Category: 624-49-7

Kitazaki, Yuki published the artcilePrimary diffuse large B-cell lymphoma of the central nervous system with rapidly progressing lesions after dimethyl fumarate treatment, showing relapsing and remitting symptoms: A case report, Synthetic Route of 624-49-7, the publication is Clinical & Experimental Neuroimmunology (2022), 13(1), 60-65, database is CAplus.

Background : We present a case of B-cell type primary central nervous system lymphoma that rapidly progressed after di-Me fumarate (DMF) administration. Case presentation : An asymptomatic white matter lesion of the left frontal lobe was observed in a 56-yr-old Japanese man on magnetic resonance imaging during a medical checkup. For the subsequent 5 mo, the sporadic white matter lesion showed no change and no contrast effect. He suddenly presented with right upper limb paralysis on day 74. After improvement, he had a recurrence of right upper limb paralysis and diminished vision loss. Based on the 2017 revised McDonald criteria, two attacks, objective clin. evidence of one lesion and cerebrospinal fluid oligoclonal band assay positivity, he was diagnosed with relapsing-remitting multiple sclerosis and administered DMF. Three months after DMF administration, he developed new brain lesions that progressed rapidly; addnl. immunotherapy was ineffective. He was pathol. diagnosed with B-cell type primary central nervous system lymphoma using brain biopsy on day 301. Conclusion : Patients with rapidly progressing white matter lesions after DMF administration should be suspected for B-cell type primary central nervous system lymphoma and pathol. diagnosed using brain biopsy.

Clinical & Experimental Neuroimmunology published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Synthetic Route of 624-49-7.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Prosperini, Luca published the artcileDeterminants of COVID-19-related lethality in multiple sclerosis: a meta-regression of observational studies, Safety of Dimethyl fumarate, the publication is Journal of Neurology (2022), 269(5), 2275-2285, database is CAplus and MEDLINE.

To identify risk factors for an increased lethality of COVID-19 in patients with multiple sclerosis (MS). The author searched scientific databases to identify cohort studies with the number of deaths in patients with MS. The author fitted inverse-variance weighted meta-regressions with random-effects models to identify potential moderators (determinants) of COVID-19-related lethality (outcome). After an independent screening, 18 articles satisfied the eligibility criteria; all data were collected before anti-SARS-COV-2 vaccination was available. Out of 5,634 patients, 111 died, yielding a pooled death rate of 1.97% (95% confidence intervals 1.61-2.33). There was a substantial heterogeneity between the included studies (Q₁₇ = 66.9, p < 0.001; I² = 77.5%), but no relevant publication bias (p = 0.085). Higher lethality was observed in studies including older patients (β = 0.80, p = 0.025) and in studies with higher proportions of patients with comorbidity (β = 0.17, p = 0.046), progressive disease course (β = 0.15, p = 0.027), and current treatment with anti-CD20 agents (β = 0.18, p < 0.001). Otherwise, higher proportions of patients treated with interferon beta (β = – 0.16, p < 0.001) and teriflunomide (β = – 0.11, p = 0.035) were associated with lower lethality. These estimates did not change even in both multivariable meta-regressions including adjustment variables and leave-one-out sensitivity analyses. Except for age and comorbidities, risk factors in common with the general population, the author identified MS-specific determinants influencing the lethality of COVID-19. Our findings suggest the implementation of a risk mitigation plan for patients with progressive MS and for those treated with anti-CD20 agents.

Journal of Neurology published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Safety of Dimethyl fumarate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Hillert, Jan published the artcileA comparative study of teriflunomide and dimethyl fumarate within the Swedish MS Registry, Related Products of esters-buliding-blocks, the publication is Multiple Sclerosis Journal (2022), 28(2), 237-246, database is CAplus and MEDLINE.

