Category: 539-74-2

The author of 《Repositioning Salirasib as a new antimalarial agent》 were Porta, Exequiel O. J.; Bofill Verdaguer, Ignasi; Perez, Consuelo; Banchio, Claudia; Ferreira de Azevedo, Mauro; Katzin, Alejandro M.; Labadie, Guillermo R.. And the article was published in MedChemComm in 2019. Related Products of 539-74-2 The author mentioned the following in the article:

Malaria is a serious tropical disease that kills thousands of people every year, mainly in Africa, due to Plasmodium falciparum infections. Salirasib is a promising cancer drug candidate that interferes with the post-translational modification of Ras. This S-farnesyl thiosalicylate inhibits isoprenylcysteine carboxyl methyltransferase (ICMT), a validated target for cancer drug development. There is a high homol. between the human and the parasite enzyme isoforms, in addition to being a druggable target. Looking to repurpose its structure as an antimalarial drug, a collection of S-substituted derivatives of thiosalicylic acid were prepared by introducing 1,2,3-triazole as a diversity entry point or by direct alkylation of the thiol. We further investigated the in vitro toxicity of FTS analogs to Plasmodium falciparum in the asexual stages and in Vero cells. An antiplasmodial activity assay was performed using a simple, high-sensitivity methodol. based on nanoluciferase (NLuc)-transfected P. falciparum parasites. The results showed that some of the analogs were active at low micromolar concentration, including Salirasib. The most potent member of the series has S-farnesyl and the 1,2,3-triazole moiety substituted with phytyl. However, the compound substituted with methyl-naphthyl shows promising physicochem. and activity values. The low cytotoxicity in eukaryotic cells of the most active analogs provided good therapeutic indexes, being starting-point candidates for future antimalarial drug development. In the experimental materials used by the author, we found Ethyl 3-bromopropanoate(cas: 539-74-2Related Products of 539-74-2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Related Products of 539-74-2 Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The author of 《Tailored Polymers with Complement Activation Ability To Improve Antitumor Immunity》 were Li, Chenxi; Lu, Yue; Chen, Qing; Hu, Haiyang; Zhao, Xiuli; Qiao, Mingxi; Chen, Dawei. And the article was published in Molecular Pharmaceutics in 2019. Safety of Ethyl 3-bromopropanoate The author mentioned the following in the article:

The complement system plays an important role in host innate immunity, and its activation can be exploited as a potential strategy for vaccine adjuvants. Herein, a pH-responsive micellar vaccine platform (COOH-NPs) was developed using a carboxyl-modified diblock copolymer of poly(2-ethyl-2-oxazoline)-poly(D,L-lactide) (COOH-PEOz-PLA). The copolymer self-assembled into micelles with hydroxyl groups shielding on the surface, which activated the complement system for the enhanced immune responses. Compared with the control nanoparticles (OCH3-NPs), COOH-NPs significantly enhanced lymph node-resident dendritic cell maturation, antigen-specific IgG production, antigen-specific CD4+ and CD8+ T-cell activation, and the amount of memory T-cell generation in vivo. Furthermore, immunization with COOH-NPs/OVA in E.G7-OVA tumor-bearing mice not only remarkably inhibited tumor growth but also prolonged the survival of tumor-bearing mice. These results indicated that COOH-NPs with the capability of complement activation efficiently boosted the immune responses for the antitumor effect. The study demonstrated the significance of taking advantage of a complement-activating vaccine platform for cancer immunotherapy.Ethyl 3-bromopropanoate(cas: 539-74-2Safety of Ethyl 3-bromopropanoate) was used in this study.

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Safety of Ethyl 3-bromopropanoateSome of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Improved HDAC inhibition, stronger cytotoxic effect and higher selectivity against leukemias and lymphomas of novel, tricyclic vorinostat analogues》 was written by Bieszczad, Bartosz; Garbicz, Damian; Switalska, Marta; Dudek, Marta K.; Warszycki, Dawid; Wietrzyk, Joanna; Grzesiuk, Elzbieta; Mieczkowski, Adam. COA of Formula: C5H9BrO2This research focused ontricyclic vorinostat analog lymphoma leukemia HDAC inhibition cytotoxic effect; HDAC inhibitors; Vorinostat; dibenzodiazocines; histone deacetylase; hydroxamic acid; selectivity. The article conveys some information:

Histone deacetylase (HDAC) inhibitors are a class of drugs used in the cancer treatment. Here, we developed a library of 19 analogs of Vorinostat, an HDAC inhibitor used in lymphomas treatment. In Vorinostat, we replaced the hydrophobic Ph group with various tricyclic ′caps′ possessing a central, eight-membered, heterocyclic ring, and investigated the HDAC activity and cytotoxic effect on the cancer and normal cell lines. We found that 3 out of the 19 compounds, based on dibenzo[b,f]azocin-6(5H)-one, 11,12-dihydrodibenzo[b,f]azocin-6(5H)-one, and benzo[b]naphtho[2,3-f][1,5]diazocine-6,14(5H,13H)-dione scaffolds, showed better HDACs inhibition than the referenced Vorinostat. In leukemic cell line MV4-11 and in the lymphoma cell line Daudi, three compounds showed lower IC50 values than Vorinostat. These compounds had higher activity and selectivity against MV4-11 and Daudi cell lines than reference Vorinostat. We also observed a strong correlation between HDACs inhibition and the cytotoxic effect. Cell lines derived from solid tumors: A549 (lung carcinoma) and MCF-7 (breast adenocarcinoma) as well as reference BALB/3T3 (normal murine fibroblasts) were less susceptible to compounds tested. Developed derivatives show improved properties than Vorinostat, thus they could be considered as possible agents for leukemia and lymphoma treatment. The experimental part of the paper was very detailed, including the reaction process of Ethyl 3-bromopropanoate(cas: 539-74-2COA of Formula: C5H9BrO2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. COA of Formula: C5H9BrO2 In contrast, terrestrial plants account only for a few bromine-containing compounds.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2022,Liu, Genyan; Zhou, Congwei; Zhang, Zhisong; Wang, Chenchen; Luo, Xiaogang; Ju, Xiulian; Zhao, Chunqing; Ozoe, Yoshihisa published an article in Pest Management Science. The title of the article was 《Novel insecticidal 1,6-dihydro-6-iminopyridazine derivatives as competitive antagonists of insect RDL GABA receptors》.SDS of cas: 539-74-2 The author mentioned the following in the article:

BACKGROUND : The ionotropic γ-aminobutyric acid (GABA) receptor (iGABAR) is an important target for insecticides and parasiticides. Our previous studies showed that competitive antagonists (CAs) of insect iGABARs have the potential to be used for developing novel insecticides and that the structural modification of gabazine (a representative CA of mammalian iGABARs) could lead to the identification of novel CAs of insect iGABARs. RESULTS : In the present study, a novel series of 1,3-di- and 1,3,5-trisubstituted 1,6-dihydro-6-iminopyridazines (DIPs) was designed using a versatile strategy and synthesized using facile methods. Electrophysiol. studies showed that several target DIPs (30μM) exhibited excellent antagonistic activities against common cutworm and housefly iGABARs consisting of RDL subunits. The IC50 values of 3-(4-methoxyphenyl), 3-(4-trifluoromethoxyphenyl), 3-(4-biphenylylphenyl), 3-(2-naphthyl), 3-(3,4-methylenedioxyphenyl), and 3,5-(4-methoxyphenyl) analogs ranged from 2.2 to 24.8μM. Addnl., several 1,3-disubstituted DIPs, especially 3-(4-trifluoromethoxyphenyl) and 3-(3,4-methylenedioxyphenyl) analogs, exhibited moderate insecticidal activity against common cutworm larvae, with >60% mortality at a concentration of 100 mg kg-1. Mol. docking studies showed that the oxygen atom on the three-substituted aromatic ring could form a hydrogen bond with Arg254, which may enhance the activity of these DIPs against housefly iGABARs. CONCLUSION : This systematic study indicated that the presence of a carboxyl side chain shorter by one methylene than that of gabazine at the 1-position of the pyridazine ring is effective for maintaining the stable binding of these DIPs in insect iGABARs. Our study provides important information for the design of novel insect iGABAR CAs. 2022 Society of Chem. Industry. In the part of experimental materials, we found many familiar compounds, such as Ethyl 3-bromopropanoate(cas: 539-74-2SDS of cas: 539-74-2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. In contrast, terrestrial plants account only for a few bromine-containing compounds.SDS of cas: 539-74-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Category: bromides-buliding-blocksIn 2019 ,《Discovery of Novel Dual Histone Deacetylase and Mammalian Target of Rapamycin Target Inhibitors as a Promising Strategy for Cancer Therapy》 appeared in Journal of Medicinal Chemistry. The author of the article were Chen, Yong; Yuan, Xue; Zhang, Wanhua; Tang, Minghai; Zheng, Li; Wang, Fang; Yan, Wei; Yang, Shengyong; Wei, Yuquan; He, Jun; Chen, Lijuan. The article conveys some information:

In the present study, a series of novel dual-target histone deacetylase (HDAC) and mammalian target of rapamycin (mTOR) inhibitors were designed and synthesized using pyrimidine-pyrazolyl pharmacophore to append HDAC recognition cap and hydroxamic acid as a zinc-binding motif. Among them, I was the optimal lead compound with potent inhibition activities against mTOR and HDAC1 with half-maximal inhibitory concentration of 1.2 and 0.19 nM, resp. Western blot confirmed that I could upregulate acetylation of H3 and α-tubulin and downregulate mTOR-related downstream mediators. I could also stimulate cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis. I showed comparable antitumor activity with the combination medication in MM1S xenograft model with a tumor growth inhibitory rate of 72.5%, without causing significant loss of body weight and toxicity. All of the results indicated that I could be a promising dual target inhibitor for treating hematol. malignancies. The experimental process involved the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Category: bromides-buliding-blocks)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. In contrast, terrestrial plants account only for a few bromine-containing compounds.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Cheng, Meng; Yu, Xufen; Lu, Kaylene; Xie, Ling; Wang, Li; Meng, Fanye; Han, Xiaoran; Chen, Xian; Liu, Jing; Xiong, Yue; Jin, Jian. Recommanded Product: Ethyl 3-bromopropanoate The article mentions the following:

Several epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors have been developed and approved by Food and Drug Administration for the treatment of non-small-cell lung cancers, but their efficacy can be compromised by acquired drug resistance conferred by EGFR-mutant variants. Here, we described the discovery of a novel E3 ligase von Hippel-Lindau-recruiting EGFR degrader, MS39 (compound 6), and a first-in-class E3 ligase cereblon-recruiting EGFR degrader, MS154 (compound 10), using the proteolysis targeting chimera technol. These compounds potently induced the degradation of mutant but not wild-type EGFR in an E3 ligase-dependent manner in cancer cell lines and effectively suppressed the growth of lung cancer cells compared with the corresponding neg. controls. The global proteomic analyses revealed that the compounds were highly selective for EGFR. Furthermore, both compounds were bioavailable in mouse pharmacokinetic studies, and compound 6 is the first EGFR degrader suitable for in vivo efficacy studies. Overall, we provide a set of well-characterized chem. tools to the research community. The experimental part of the paper was very detailed, including the reaction process of Ethyl 3-bromopropanoate(cas: 539-74-2Recommanded Product: Ethyl 3-bromopropanoate)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Recommanded Product: Ethyl 3-bromopropanoateSome of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Thiocyanation and 2-Amino-1,3-thiazole Formation in Water Using Recoverable and Reusable Glycosylated Resorcin[4]arene Cavitands》 was published in Journal of Organic Chemistry in 2020. These research results belong to Husain, Ali A.; Bisht, Kirpal S.. Safety of Ethyl 3-bromopropanoate The article mentions the following:

A family of three spatially directional resorcin[4]arene cavitand glycoconjugates (RCGs) have been applied as efficient recoverable and reusable inverse phase transfer catalysts for eco- and environmentally friendly thiocyanation and 2-amino-1,3-thiazole formation reactions in water. The results show that RCGs (1 mol %) were capable of hosting and catalyzing various water-insoluble bromo/thiocyanato substrates in water without the use of any co-organic solvents. The recoverability and reusability of RCG catalytic systems, i.e., RCG1 and RCG3, were also examined upon a simple extraction of the desired products using DCM or Et acetate, followed by subjecting the recovered aqueous solution containing the RCG catalysts to the next reaction cycles. The experimental process involved the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Safety of Ethyl 3-bromopropanoate)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals.Safety of Ethyl 3-bromopropanoate Organobromine compounds have fallen under increased scrutiny for their environmental impact.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Geniller, Lilian; Taillefer, Marc; Jaroschik, Florian; Prieto, Alexis published an article in 2022. The article was titled 《Photo-Induced Halogen-Atom Transfer: Generation of Halide Radicals for Selective Hydrohalogenation Reactions》, and you may find the article in Chemistry – A European Journal.Formula: C5H9BrO2 The information in the text is summarized as follows:

The first photo-mediated process enabling the generation of halide radicals by Halogen-Atom Transfer (XAT) is described. Contrary to radical transformations involving XAT reactivity, which exploit stable carbon radicals, this unique approach uses 1,2-dihaloethanes for the generation of unstable carbon radicals by XAT. These transient radicals then underwent β-scission with release of ethylene and formation of more stable halide radicals which have been used in selective hydrohalogenations of a large number of unsaturated hydrocarbons, including Michael acceptors, unactivated alkenes and alkynes. This hydrohalogenation is tolerant of a broad range of functionalities and is believed to proceed through a radical-chain manifold that propagates by the use of silane derivatives In addition to this study using Ethyl 3-bromopropanoate, there are many other studies that have used Ethyl 3-bromopropanoate(cas: 539-74-2Formula: C5H9BrO2) was used in this study.

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Formula: C5H9BrO2 In contrast, terrestrial plants account only for a few bromine-containing compounds.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The author of 《Enzymatic assembly of carbon-carbon bonds via iron-catalysed sp3 C-H functionalization》 were Zhang, Ruijie K.; Chen, Kai; Huang, Xiongyi; Wohlschlager, Lena; Renata, Hans; Arnold, Frances H.. And the article was published in Nature (London, United Kingdom) in 2019. HPLC of Formula: 539-74-2 The author mentioned the following in the article:

Although abundant in organic mols., carbon-hydrogen (C-H) bonds are typically considered unreactive and unavailable for chem. manipulation. Recent advances in C-H functionalization technol. have begun to transform this logic, while emphasizing the importance of and challenges associated with selective alkylation at a sp3 carbon. Here we describe iron-based catalysts for the enantio-, regio- and chemoselective intermol. alkylation of sp3 C-H bonds through carbene C-H insertion. The catalysts, derived from a cytochrome P 450 enzyme in which the native cysteine axial ligand has been substituted for serine (cytochrome P411), are fully genetically encoded and produced in bacteria, where they can be tuned by directed evolution for activity and selectivity. That these proteins activate iron, the most abundant transition metal, to perform this chem. provides a desirable alternative to noble-metal catalysts, which have dominated the field of C-H functionalization. The laboratory-evolved enzymes functionalize diverse substrates containing benzylic, allylic or α-amino C-H bonds with high turnover and excellent selectivity. Furthermore, they have enabled the development of concise routes to several natural products. The use of the native iron-haem cofactor of these enzymes to mediate sp3 C-H alkylation suggests that diverse haem proteins could serve as potential catalysts for this abiol. transformation, and will facilitate the development of new enzymic C-H functionalization reactions for applications in chem. and synthetic biol. The experimental process involved the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2HPLC of Formula: 539-74-2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. HPLC of Formula: 539-74-2 Moreover, several studies demonstrate that the average proportion of bromine in drugs is significantly higher than that in natural products.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Efficient Oral Delivery of Poorly Water-Soluble Drugs Using Carnitine/Organic Cation Transporter 2-Mediated Polymeric Micelles》 was published in ACS Biomaterials Science & Engineering in 2020. These research results belong to He, Chuyu; Jin, Yao; Deng, Yunqiang; Zou, Yang; Han, Shidi; Zhou, Chuhang; Zhou, Yuanhang; Liu, Yan. HPLC of Formula: 539-74-2 The article mentions the following:

The intestine epithelium is considered to be the most critical obstacle for nanoparticles for oral delivery of water-insoluble and poorly absorbed drugs. Based on the specific transporters located on the apical membrane of the intestinal epithelium, the carnitine-conjugated polymeric micelles targeting to the carnitine/organic cation transporter 2 (OCTN2) were developed by combining carnitine-conjugated poly(2-ethyl-2-oxazoline)-poly(D,L-lactide) with monomethoxy poly(ethylene-glycol)-poly(D,L-lactide). The carnitine-conjugated micelles with favorable stability in gastrointestinal fluid were validated to remarkably increase the cellular internalization and transcellular transport, while these were not the cases in the presence of free carnitine. These were further confirmed by more distribution of the micelles within epithelial cells, on the apical and basolateral side of the epithelium in mice. Addnl., identification of the carnitine-conjugated micelles by OCTN2 was detected to facilitate cellular uptake of the micelles via fluorescence immunoassay. Both clathrin and caveolae/lipid rafts pathways mediated endocytosis and transcellular transport of the carnitine-conjugated micelles, implying the enrichment of endocytic and transcellular transport pathway compared with that of carnitine-unconjugated micelles. Further, the intracellular trafficking process of the carnitine-conjugated micelles was tracked under confocal laser scanning microscopy, which involved in intracellular compartments such as late endosomes, lysosomes, endoplasmic reticulum, and Golgi apparatus as well. In conclusion, the current study provided an efficient strategy to facilitate the oral absorption of water-insoluble and poorly absorbed agents using intestinal transporter-mediated polymeric micelles. After reading the article, we found that the author used Ethyl 3-bromopropanoate(cas: 539-74-2HPLC of Formula: 539-74-2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides. HPLC of Formula: 539-74-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary