Tag: M.W=200-350

Ek, Frida published the artcileSorafenib and nitazoxanide disrupt mitochondrial function and inhibit regrowth capacity in three-dimensional models of hepatocellular and colorectal carcinoma, COA of Formula: C12H9N3O5S, the main research area is sorafenib nitazoxanide hepatocellular colorectal carcinoma three dimensional model.

Quiescent cancer cells in malignant tumors can withstand cell-cycle active treatment and cause cancer spread and recurrence. Three-dimensional (3D) cancer cell models have led to the identification of oxidative phosphorylation (OXPHOS) as a context-dependent vulnerability. The limited treatment options for advanced hepatocellular carcinoma (HCC) and colorectal carcinoma (CRC) metastatic to the liver include the multikinase inhibitors sorafenib and regorafenib. Off-target effects of sorafenib and regorafenib are related to OXPHOS inhibition; however the importance of this feature to the effect on tumor cells has not been investigated in 3D models. We began by assessing global transcriptional responses in monolayer cell cultures, then moved on to multicellular tumor spheroids (MCTS) and tumoroids generated from a CRC patient. Cells were treated with chemotherapeutics, kinase inhibitors, and the OXPHOS inhibitors. Cells grown in 3D cultures were sensitive to the OXPHOS inhibitor nitazoxanide, sorafenib, and regorafenib and resistant to other multikinase inhibitors and chemotherapeutic drugs. Furthermore, nitazoxanide and sorafenib reduced viability, regrowth potential and inhibited mitochondrial membrane potential in an additive manner at clin. relevant concentrations This study demonstrates that the OXPHOS inhibition caused by sorafenib and regorafenib parallels 3D activity and can be further investigated for new combination strategies.

Scientific Reports published new progress about Cancer recurrence. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, COA of Formula: C12H9N3O5S.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Swale, Christopher published the artcileMetal-captured inhibition of pre-mRNA processing activity by CPSF3 controls Cryptosporidium infection, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is CPSF metal water interaction cryptosporidium infection.

Cryptosporidium is an intestinal pathogen that causes severe but self-limiting diarrhea in healthy humans, yet it can turn into a life-threatening, unrelenting infection in immunocompromised patients and young children. Severe diarrhea is recognized as the leading cause of mortality for children below 5 years of age in developing countries. The only approved treatment against cryptosporidiosis, nitazoxanide, has limited efficacy in the most vulnerable patient populations, including malnourished children, and is ineffective in immunocompromised individuals. Here, we investigate inhibition of the parasitic cleavage and polyadenylation specificity factor 3 (CPSF3) as a strategy to control Cryptosporidium infection. We show that the oxaborole AN3661 selectively blocked Cryptosporidium growth in human HCT-8 cells, and oral treatment with AN3661 reduced intestinal parasite burden in both immunocompromised and neonatal mouse models of infection with greater efficacy than nitazoxanide. Furthermore, we present crystal structures of recombinantly produced Cryptosporidium CPSF3, revealing a mechanism of action whereby the mRNA processing activity of this enzyme is efficiently blocked by the binding of the oxaborole group at the metal-dependent catalytic center. Our data provide insights that may help accelerate the development of next-generation anti-Cryptosporidium therapeutics.

Science Translational Medicine published new progress about Cell proliferation. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Asawa, Rosita R. published the artcileA Comparative Study of Target Engagement Assays for HDAC1 Inhibitor Profiling, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is cancer neurodegeneration HDAC1 NanoBRET SplitLuc CETSA; HDAC1; NanoBRET; SplitLuc CETSA; epigenetic compound library; profiling; qHTS; target engagement.

Histone deacetylases (HDACs) are epigenetic modulators linked to diseases including cancer and neurodegeneration. Given their therapeutic potential, highly sensitive biochem. and cell-based profiling technologies have been developed to discover small-mol. HDAC inhibitors. Ultimately, the therapeutic action of these inhibitors is dependent on a phys. engagement with their intended targets in cellular and tissue environments. Confirming target engagement in the cellular environment is particularly relevant for HDACs since they function as part of cell type-specific multiprotein complexes. Here we implemented two recently developed high-throughput target engagement technologies, NanoBRET and SplitLuc CETSA, to profile 349 compounds in the Epigenetic-Focused collection for HDAC1 binding. We found that the two HDAC1 target engagement assays correlated well with each other and with orthogonal activity-based assays, in particular those carried out in cellular environments rather than with isolated HDAC proteins. The assays detected a majority of the previously described HDAC1 inhibitors in the collection and, importantly, triaged HDAC inhibitors known to target other HDACs.