Teriflunomide and di-Me fumarate (DMF) are first-line disease-modifying treatments for multiple sclerosis with similar labels that are used in comparable populations. The objective of this study was to compare the effectiveness and persistence of teriflunomide and DMF in a Swedish real-world setting. All relapsing-remitting multiple sclerosis (RRMS) patients in the Swedish MS registry initiating teriflunomide or DMF were included in the anal. The primary endpoint was treatment persistence. Propensity score matching was used to adjust comparisons for baseline confounders. A total of 353 teriflunomide patients were successfully matched to 353 DMF. There was no difference in the rate of overall treatment discontinuation by treatment group across the entire observation period (hazard ratio (HR) = 1.12; 95% confidence interval (CI) = 0.91-1.39; p = 0.277; reference = teriflunomide). Annualised relapse rate (ARR) was comparable (p = 0.237) between DMF (0.07; 95% CI = 0.05-0.10) and teriflunomide (0.09; 95% CI = 0.07-0.12). There was no difference in time to first on-treatment relapse (HR = 0.78; 95% CI = 0.50-1.21), disability progression (HR = 0.55; 95% CI = 0.27-1.12) or confirmed improvement (HR = 1.17; 95% CI = 0.57-2.36). This population-based real-world study reports similarities in treatment persistence, clin. effectiveness and quality of life outcomes between teriflunomide and di-Me fumarate.

Multiple Sclerosis Journal published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Related Products of esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Tsurushima, Katsumasa published the artcileDimethyl Fumarate Induces Apoptosis via Inhibition of NF-κB and Enhances the Effect of Paclitaxel and Adriamycin in Human TNBC Cells., Recommanded Product: Dimethyl fumarate, the publication is International journal of molecular sciences (2022), 23(15), database is MEDLINE.

Triple-negative breast cancer (TNBC) has the poorest prognosis of all breast cancer subtypes. Recently, the activation of NF-κB, which is involved in the growth and survival of malignant tumors, has been demonstrated in TNBC, suggesting that NF-κB may serve as a new therapeutic target. In the present study, we examined whether dimethyl fumarate (DMF), an NF-κB inhibitor, induces apoptosis in TNBC cells and enhances the apoptosis-inducing effect of paclitaxel and adriamycin. Cell survival was analyzed by the trypan blue assay and apoptosis assay. Protein detection was examined by immunoblotting. The activation of NF-κB p65 was correlated with poor prognosis in patients with TNBC. DMF induced apoptosis in MDA-MB-231 and BT-549 cells at concentrations that were non-cytotoxic to the normal mammary cell line MCF-10A. Furthermore, DMF inhibited NF-κB nuclear translocation and Survivin, XIAP, Bcl-xL, and Bcl-2 expression in MDA-MB-231 and BT-549 cells. Moreover, DMF enhanced the apoptosis-inducing effect of paclitaxel and adriamycin in MDA-MB-231 cells. These findings suggest that DMF may be an effective therapeutic agent for the treatment of TNBC, in which NF-κB is constitutively active. DMF may also be useful as an adjuvant therapy to conventional anticancer drugs.

International journal of molecular sciences published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O6, Recommanded Product: Dimethyl fumarate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Wray, Sibyl published the artcileEfficacy and Safety Outcomes with Diroximel Fumarate After Switching from Prior Therapies or Continuing on DRF: Results from the Phase 3 EVOLVE-MS-1 Study, Name: Dimethyl fumarate, the publication is Advances in Therapy (2022), 39(4), 1810-1831, database is CAplus and MEDLINE.

Diroximel fumarate (DRF) is an oral fumarate for relapsing multiple sclerosis (MS) with the same active metabolite as di-Me fumarate (DMF). DRF has a safety/efficacy profile similar to DMF but with improved gastrointestinal (GI) tolerability and low (< 1%) treatment discontinuation due to GI adverse events (AEs). Efficacy and safety outcomes in patients who switched to DRF from other disease-modifying therapies (DMTs) have not been evaluated. EVOLVE-MS-1 is an ongoing, 2-yr, open-label, phase 3 study of DRF in adults with relapsing-remitting MS. Patients either entered as newly enrolled to DRF trials, or from the 5-wk, randomized, head-to-head, phase 3 EVOLVE-MS-2 study of DRF and DMF. This anal. evaluated safety and GI tolerability in patients continuing on DRF (DRF-rollover) or switching from DMF (DMF-rollover) following EVOLVE-MS-2. Safety and efficacy were evaluated in a subset of newly enrolled patients who had received prior glatiramer acetate (GA; GA/DRF) or interferons (IFN; IFN/DRF) as their most recent DMT, prior to switching to DRF in EVOLVE-MS-1. As of Sept. 1, 2020, 1057 patients were enrolled in EVOLVE-MS-1, including 166, 182, 239, and 225 patients in the GA/DRF, IFN/DRF, DRF-rollover, and DMF-rollover groups, resp. Treatment discontinuation due to GI AEs was < 1% in all groups. GA/DRF and IFN/DRF patients experienced improvements from baseline in clin. and radiol. efficacy outcomes, including significantly reduced annualized relapse rates. Rollover patients had low rates of new or recurrent GI AEs (DRF-rollover, 26.8%/4.2%; DMF-rollover, 27.1%/4.9%). After 2 years of DRF exposure, patients with prior GA, IFN, or fumarate treatment had safety outcomes consistent with previous fumarate studies. Efficacy in patients with prior GA or IFN treatment was consistent with previous fumarate studies. The data suggest that transition to DRF from GA, IFN, or DMF is a reasonable treatment strategy, with low rates of discontinuation due to GI AEs.

Advances in Therapy published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C15H12O8, Name: Dimethyl fumarate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Mastorino, Luca published the artcileRisankizumab shows high efficacy and maintenance in improvement of response until week 52, Safety of Dimethyl fumarate, the publication is Dermatologic Therapy (2022), 35(5), e15378, database is CAplus and MEDLINE.

Risankizumab has been recently approved for moderate-to-severe plaque psoriasis; however, real-life studies are scarce. Anal. of possible predictor factors of treatment response are limited to body mass index (BMI) and previous biol. experience. Our objectives were to evaluate the effectiveness and safety of Risankizumab and to investigate on possible predictor factors response. We retrospectively analyzed 166 patients from two centers in Italy who undergone Risankizumab for psoriasis. The proportion of patients achieving a 100%, 90%, 75% of improvement in Psoriasis Area Severity Index (PASI) and PASI <3 were collected at weeks 16, 28, 40, and 52. Study population was analyzed in subgroups to investigate possible predictors of response to Risankizumab since week 40. At the time of anal. 165, 103, 30, and 11 patients had completed 16, 28, 40, and 52 wk of treatment, resp. The mean PASI score decreased from 12.5 ± 5.1 at baseline to 1.9 ± 2.4 at week 16. Similar reductions were observed when considering PASI <3, PASI 75, PASI 90, and PASI 100. Previous biologics failure, different smoking habits, obesity, and joint involvement resulted in a lower response to risankizumab. In particular, significant differences in mean PASI at any time-points was observed between psoriatic arthritis (PSA) and non-PSA patients: 2.7 vs. 1.7 (p = 0.036), 1.9 vs. 0.4 (p = 0.006), and 4.1 vs. 0.5 (p = 0.016) at 16, 28, and 40 wk, resp. No difference in response to risankizumab occurred in the case of involvement of difficult-to-treat areas. In this population, Risankizumab was effective and safe. Smoking habits, joint involvement, obese status, and previous biol. experience may neg. affect treatment response, while difficult body sites involvement have minor impact.

Dermatologic Therapy published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Safety of Dimethyl fumarate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Jana, Kalipada published the artcileAllylboronic Esters as Acceptors in Radical Addition, Boron 1,2-Migration, and Trapping Cascades, SDS of cas: 624-49-7, the publication is Organic Letters (2022), 24(4), 1100-1104, database is CAplus and MEDLINE.

Radical 1,3-carboheteroarylation and 1,3-hydroalkylation of allylboronic esters comprising a 1,2-B shift is reported. Allylboronic esters are generally used in synthesis as allylation reagents where the boronic ester moiety gets lost. In the introduced cascades, alkyl boronic esters were obtained with the B entity remaining in the product. The carboheteroarylation of the allylboronic esters are conducted without metal catalyst and the 1,3-hydroalkylation is achieved using Fe catalysis. Both reactions work efficiently under mild conditions.

Organic Letters published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, SDS of cas: 624-49-7.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Selmani, Aymane published the artcileModularity in the C_sp3 Space-Alkyl Germanes as Orthogonal Molecular Handles for Chemoselective Diversification, Related Products of esters-buliding-blocks, the publication is ACS Catalysis (2022), 12(9), 4833-4839, database is CAplus.

To meet the need for a rapid, streamlined, and potentially automatable mol. synthesis, modular coupling approaches are highly desired. While the diversification of aromatic mols., i.e., C_sp2 space, has greatly advanced, modular syntheses in the C_sp3 space are comparably much less developed. This report explores the potential of alternative functional handles, i.e., alkyl germanes, in this context, which combine features of stability and synthesizability with selective reactivity. The authors show the chemoselective functionalization of alkyl germanes (R-GeEt₃) under photoredox conditions (Giese addition) and the implementation in a modular building block, which allows for selective diversification of C_sp3-halogen vs. C_sp3-Bpin vs. C_sp3-GeEt₃ sites.

ACS Catalysis published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C7H8BFO2, Related Products of esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Sormani, Maria Pia published the artcileBreakthrough SARS-CoV-2 infections after COVID-19 mRNA vaccination in MS patients on disease modifying therapies during the Delta and the Omicron waves in Italy, Computed Properties of 624-49-7, the publication is EBioMedicine (2022), 104042, database is CAplus and MEDLINE.

In this study we aimed to monitor the risk of breakthrough SARS-CoV-2 infection in patients with MS (pwMS) under different DMTs and to identify correlates of reduced protection. This is a prospective Italian multicenter cohort study, long-term clin. follow-up of the CovaXiMS (Covid-19 vaccine in Multiple Sclerosis) study. 1855 pwMS scheduled for SARS-CoV-2 mRNA vaccination were enrolled and followed up to a mean time of 10 mo. The cumulative incidence of breakthrough Covid-19 cases in pwMS was calculated before and after Dec. 2021, to sep. the Delta from the Omicron waves and to account for the advent of the third vaccine dose.1705 pwMS received 2 m-RNA vaccine doses, 21/28 days apart. Of them, 1508 (88.5%) had blood assessment 4 wk after the second vaccine dose and 1154/1266 (92%) received the third dose after a mean interval of 210 days (range 90-342 days) after the second dose. During follow-up, 131 breakthrough Covid-19 infections (33 during the Delta and 98 during the Omicron wave) were observed The probability to be infected during the Delta wave was associated with SARS-CoV-2 antibody levels measured after 4 wk from the second vaccine dose (HR=0.57, p < 0.001); the protective role of antibodies was preserved over the whole follow up (HR=0.57, 95%CI=0.43-0.75, p < 0.001), with a significant reduction (HR=1.40, 95%CI=1.01-1.94, p=0.04) for the Omicron cases. The third dose significantly reduced the risk of infection (HR=0.44, 95%CI=0.21-0.90,p=0.025) during the Omicron wave. The risk of breakthrough SARS-CoV-2 infections is mainly associated with reduced levels of the virus-specific humoral immune response. Supported by FISM – Fondazione Italiana Sclerosi Multipla – cod. 2021/Special-Multi/001 and financed or co-financed with the ‘5 per mille’ public funding.

EBioMedicine published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C13H14N2O, Computed Properties of 624-49-7.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Morozzi, Chiara published the artcileSynthesis and cellular evaluation of click-chemistry probes to study the biological effects of alpha, beta-unsaturated carbonyls, Product Details of C6H8O4, the publication is Redox Biology (2022), 102299, database is CAplus and MEDLINE.

Humans are commonly exposed to α,β-unsaturated carbonyls as both environmental toxins (e.g. acrolein) and therapeutic drugs (e.g. dimethylfumarate, DMFU, a front-line drug for the treatment of multiple sclerosis and psoriasis). These compounds undergo rapid Michael addition reactions with amine, imidazole and thiol groups on biol. targets, with reaction at protein Cys residues being a major reaction pathway. However, the cellular targets of these species (the ‘adductome’) are poorly understood due to the absence of readily identifiable tags or reporter groups (chromophores/fluorophores or antigens) on many α,β-unsaturated carbonyls. Here we report a ‘proof of concept’ study in which we synthesize novel α,β-unsaturated carbonyls containing an alkyne function introduced at remote sites on the α,β-unsaturated carbonyl compounds (e.g. one of the Me groups of dimethylfumarate). The presence of this tag allows ‘click-chem.’ to be used to visualize, isolate, enrich and characterize the cellular targets of such compounds The probes show similar selectivity and reactivity to the parent compounds and compete for cellular targets, yielding long-lived (stable) adducts that can be visualized in intact cells (such as primary human coronary artery smooth muscle cells), and extracted and enriched for subsequent target anal. It is shown using this approach that dimethylfumarate forms adducts with multiple intracellular targets including cytoskeletal, organelle and nuclear species, with these including the rate-limiting glycolytic enzyme, glyceraldehyde-3-phosphate dehydrogenase (GAPDH). This approach should be amenable to use with multiple α,β-unsaturated carbonyls and a wide variety of targets containing nucleophilic sites.

Redox Biology published new progress about 624-49-7. 624-49-7 belongs to esters-buliding-blocks, auxiliary class Inhibitor,Natural product, name is Dimethyl fumarate, and the molecular formula is C6H8O4, Product Details of C6H8O4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics