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 501892-90-6, help many people in the next few years.Formula: C10H7BrO3

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Benzofuran – Wikipedia,
Benzofuran | C8H3982O – PubChem

Final Thoughts on Chemistry for 5-(2-Bromoethyl)-2,3-dihydrobenzofuran

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A new copper-catalyzed trifluoromethylarylation reaction of alkynes has been developed. The transformation represents the first example of endo-type carbotrifluoromethylation of unsaturated carbon-carbon bonds and provides efficient access to a variety of CF3-substituted dihydronaphthalenes and chromenes.

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Extended knowledge of Methyl 3-bromobenzofuran-5-carboxylate

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Background: The therapeutic management of people with metastatic colorectal cancer (CRC) who did not respond to first-line treatment represents a formidable challenge. Objectives: To determine the efficacy and toxicity of second-line systemic therapy in people with metastatic CRC. Search methods: We searched the Cochrane Central Register of Controlled Trials (CENTRAL) (the Cochrane Library 2016, Issue 4), Ovid MEDLINE (1950 to May 2016), Ovid MEDLINE In-process & Other Non-Indexed Citations (1946 to May 2016) and Ovid Embase (1974 to May 2016). There were no language or date of publication restrictions. Selection criteria: Randomized controlled trials (RCTs) assessing the efficacy (survival, tumour response) and toxicity (incidence of severe adverse effects (SAEs)) of second-line systemic therapy (single or combined treatment with any anticancer drug, at any dose and number of cycles) in people with metastatic CRC that progressed, recurred or did not respond to first-line systemic therapy. Data collection and analysis: Authors performed a descriptive analysis of each included RCT in terms of primary (survival) and secondary (tumour response, toxicity) endpoints. In the light of the variety of drug regimens tested in the included trials, we could carry out meta-analysis considering classes of (rather than single) anticancer regimens; to this aim, we applied the random-effects model to pool the data. We used hazard ratios (HRs) and risk ratios (RRs) to describe the strength of the association for survival (overall (OS) and progression-free survival (PFS)) and dichotomous (overall response rate (ORR) and SAE rate) data, respectively, with 95% confidence intervals (CI). Main results: Thirty-four RCTs (enrolling 13,787 participants) fulfilled the eligibility criteria. Available evidence enabled us to address multiple clinical issues regarding the survival effects of second-line systemic therapy of people with metastatic CRC.1. Chemotherapy (irinotecan) was more effective than best supportive care (HR for OS: 0.58, 95% CI 0.43 to 0.80; 1 RCT; moderate-quality evidence); 2. modern chemotherapy (FOLFOX (5-fluorouracil plus leucovorin plus oxaliplatin), irinotecan) is more effective than outdated chemotherapy (5-fluorouracil) (HR for PFS: 0.59, 95% CI 0.49 to 0.73; 2 RCTs; high-quality evidence) (HR for OS: 0.69, 95% CI 0.51 to 0.94; 1 RCT; moderate-quality evidence); 3. irinotecan-based combinations were more effective than irinotecan alone (HR for PFS: 0.68, 95% CI 0.60 to 0.76; 6 RCTs; moderate-quality evidence); 4. targeted agents improved the efficacy of conventional chemotherapy both when considered together (HR for OS: 0.84, 95% CI 0.77 to 0.91; 6 RCTs; high-quality evidence) and when bevacizumab was used alone (HR for PFS: 0.67, 95% CI 0.60 to 0.75; 4 RCTs; high-quality evidence). With regard to secondary endpoints, tumour response rates generally paralleled the survival results; moreover, higher anticancer efficacy was generally associated with worse treatment-related toxicity, with the important exception of bevacizumab-containing regimens, where the addition of the targeted agent to chemotherapy did not result in a significant increase in the rate of SAE. Finally, we found that oral (instead of intravenous) fluoropyrimidines significantly reduced the incidence of adverse effects (without compromising efficacy) in people treated with oxaliplatin-based regimens. We could not draw any conclusions on other debated aspects in this field of oncology, such as ranking of treatments (not all possible comparisons have been tested and many comparisons were based on single trials enrolling a small number of participants) and quality of life (virtually no data available). Authors’ conclusions: Systemic therapy offers a survival benefit to people with metastatic CRC who did not respond to first-line treatment, especially when targeted agents are combined with conventional chemotherapeutic drugs. Further research is needed to define the optimal regimen and to identify people who most benefit from each treatment.

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Benzofuran – Wikipedia,
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Discovery of Ethyl 5-nitrobenzofuran-2-carboxylate

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The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formulae (I), (II) and (III). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

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Archives for Chemistry Experiments of 5-Bromobenzofuran-3(2H)-one

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Btk inhibitors and PI3Kdelta inhibitors play crucial roles in the treatment of leukemia, and studies confirmed that the synergetic inhibition against Btk and PI3Kdelta could gain an optimal response. Herein, a series of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives were designed and synthesized as dual Btk/PI3Kdelta kinases inhibitors for the treatment of leukemia. Studies indicated that most compounds could suppress the proliferation of multiple leukemia or lymphoma cells (Raji, HL60 and K562 cells) at low micromolar concentrations in vitro. Further kinase assays identified several compounds could simultaneously inhibit Btk kinase and PI3Kdelta kinase. Thereinto, compound 16b exhibited the best inhibitory activity (Btk: IC50 = 139 nM; PI3Kdelta: IC50 = 275 nM) and showed some selectivity against PI3Kdelta compared to PI3Kbeta/gamma. Finally, the SAR of target compounds was preliminarily discussed combined with docking results. In brief, 16b possessed of the potency for the further optimization as anti-leukemia drugs by inhibiting simultaneously Btk kinase and PI3Kdelta kinase.

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Benzofuran – Wikipedia,
Benzofuran | C8H3614O – PubChem

A new application about Ethyl 6-methoxybenzofuran-2-carboxylate

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Modification of the 1,4-benzodioxan ring present in RX 781094 (1) has not previously been considered.This paper describes a number of analogues of this ring system, including compounds in which one of the oxygen atoms has been replaced by a methylene group and also those in which the ring size has been changed to give, for example, furan and thiophene derivatives.The dihydroxybenzofuranylimidazoline compound 7 is the only analogue possesing presynaptic antagonist potency and selectivity comparable to that of 1.In view of this result, a number of derivatives was prepared to determine the structure-activity relationships within this series.Many derivatives, as well as the parent compound 7, were found to possess presynaptic alpha2-adrenoreceptor antagonist and postsynaptic alpha1-adrenoreceptor partial agonist properties.Two of the selective presynaptic antagonists,13 and 14, possess greater potency and selectivity than that possessed by 1.The 5-chloro derivative 25 is twice as potent as 1 after oral administration but only about half as potent when given intravenously.

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Benzofuran – Wikipedia,
Benzofuran | C8H3794O – PubChem