Tag: M.W=200-300

Related Products of 17696-11-6. 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: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). Author is Zhang, Hao; Zhao, Hong-Yi; Xi, Xiao-Xiao; Liu, Yan-Jie; Xin, Minhang; Mao, Shuai; Zhang, Jun-Jie; Lu, A-Xin; Zhang, San-Qi.

Herein, the discovery of small mol. EGFR degraders based on the proteolysis targeting chimera (PROTAC) strategy was reported. In the present study, 13 EGFR degraders containing pyrido[3,4-d]pyrimidine moiety I [X = CH2C(O)NHCH2CH2C(O), CH2CH2CH2CH2C(O), CH2CH2CH2CH2CH2C(O), etc.], II [C = CH2C(O)NHCH2CH2C(O), CH2CH2CH2CH2CH2CH2CH2C(O)] and III [X = CH2CH2CH2CH2C(O), CH2CH2OCH2CH2OCH2CH2, CH2CH2CH2CH2CH2CH2C(O), etc.] were designed and synthesized. Promising PROTACs I [X = CH2CH2CH2CH2CH2CH2CH2C(O)] and III [X = CH2CH2CH2CH2CH2CH2C(O)] induced degradation of EGFR in HCC827 cells with the DC50 values of 45.2 and 34.8 nM, resp. Cellular protein-controlling machinery ubiquitin proteasome system (UPS) was involved in the degradation process. Furthermore, the degraders I [X = CH2CH2CH2CH2CH2CH2CH2C(O)] and III [X = CH2CH2CH2CH2CH2CH2C(O)] could significantly induce the apoptosis of HCC827 cells and arrest the cells in G1 phase. These findings demonstrated that compounds I [X = CH2CH2CH2CH2CH2CH2CH2C(O)] and III [X = CH2CH2CH2CH2CH2CH2C(O)] could serve as effective EGFRdel19-targeting degraders in HCC827 cells. v.

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Synthetic Route of C8H15BrO2. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 8-Bromooctanoic acid, is researched, Molecular C8H15BrO2, CAS is 17696-11-6, about New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes. Author is Rangasamy, Loganathan; Ortin, Irene; Zapico, Jose Maria; Coderch, Claire; Ramos, Ana; de Pascual-Teresa, Beatriz.

Four potent CK2 inhibitors derived from CX-4945 are described. They also provided nanomolar activity against HDAC1, therefore having promising utility as dual-target agents for cancer. The linker length between the hydroxamic acid and the CX-4945 scaffold plays an important role in dictating balanced activity against the targeted enzymes. The seven-carbon linker (compound 15c) was optimal for inhibition of both CK2 and HDAC1. Remarkably, 15c showed 3.0 and 3.5 times higher inhibitory activity than the reference compounds CX-4945 (against CK2) and SAHA (against HDAC1), resp. Compound 15c exhibited micromolar activity in cell-based cytotoxic assays against multiple cell lines.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum, published in 2007-01-01, which mentions a compound: 837-52-5, Name is 7-Chloro-4-(piperazin-1-yl)quinoline, Molecular C13H14ClN3, Recommanded Product: 7-Chloro-4-(piperazin-1-yl)quinoline.

A targeted series of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives were synthesized and evaluated in vitro against the malarial cysteine protease falcipain-2 and a chloroquine resistant strain (W2) of Plasmodium falciparum. A novel series of 4-aminoquinoline semicarbazones were the most effective inhibitors of falcipain-2 (most potent inhibitor had IC50 = 0.63 μM) while a bisquinoline semicarbazone compound 8f (I) was the most potent antimalarial compound with an IC50 of 0.07 μM against W2. Compound 8f also weakly inhibited falcipain-2, with an IC50 of 3.16 μM, although its principal antiparasitic activity did not appear to be due to inhibition of this enzyme.

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Synthetic Route of C10H8N2S2. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4,4-Dipyridyl Disulfide, is researched, Molecular C10H8N2S2, CAS is 2645-22-9, about Crystal structures and magnetic properties of two Co(II) coordination polymers created via in situ ligand synthesis. Author is Zhao, Ying; Dang, Li-Long; Zhai, Zhi-Min; Ma, Lu-Fang; Wang, Li-Ya.

The authors present two new coordination polymers, [Co3(iBuOIPA)3(bps)(H2O)]n (1) and [Co2(iPrIPA)2(bps)]n (2) (bps = 4,4′-bipyridyl sulfide, iBuOIPA = 5-i-butoxyisophthalate, iPrIPA = 5-i-propoxyisophthalate), by the hydrothermal reactions of Co(OAc)2·4H2O and 4,4′-bipyridyl disulfide (bpds) with iBuOIPA or iPrIPA, resp. Both crystal structures were determined by single-crystal x-ray diffraction analyses and further characterized by elemental analyses, IR spectra and TG analyses. For 1 and 2, the starting bpds ligands were wholly transformed into bps. Polymer 1 displays a 3-dimensional network constructed from binuclear Co nodes while polymer 2 features a 2-dimensional infinite layer consisting of Co dimers. The existence of electron-donating groups in isophthalate derivatives plays a significant role during the self-assembly of polymers. Also, both 1 and 2 exhibit remarkable magnetic properties, which were studied and discussed in detail, showing a good prospect in magnetic and energy storage devices.

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Shi, Xiaolin; Li, Xiaowei; Ma, Lina; Shi, Dayong published an article about the compound: 6-Bromo-3-methyl-1H-indole( cas:1219741-50-0,SMILESS:CC1=CNC2=C1C=CC(Br)=C2 ).Application of 1219741-50-0. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:1219741-50-0) through the article.

An efficient copper-catalyzed oxidative trifluoromethylation of indoles I (R1 = H, Boc, Bn, Bz; R2 = Me, cyclohexyl, CH2C(O)CH3, CH2CN, etc.; R3 = H, 4-F, 5-MeO, 6-Cl, 7-Br, etc.) with low-cost CF3SO2Na via C-H activation has been described. Notably, the use of a base is crucial for the trifluoromethylation of indoles I. This reaction proceeds efficiently in good to excellent yields and is tolerance of a broad range of functional groups. Furthermore, melatonin, a medicine for sleep disorders, is converted to its 2-CF3 analog in 68% yield. Studies of possible reaction pathways suggest that this reaction proceeds through a radical process.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety, the main research direction is oxadiazolylmethylpiperazinyl quinoline derivative preparation antituberculosis; Antitubercular activity; Bioavailability; Cytotoxicity; Oxadiazole; Quinoline.Reference of 7-Chloro-4-(piperazin-1-yl)quinoline.

Tuberculosis is the infectious disease caused by mycobacterium tuberculosis (Mtb), responsible for the utmost number of deaths annually across the world. Herein, twenty-one new substituted 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl-quinoline derivatives were designed and synthesized through multistep synthesis followed by in vitro evaluation of their antitubercular potential against Mtb WT H37Rv. The compound I was found to be promising with MIC value of 0.5 μg/mL and QD-19 to QD-21 were also remarkable with MIC value of 0.25 μg/mL. Addnl., we have carried out experiments to confirm the metabolic stability, cytotoxicity and pharmacokinetics of these compounds along with kill kinetics of QD-18. These compounds were found to be orally bioavailable and highly effective. Altogether, these results indicate that I and II (R = 2,3-Me2Ph, cyclopentyl, and 4-iPrPh) are promising lead compounds for the development of a novel chem. class of antitubercular drugs.

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Solomon, V. Raja; Pundir, Sheetal; Lee, Hoyun published the article 《Examination of novel 4-aminoquinoline derivatives designed and synthesized by a hybrid pharmacophore approach to enhance their anticancer activities》. Keywords: structure activity aminoquinoline antitumor; bortezomib monastrol aminoquinoline derivative anticancer breast cancer progression.They researched the compound: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5 ).Category: bromides-buliding-blocks. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:837-52-5) here.

In an attempt to develop effective and potentially safe anticancer agents, thirty-six 4-aminoquinoline-derived sulfonyl analogs I (R = CH3, 4-ClC6H4, p-tolyl, etc., X = Cl, CF3) and II were designed and synthesized using a hybrid pharmacophore approach. The cytotoxicity of these compounds was determined using three breast tumor cell lines (MDA-MB231, MDA-MB468 and MCF7) and two matching non-cancer breast epithelial cell lines (184B5 and MCF10A). Although most of the compounds were quite effective on the breast cancer cells, I [R = 2,4-(O2N)2C6H3, X = Cl] (III; VR23) emerged as potentially the most desirable one in this series of compounds Data from the NCI-60 cancer panel screening show that compound III is effective on a wide range of different cancers. Importantly, compound III needed up to 17.6-fold less doses to achieve the same IC50 against cancer than non-cancer cells (MDA-MB468 vs MCF10A), suggesting that it can potentially be less toxic to normal cells. Cancer cells formed multiple centrosomes in the presence of compound III, resulting in the cell cycle arrest at prometa-meta phase. This abnormality leads to eventual cell demise with sub-G1 DNA content typically shown with apoptotic cells. In addition, compound III also causes an increase in lysosomal volume in cancer but not in non-cancer cells, which may contribute at least in part to its preferential cancer cell-killing. The cancer cell-killing effect of compound III is highly potentiated when combined with either bortezomib or monastrol.

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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: 7-Chloro-4-(piperazin-1-yl)quinoline( cas:837-52-5 ) is researched.Related Products of 837-52-5.Maether, Marie-Pierre; Bernat, Virginie; Maturano, Marie; Andre-Barres, Christiane; Ladeira, Sonia; Valentin, Alexis; Vial, Henri; Payrastre, Corinne published the article 《Synthesis and antiplasmodial activity of streptocyanine/peroxide and streptocyanine/4-aminoquinoline hybrid dyes》 about this compound( cas:837-52-5 ) in Organic & Biomolecular Chemistry. Keywords: streptocyanine dye cyclic peroxide aminoquinoline antiplasmodial. Let’s learn more about this compound (cas:837-52-5).

Two series of streptocyanine dyes incorporating cyclic peroxide or 4-aminoquinoline moieties are prepared and X-ray diffraction structures for three compounds are determined All hybrid dyes show good antiplasmodial activity (0.06 to 0.66 μM) and are not or are slightly cytotoxic, except 10a.

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Related Products of 837-52-5. 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: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Discovery of a novel CCR5 antagonist lead compound through fragment assembly. Author is Liu, Yanqing; Zhou, Enkun; Yu, Kunqian; Zhu, Jin; Zhang, Yu; Xie, Xin; Li, Jian; Jiang, Hualiang.

CCR5, as the major co-receptor for HIV-1 entry, is an attractive novel target for the pharmaceutical industry in the HIV-1 therapeutic area. In this study, based on the structures of maraviroc and 1,4-bis(4-(7-chloroquinolin-4-yl)piperazin-1-yl)butane-1,4-dione (1), which was identified using structure-based virtual screening in conjunction with a calcium mobilization assay, a series of novel small mol. CCR5 antagonists have been designed and synthesized through fragment assembly. Preliminary SARs were obtained, which are in good agreement with the mol. binding model and should prove helpful for future antagonist design. The novel scaffold presented here might also be useful in the development of maraviroc-derived second generation CCR5 antagonists.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Bioorganic & Medicinal Chemistry Letters called Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids, Author is Lombard, Marli C.; N’Da, David D.; Breytenbach, Jaco C.; Smith, Peter J.; Lategan, Carmen A., which mentions a compound: 837-52-5, SMILESS is C1=C(Cl)C=C2C(=C1)C(=CC=N2)N3CCNCC3, Molecular C13H14ClN3, Computed Properties of C13H14ClN3.

Dihydroartemisinin (DHA) was coupled to different aminoquinoline moieties forming hybrids, which were then treated with oxalic acid to form oxalate salts. Some of the compounds showed comparable potency in vitro to that of chloroquine (CQ) against the chloroquine sensitive (CQS) strain, and were found to be more potent against the chloroquine resistant CQR strain. Hybrid I and its oxalate salt were the most active against CQR strain, being 9- and 7-fold more active than CQ resp. (17.12 nM; 20.76 nM vs. 157.9 nM). An optimum chain length was identified having 2 or 3 Cs with or without an extra methylene substituent.

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