SLAS Discovery published new progress about Cell proliferation. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Azeem, Waqas published the artcileEvaluation of β-Catenin Inhibition of Axitinib and Nitazoxanide in Human Monocyte-Derived Dendritic Cells, SDS of cas: 55981-09-4, the main research area is monocyte derived dendritic cell Axitinib Nitazoxanide beta catenin inhibitor; ICG-001; axitinib; beta-catenin; monocyte-derived dendritic cell; nitazoxanide.

Modulation of β-catenin signaling has attractive therapeutic potential in cancer immunotherapy. Several studies have found that β-catenin can mediate immune evasion in cancer and promote anti-inflammatory features of antigen-presenting dendritic cells. Many small mol. compounds that inhibit Wnt/β-catenin signaling are currently in clin. development, but none have entered routine clin. use. New inhibitors of β-catenin signaling are consequently desirable. Here, we have tested, in monocyte-derived dendritic cells, the effects of two small mol. compounds, axitinib and nitazoxanide, that previously have been discovered to inhibit β-catenin signaling in colon cancer cells. Immature and lipopolysaccharide-matured dendritic cells prepared from healthy blood donor buffy coats were stimulated with 6-bromoindirubin-3â€?oxime (6-BIO) to boost basal β-catenin activity, and the effects of axitinib and nitazoxanide were compared with the com. β-catenin inhibitor ICG-001. Assays, including genome-wide RNA-sequencing, indicated that neither axitinib nor nitazoxanide demonstrated considerable β-catenin inhibition. Both compounds were found to be less toxic to monocyte-derived dendritic cells than either 6-BIO or ICG-001. Axitinib stimulated several aspects of dendritic cell function, such as IL12-p70 secretion, and counteracted IL-10 secretion, according to the present study. However, neither axitinib nor nitazoxanide were found to be efficient β-catenin inhibitors in monocyte-derived dendritic cells.

Biomedicines published new progress about Cellular processes. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, SDS of cas: 55981-09-4.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Hossen, Shafiul Md. published the artcileA Review on Current Repurposing Drugs for the Treatment of COVID-19: Reality and Challenges, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is review drug Repurposing safety COVID 19; COVID-19; Chloroquine; Clinical trial; Convalescent plasma; Hydroxychloroquine; Remdesivir.

Abstract: The coronavirus disease 2019 (COVID-19) caused by the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become a global pandemic with a high growth rate of confirmed cases. Therefore, therapeutic options are desperately urgent to fight with this damning virus. As it may take years to develop a specific therapy of COVID-19, it is urgent to emphasize the repurposing of drugs used for other conditions. This study reviewed the most common drugs for COVID-19 based on available online literature representing the latest in vitro clin. trial database, rational of use, adverse effects, potential toxicities, and US National Institute of Health (NIH) recommendation to use for COVID-19. Based on the preliminary data from clin. trials and considering the NIH and FDA recommendation, remdesivir and convalescent blood products are the most promising potential for COVID-19 treatment. The use of chloroquine, hydroxychloroquine, favipiravir, ivermectin, and colchicine might also be effective. However, furthermore, in vivo investigations are needed in detail individually and in combination for possible benefits in humans. Besides, tocilizumab might be deemed as adjunctive therapy for patients with cytokine release syndrome. However, lopinavir-ritonavir, anakinra, and sarilumab had not proven their clin. efficacy. Eventually, sarilumab has been withdrawn from sponsored clin. trials based on the preliminary data. Baricitinib and ruxolitinib have the additive immunosuppressive effect. Consequently, all of these drugs are being evaluated with further studies. In addition, drug-drug interaction and safety concerns must be taken into account before the administration of the recommended drugs.

SN Comprehensive Clinical Medicine published new progress about Convalescent plasma. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Luganini, Anna published the artcileThe isoquinoline alkaloid berberine inhibits human cytomegalovirus replication by interfering with the viral Immediate Early-2 (IE2) protein transactivating activity., Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is HCMV virus replication IE2 isoquinoline alkaloid berberine; Berberine chloride; Human cytomegalovirus; IE2; IE3; Murine cytomegalovirus; Promoter transactivation.

The identification and validation of new small mols. able to inhibit the replication of HCMV remains a priority to develop alternatives to the currently used DNA polymerase inhibitors, which are often burdened by long-term toxicity and emergence of cross-resistance. Low micromolar concentrations of BBR were confirmed to suppress the replication of different HCMV strains, including clin. isolates and strains resistant to approved DNA polymerase inhibitors. Anal. of the HCMV replication cycle in infected cells treated with BBR then revealed that the bioactive compound compromised the progression of virus cycle at a stage prior to viral DNA replication and Early (E) genes expression, but after Immediate-Early (IE) proteins expression. Mechanistic studies in fact highlighted that BBR interferes with the transactivating functions of the viral IE2 protein, thus impairing efficient E gene expression and the progression of HCMV replication cycle. Finally, the mechanism of the antiviral activity of BBR appears to be conserved among different CMVs, since BBR suppressed MCMV replication and inhibited the transactivation of the prototypic MCMV E1 gene by the IE3 protein, the murine homolog of IE2. Together, these observations warrant for further experimentation to obtain proof of concept that BBR could represent an attractive candidate for alternative anti-HCMV therapeutic strategies.

Antiviral Research published new progress about Alkaloids Role: THU (Therapeutic Use), BIOL (Biological Study), USES (Uses). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Maryam, Samina published the artcileStudy to determine the clinical effectiveness of nitazoxanide in treatment of giardiasis among children, SDS of cas: 55981-09-4, the main research area is Giardia giardiasis diarrhea nitazoxanide.

Giardia lambia intestinal infection is a common cause of diarrhea not only in Pakistan but around the world. It is believed to be a significant cause of morbidity and mortality in the pediatric age group. Aim: The aim of the study was to test the effectiveness of Nitazoxanide treatment in children with diarrhea caused by G. lambia. Methods: A total of 50 children with diarrhea caused by G. intestinalis received a 3-day nitazoxanide therapy (10 mg / kg / day in 2 doses for 3 days). Patients were monitored for clin. response 7 days after initiation of treatment, and then a stool sample was collected for parasitol. and lamblia antigen testing. Results: Diarrhea resolved in all 50 (100%) children treated with nitazoxanide prior to the 7-day follow-up visit. Most diarrhea resolved within 4 days. The Giardia antigen turned neg. in 96.0% of the population after 3 days of treatment. Whereas the giardia and / or oocytes / cysts became neg. in 86.0% of the patient population. Conclusions: The 3-day cycle of nitazoxanide suspension is as effective as the treatment of lamblia in children. It is well tolerated and has no significant side effects.

Indo American Journal of Pharmaceutical Sciences published new progress about Antigens Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, SDS of cas: 55981-09-4.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Lubinsky, Anthony Steven published the artcileInhaled pulmonary vasodilators are not associated with improved gas exchange in mechanically ventilated patients with COVID-19: A retrospective cohort study, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is inhaled pulmonary vasodilator mech ventilation COVID19 population; ARDS; COVID-19; Epoprostenol; Inhaled nitric oxide; Respiratory failure; Ventilatory ratio.

