Category: 3395-91-3

Recommanded Product: Methyl 3-bromopropanoate. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about A nano-cocktail of an NIR-II emissive fluorophore and organoplatinum(II) metallacycle for efficient cancer imaging and therapy. Author is Ding, Feng; Chen, Zhao; Kim, Won Young; Sharma, Amit; Li, Chonglu; Ouyang, Qingying; Zhu, Hua; Yang, Guangfu; Sun, Yao; Kim, Jong Seung.

The scarcity of efficient imaging technologies for precise cancer treatment greatly drives the development of new nanotheranostic based platforms that enable both diagnostic and therapeutic functions, together in a single formulation. Owing to the complicated physiol. microenvironment, nanosystems designed with the possibility of noninvasive real-time monitoring of therapeutic progression in the second near-IR channel (NIR-II, 1000-1700 nm) could substantially improve the current cancer therapies. Herein, we design a novel NIR-II theranostic nanoprobe, PSY (size ∼110 nm), by incorporating organoplatinum(II) metallacycles P1 and an organic NIR-II mol. dye, SY1030, into the FDA-approved polymer Pluronic F127. Preliminary in vitro and in vivo studies suggest that PSY is capable of being internalized into glioma U87MG-cells with no significant internalization in non-cancerous tissues. In addition, it shows excellent photostability and minimal background for real-time monitoring the process of therapy in the NIR-II region. Furthermore, in U87MG xenografts and orthotopic breast tumor, PSY demonstrat significantly improved anticancer efficacy compared to a clin. approved Pt(II)-based anticancer drug, cisplatin. The engineered nano-cocktail PSY offers a simple strategy for delivering the organoplatinum(II) macrocycle P1 and NIR-II fluorophore SY1030 as a cocktail of diagnostic and therapeutic functions and highlights its promising capacity for future cancer treatment.

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Quality Control of Methyl 3-bromopropanoate. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about Catalytic Asymmetric Homologation of Ketones with α-Alkyl α-Diazo Esters. Author is Tan, Fei; Pu, Maoping; He, Jun; Li, Jinzhao; Yang, Jian; Dong, Shunxi; Liu, Xiaohua; Wu, Yun-Dong; Feng, Xiaoming.

The homologation of ketones with diazo compounds was a useful strategy to synthesize one-carbon chain-extended acyclic such as PhC(O)CMeCO2MeR [R = allyl, Bn, CH2(2-naphthyl), etc.] or ring-expanded cyclic ketones e.g., I. However, the asym. homologation of acyclic ketones with α-diazo esters remains a challenge due to the lower reactivity and complicated selectivity. Herein, the enantioselective catalytic homologation of acetophenone and related derivatives with α-alkyl α-diazo esters was reported utilizing a chiral scandium(III) N,N’-dioxide as the Lewis acid catalyst. This reaction supplies a highly chemo-, regio-, and enantioselective pathway for the synthesis of optically active β-keto esters with an all-carbon quaternary center through highly selective alkyl-group migration of the ketones. Moreover, the ring expansion of cyclic ketones was accomplished under slightly modified conditions, affording a series of enantioenriched cyclic β-keto esters. D. functional theory calculations was carried out to elucidate the reaction pathway and possible working models that could explain the observed regio- and enantioselectivity.

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Quality Control of Methyl 3-bromopropanoate. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about Discovery of novel aminopiperidinyl amide CXCR4 modulators through virtual screening and rational drug design. Author is Oum, Yoon Hyeun; Kell, Steven A.; Yoon, Younghyoun; Liang, Zhongxing; Burger, Pieter; Shim, Hyunsuk.

The C-X-C chemokine receptor type 4 (CXCR4) is a potential therapeutic target for HIV infection, metastatic cancer, and inflammatory autoimmune diseases. In this study, we screened the ZINC chem. database for novel CXCR4 modulators through a series of in silico guided processes. After evaluating the screened compounds for their binding affinities to CXCR4 and inhibitory activities against the chemoattractant CXCL12, we identified a hit compound (ZINC 72372983) showing 100 nM affinity and 69% chemotaxis inhibition at the same concentration (100 nM). To increase the potency of our hit compound, we explored the protein-ligand interactions at an at. level using mol. dynamics simulation which enabled us to design and synthesize a novel compound (Z7R) with nanomolar affinity (IC50 = 1.25 nM) and improved chemotaxis inhibition (78.5%). Z7R displays promising anti-inflammatory activity (50%) in a mouse edema model by blocking CXCR4-expressed leukocytes, being supported by our immunohistochem. study.

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HPLC of Formula: 3395-91-3. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about Discovery of Highly Potent and Selective IRAK1 Degraders to Probe Scaffolding Functions of IRAK1 in ABC DLBCL. Author is Fu, Liqiang; Zhang, Jing; Shen, Bin; Kong, Linglong; Liu, Yingtao; Tu, Wangyang; Wang, Wenqian; Cai, Xin; Wang, Xiaotao; Cheng, Na; Xia, Mingxuan; Zhou, Tianyuan; Liu, Qian; Xu, Yanping; Yang, Jennifer; Gavine, Paul; Philippar, Ulrike; Attar, Ricardo; Edwards, James P.; Venable, Jennifer D.; Dai, Xuedong.

MyD88 gene mutation has been identified as one of the most prevalent driver mutations in the activated B-cell-like diffuse large B-cell lymphoma (ABC DLBCL). The published literature suggests that interleukin-1 receptor-associated kinase 1 (IRAK1) is an essential gene for ABC DLBCL harboring MyD88 mutation. Importantly, the scaffolding function of IRAK1, rather than its kinase activity, is required for tumor cell survival. Herein, we present our design, synthesis, and biol. evaluation of a novel series of potent and selective IRAK1 degraders. One of the most potent compounds, Degrader-3 (JNJ-1013) (I), effectively degraded cellular IRAK1 protein with a DC50 of 3 nM in HBL-1 cells. Furthermore, JNJ-1013 potently inhibited IRAK1 downstream signaling pathways and demonstrated strong anti-proliferative effects in ABC DLBCL cells with MyD88 mutation. This work suggests that IRAK1 degraders have the potential for treating cancers that are dependent on the IRAK1 scaffolding function.

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Benzothiophene – Wikipedia,
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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 3395-91-3, is researched, Molecular C4H7BrO2, about Asymmetric α-alkylation of cyclic β-keto esters and β-keto amides by phase-transfer catalysis, the main research direction is indanone preparation enantioselective; keto ester alkyl bromide alkylation cinchona phase transfer catalyst; amide keto alkyl bromide alkylation cinchona phase transfer catalyst; tetralone preparation enantioselective.Synthetic Route of C4H7BrO2.

Without employing any transition metal, a highly enantioselective α-alkylation of cyclic β-keto esters and β-keto amides has been realized by phase-transfer catalysis. This improved procedure is applicable to different kinds of bromides with cinchona derivatives and gives the corresponding products e.g., I and e.g., II, in excellent enantiopurities (up to 98% ee) and good yields (up to 98%). Moreover, the reaction was scalable and the phase-transfer catalyst was recyclable. This provided an alternative and competitive method to the asym. α-alkylation of β-dicarbonyl compounds

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 3395-91-3, is researched, Molecular C4H7BrO2, about Design, synthesis and biological evaluation of pyridyl substituted benzoxazepinones as potent and selective inhibitors of aldosterone synthase, the main research direction is pyridyl benzoxazepinone preparation aldosterone synthase inhibitor mol docking.Name: Methyl 3-bromopropanoate.

Exorbitant aldosterone is closely associated with various severe diseases, including congestive heart failure and chronic kidney disease. As aldosterone synthase is the pivotal enzyme in aldosterone biosynthesis, its inhibition constitutes a promising treatment for these diseases. Via a structure-based approach, a series of pyridyl substituted 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-ones I (R = dimethylaminyl, F, pyrrolidin-1-yl, etc.; R1 = 4-methylpyridin-3-yl, 5-(trifluoromethyl)pyridin-3-yl, 5-fluoropyridin-3-yl, etc.) were designed as inhibitors of aldosterone synthase. Six compounds I (R = dimethylaminyl, R1 = 5-methylpyridin-3-yl; R1 = R = dimethylaminyl, 4-methylpyridin-3-yl; R = dimethylaminyl, R1 = 5-methoxypyridin-3-yl; R1 = 4-methylpyridin-3-yl, R = morpholin-4-yl; R1 = 4-methylpyridin-3-yl, R = piperazin-1-yl (II); R1 = 4-methylpyridin-3-yl, R = 4-methylpiperazin-1-yl) distinguished themselves with potent inhibition (IC50 <100 nmol/L) and high selectivity over homogenous 11β-hydroxylase. As the most promising compound, (II) exhibited an IC50 of 12 nmol/L and an excellent selectivity factor (SF) of 157, which are both superior to those of the reference fadrazole (IC50 = 21 nmol/L, SF = 7). Importantly, (II) showed no inhibition against steroidogenic CYP17, CYP19 and a panel of hepatic CYP enzymes indicating an outstanding safety profile. As it manifested satisfactory pharmacokinetic properties in rats, compound (II) was considered as a drug candidate for further development. If you want to learn more about this compound(Methyl 3-bromopropanoate)Name: Methyl 3-bromopropanoate, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(3395-91-3).

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Methyl 3-bromopropanoate( cas:3395-91-3 ) is researched.SDS of cas: 3395-91-3.Kumar, Kunal; Wang, Peng; Wilson, Jessica; Zlatanic, Viktor; Berrouet, Cecilia; Khamrui, Susmita; Secor, Cody; Swartz, Ethan A.; Lazarus, Michael; Sanchez, Roberto; Stewart, Andrew F.; Garcia-Ocana, Adolfo; DeVita, Robert J. published the article 《Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor》 about this compound( cas:3395-91-3 ) in Journal of Medicinal Chemistry. Keywords: harmine derivative preparation DYRK1A inhibitory activity diabetes SAR. Let’s learn more about this compound (cas:3395-91-3).

Recently, our group identified that harmine is able to induce β-cell proliferation both in vitro and in vivo, mediated via the DYRK1A-NFAT pathway. Since, harmine suffers from a lack of selectivity, both against other kinases and CNS off-targets, we therefore sought to expand structure-activity relationships for harmine’s DYRK1A activity, to enhance selectivity for off-targets while retaining human β-cell proliferation activity. We carried out optimization of the 9-N-position of harmine to synthesize 29 harmine-based analogs. Several novel inhibitors showed excellent DYRK1A inhibition and human β-cell proliferation capability. An optimized DYRK1A inhibitor, compound I, was identified as a novel, efficacious in vivo lead candidate. Compound I also demonstrates improved selectivity for kinases and CNS off-targets, as well as in vivo efficacy for β-cell proliferation and regeneration at lower doses than harmine. Collectively, these findings demonstrate that compound I is a much improved in vivo lead candidate as compared to harmine for the treatment of diabetes.

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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about In vitro evaluation of antiproliferative properties of novel organotin(IV) carboxylate compounds with propanoic acid derivatives on a panel of human cancer cell lines.Computed Properties of C4H7BrO2.

The synthesis of novel triphenyltin(IV) compounds, Ph3SnLn (n = 1-3), with oxaprozin (3-(4,5-diphenyloxazol-2-yl)propanoic acid), HL1, and the new propanoic acid derivatives 3-(4,5-bis(4-methoxylphenyl)oxazol-2-yl)propanoic acid, HL2, and 3-(2,5-dioxo-4,4-diphenylimidazolidin-1-yl)propanoic acid, HL3, has been performed. The ligands represent com. drugs or their derivatives and the tin complexes have been characterized by standard anal. methods. The in vitro antiproliferative activity of both ligands and organotin(IV) compounds has been evaluated on the following tumor cell lines: human prostate cancer (PC-3), human colorectal adenocarcinoma (HT-29), breast cancer (MCF-7), and hepatocellular cancer (HepG2), as well as on normal mouse embryonic fibroblast cells (NIH3T3) with the aid of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-12 diphenyltetrazolium bromide) and CV (crystal violet) assays. Contrary to the inactive ligand precursors, all organotin(IV) carboxylates showed very good activity with IC50 values ranging from 0.100 to 0.758 μM. According to the CV assay (IC50 = 0.218 ± 0.025 μM), complex Ph3SnL1 demonstrated the highest cytotoxicity against the caspase 3 deficient MCF-7 cell line. Inductively coupled plasma mass spectrometry (ICP-MS) anal. indicated a two-fold lower concentration of tin in MCF-7 cells in comparison to platinum. To investigate the mechanism of action of the compound Ph3SnL1 on MCF-7 cells, morphol., autophagy and cell cycle anal., as well as the activation of caspase and ROS/RNS and NO production, has been performed. Results suggest that Ph3SnL1 induces caspase-independent apoptosis in MCF-7 cells.

If you want to learn more about this compound(Methyl 3-bromopropanoate)Computed Properties of C4H7BrO2, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(3395-91-3).

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 3395-91-3, is researched, SMILESS is O=C(OC)CCBr, Molecular C4H7BrO2Journal, Article, Dalton Transactions called Design, synthesis and biological evaluation of dihydro-2-quinolone platinum(IV) hybrids as antitumor agents displaying mitochondria injury and DNA damage mechanism, Author is Liu, Zhifang; Li, Zuojie; Du, Tao; Chen, Yan; Wang, Qingpeng; Li, Guoshuai; Liu, Min; Zhang, Ning; Li, Dacheng; Han, Jun, the main research direction is platinum quinoloneoxoalkylcarboxylate complex preparation antitumor DNA cleavage.Recommanded Product: 3395-91-3.

The design of novel platinum(IV) complexes with mitochondria injury competence, besides the DNA damage mechanism, is a promising way to develop new platinum drugs. Herein, dihydro-2-quinolone (DHQLO) as a mitocan was incorporated into the platinum(IV) system for the first time to prepare a new series of DHQLO platinum(IV) compounds Complex 1b could effectively inhibit the proliferation of tumor cells in vitro and in vivo. It accumulated at higher levels in both whole cells and DNA, and easily underwent intercellular reduction to release platinum(II) and DHQLO moieties. The released platinum(II) complex caused serious DNA damage by covalent conjunction with the DNA duplex, and remarkably increased the expression of the γ-H2AX protein. Moreover, 1b also caused serious mitochondria injury to induce mitochondrial membrane depolarization and increase ROS generation. Such actions upon DNA and mitochondria activate the p53 apoptotic pathway synergetically in tumor cells by upregulating the protein p53 and apoptotic proteins caspase9 and caspase3, which efficiently promoted the apoptotic death of tumor cells. Compound 1b with such synergic mechanism exhibited great potential in reversing cisplatin resistance and improving antitumor efficacies.

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Name: Methyl 3-bromopropanoate. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A4 Hydrolase.

The cytosolic metalloenzyme leukotriene A4 hydrolase (LTA4H) is the final and rate-limiting enzyme in the biosynthesis of pro-inflammatory leukotriene B4 (LTB4). Preclin. studies have validated this enzyme as an attractive drug target in chronic inflammatory diseases. Despite several attempts, no LTA4H inhibitor has reached the market, yet. Herein, we disclose the discovery and preclin. profile of LYS006 (I), a highly potent and selective LTA4H inhibitor. A focused fragment screen identified hits that could be cocrystd. with LTA4H and inspired a fragment merging. Further optimization led to chiral amino acids and ultimately to LYS006, a picomolar LTA4H inhibitor with exquisite whole blood potency and long-lasting pharmacodynamic effects. Due to its high selectivity and its ability to fully suppress LTB4 generation at low exposures in vivo, LYS006 has the potential for a best-in-class LTA4H inhibitor and is currently investigated in phase II clin. trials in inflammatory acne, hidradenitis suppurativa, ulcerative colitis, and NASH.

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