Measure the effect of inhaled pulmonary vasodilators on gas exchange in mech. ventilated patients with COVID-19. A retrospective observational cohort study at three New York University Hospitals was performed including eighty-four mech. ventilated SARS Cov-2 nasopharyngeal PCR pos. patients, sixty nine treated with inhaled nitric oxide (iNO) and fifteen with inhaled epoprostenol (iEPO). The primary outcomes were change in PAO2:FIO2 ratio, oxygenation Index (OI), and ventilatory ratio (VR) after initiation of inhaled pulmonary vasodilators. There was no significant change in PAO2:FIO2ratio after initiation of iNO (mean – 4.1, 95% CI -17.3-9.0, P = 0.54) or iEPO (mean – 3.4, 95% CI -19.7-12.9, P = 0.66), in OI after initiation of iNO (mean 2.1, 95% CI-0.04-4.2, P = 0.054) or iEPO (mean – 3.4, 95% CI -19.7-12.9, P = 0.75), or in VR after initiation of iNO (mean 0.17, 95% CI -0.03-0.36, P = 0.25) or iEPO (mean 0.33, 95% CI -0.0847-0.74, P = 0.11). PAO2:FIO2, OI and VR did not significantly change over a five day period starting the day prior to drug initiation in patients who received either iNO or iEPO assessed with a fixed effects model. Inhaled pulmonary vasodilators were not associated with significant improvement in gas exchange in mech. ventilated patients with COVID-19.

Journal of Critical Care published new progress about Albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Braima, Kamil published the artcileZoonotic infection by Cryptosporidium fayeri IVgA10G1T1R1 in a Western Australian human, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is nitazoxanide gp60 18S rRNA Crytosporidium zoonotic infection; Cryptosporidium ; C. fayeri IVgA10G1T1R1; Western Australia; gp60 locus; next generation sequencing; zoonoses.

In the present study, a 37-yr-old immunosuppressed female in Western Australia (WA) was identified as pos. for Cryptosporidium by microscopy and treated with nitazoxanide. Mol. analyses at the 18S rRNA (18S) and 60 kDa glycoprotein (gp60) loci identified C. fayeri subtype IVgA10G1T1R1, which had previously been identified in western gray kangaroos (Macropus fuliginosus) in WA. Next generation sequencing (NGS) of the gp60 locus confirmed the absence of mixed infections with other Cryptosporidium species. This is only the second report of C. fayeri in a human host highlighting the zoonotic potential of this wildlife-associated species. Routine diagnosis using mol. methods in laboratories is required to better understand the diversity and epidemiol. of Cryptosporidium parasite.

Zoonoses and Public Health published new progress about 18S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Parmar, Hamendra Singh published the artcileCross Talk between COVID-19 and Breast Cancer, COA of Formula: C12H9N3O5S, the main research area is review COVID19 prognosis breast cancer; ACE-2 receptors; Cytokine storm; DPP-IV.; TMPRSS2; breast cancer; diabetes.

Cancer patients are more susceptible to COVID-19; however, the prevalence of COVID-19 in different types of cancer is still inconsistent and inconclusive. Here, we delineate the intricate relationship between breast cancer and COVID-19. Breast cancer and COVID-19 share the involvement of common comorbidities, hormonal signalling pathways, gender differences, rennin- angiotensin system (RAS), angiotensin-converting enzyme-2 (ACE-2), transmembrane protease serine 2 (TMPRSS2) and dipeptidyl peptidase-IV (DPP-IV). We also shed light on the possible effects of therapeutic modalities of COVID-19 on breast cancer outcomes. Briefly, we conclude that breast cancer patients are more susceptible to COVID-19 in comparison with their normal counterparts. Women are more resistant to the occurrence and severity of COVID-19. Increased expressions of ACE2 and TMPRSS2 are correlated with occurrence and severity of COVID-19, but higher expression of ACE2 and lower expression of TMPRSS2 are prognostic markers for overall disease free survival in breast cancer. The ACE2 inhibitors and ibuprofen therapies for COVID-19 treatment may aggravate the clin. condition of breast cancer patients through chemo-resistance and metastasis. Most of the available therapeutic modalities for COVID-19 were also found to exert pos. effects on breast cancer outcomes. Besides drugs in clin. trend, TMPRSS2 inhibitors, estrogen supplementation, androgen deprivation and DPP-IV inhibitors may also be used to treat breast cancer patients infected with SARS-CoV-2. However, drug-drug interactions suggest that some of the drugs used for the treatment of COVID-19 may modulate the drug metabolism of anticancer therapies which may lead to adverse drug reaction events.

Current Cancer Drug Targets published new progress about Androgens Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, COA of Formula: C12H9N3O5S.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics