Category: 76283-09-5

Ren, Bo published the artcileDesign, synthesis and in vitro antitumor evaluation of novel pyrazole-benzimidazole derivatives, Name: 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 128097, database is CAplus and MEDLINE.

A series of novel pyrazole-benzimidazole derivatives I [R = Br, MeO; R¹ = Pr, benzyl, cinnamyl, etc.] were designed, synthesized and evaluated for their in-vitro antiproliferative activity against the HCT116, MCF-7 and Huh-7 cell lines. Among them, compounds I [R = Br, R¹ = Pr, 4-(trifluoromethyl)benzyl; R = MeO, 4-cyanomethyl] showed significant antiproliferative activity against HCT116 cell lines with the IC₅₀ values of 4.33, 5.15 and 4.84μM, resp. Moreover, fluorescent staining studies showed compound I [R = Br, R¹ = 4-(trifluoromethyl)benzyl] could induce cancer cells apoptosis. The flow cytometry assay revealed that compound I [R = Br, R¹ = 4-(trifluoromethyl)benzyl] could induce cell cycle arrest at G0/G1 phase. All in all, these consequences suggested that pyrazole-benzimidazole derivatives I could serve as promising compounds for further research to develop novel and highly potent cancer therapy agents.

Bioorganic & Medicinal Chemistry Letters published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Name: 4-Bromo-1-(bromomethyl)-2-fluorobenzene.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Li, Minglei published the artcileSynthesis and fungicidal activities of (E)-α-oxocyclododecanone oxime ethers, COA of Formula: C7H5Br2F, the publication is Nongyaoxue Xuebao (2006), 8(3), 209-213, database is CAplus.

A series of (E)-α-oxocyclododecanone oxime ethers were synthesized by etherification of corresponding hydroxylimines in yields of 59%-92%. The (E)-configuration was confirmed by single X-ray diffraction anal. of a representative compound Bioassay results showed that most of the synthesized compounds present good fungicidal activities against Rhizoctonia solani, Cladosporium cucumerinum, Colletotrichum orbiculare, Botrytis cinerea, Fusarium oxysporum, and Phomopsis asparagi. For example, the EC₅₀ values of I against mentioned-above six fungi were 13, 9, 12, 19, 14, 3 mg/L, resp.

Nongyaoxue Xuebao published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, COA of Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Li, Hao-Chun published the artcileColor tuning and highly efficient blue emitters of finite diphenylamino-containing oligo(arylenevinylene) derivatives using fluoro substituents, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is Advanced Functional Materials (2007), 17(4), 520-530, database is CAplus.

New fluoro derivatives of Ph₂N-containing (Ph: phenyl) oligo(arylenevinylene) derivatives were prepared by using double Heck-coupling reactions or Horner-Wadsworth-Emmons reactions. These oligomers are highly fluorescent (fluorescence quantum yields Φ = 0.93-0.68) with emissions in a broad wavelength region (448-579 nm), depending on the position of the fluoro substituents. The highest occupied and LUMO (HOMO-LUMO) energy levels of these oligomers were characterized by electrochem. and UV spectroscopy. The effects of the fluoro substituents on the energy levels are rationalized with HOMO-LUMO simulations. In a classical organic light emitting diode (OLED), one representative (5a) shows a remarkable external quantum efficiency value (η_ext = 4.87 %) at J = 20 mA cm^-2; the maximum brightness at 10.2 V is 22,506 cd m^-2 (λ = 458 nm; Commission Internationale de l’Eclairage (CIE) coordinates x = 0.14, y = 0.14) with a full width at half-maximum of 54 nm, demonstrating the superiority of these fluoro-containing oligomers in OLED devices.

Advanced Functional Materials published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Li, Hui published the artcileAllosteric Inhibitors of Hepatitis C Polymerase: Discovery of Potent and Orally Bioavailable Carbon-Linked Dihydropyrones, Product Details of C7H5Br2F, the publication is Journal of Medicinal Chemistry (2007), 50(17), 3969-3972, database is CAplus and MEDLINE.

The discovery and optimization of a novel class of carbon-linked dihydropyrones as allosteric HCV NS5B polymerase inhibitors are presented. Replacement of the sulfur linker atom with carbon reduced compound acidity and greatly increased cell permeation. Further structure-activity relationship (SAR) studies led to the identification of compounds, exemplified by (I) and (II), with significantly improved antiviral activities in the cell-based replicon assay and favorable pharmacokinetic profiles.

Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Product Details of C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Zhang, Wen-Jin published the artcileSynthesis and identification of quinoline derivatives as topoisomerase I inhibitors with potent antipsoriasis activity in an animal model, Category: bromides-buliding-blocks, the publication is Bioorganic Chemistry (2019), 102899, database is CAplus and MEDLINE.

Psoriasis is a chronic inflammatory and immune-mediated skin disease. Although certain agents have shown clin. success in treating psoriasis, development of safe and effective strategies for the treatment of this condition remains important. Research suggests that DNA topoisomerase I (Topo I) inhibitors may have potent psoriasis-ameliorating effects. Here, 25 quinoline derivatives were synthesized and identified as Topo I inhibitors. These compounds inhibited the 12-O-tetradecanoylphorbol-13-acetate-induced mouse ear inflammation. The most potent analogs, 5i and 5l, suppressed the expression of inflammatory cytokines in lipopolysaccharide-stimulated HaCaT cells. Addnl., the lead compounds significantly improved imiquimod-induced psoriasis-like inflammation in mice. Moreover, the expression levels of cytokines and inflammatory mediators, such as interleukin (IL)-17A, IL-22, IL-23, nuclear factor-κB subunit p65, tumor necrosis factor-α, and interferon-γ, were dramatically inhibited in the dorsal skin of 5i- and 5l-treated mice. These findings indicate that the inhibition of Topo I activity may potentially be an effective strategy for psoriasis treatment.

Bioorganic Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C42H63O3P, Category: bromides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Wang, Yaping published the artcileOne-Pot Double Benzylation of 2-Substituted Pyridines using Palladium-Catalyzed Decarboxylative Coupling of sp² and sp³ Carbons, Related Products of bromides-buliding-blocks, the publication is Advanced Synthesis & Catalysis (2014), 356(16), 3307-3313, database is CAplus.

An efficient and practical decarboxylative double benzylation method for various 2-picolinic acids has been established by using a bimetallic catalytic system of palladium(II) chloride (PdCl₂) and silver(I) oxide (Ag₂O), which offered a variety of diarylmethane derivatives e.g., I, with moderate to good yields.

Advanced Synthesis & Catalysis published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C15H14Cl2S2, Related Products of bromides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Ding, Xiao published the artcileDe Novo Design, Synthesis and Evaluation of Benzylpiperazine Derivatives as Highly Selective Binders of Mcl-1, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is ChemMedChem (2013), 8(12), 1986-2014, database is CAplus and MEDLINE.

Considerable efforts have been made towards the development of small-mol. inhibitors of antiapoptotic B-cell lymphoma 2 (Bcl-2) family proteins (such as Bcl-2, Bcl-x_L, and Mcl-1) as a new class of anticancer therapies. Unlike general inhibitors of the entire family, selective inhibitors of each member protein can hopefully reduce the adverse side effects in chemotherapy treatments of cancers overexpressing different Bcl-2 family proteins. In this study, we designed four series of benzylpiperazine derivatives as plausible Bcl-2 inhibitors based on the outcomes of a computational algorithm. A total of 81 compounds were synthesized, and their binding affinities to Bcl-2, Bcl-x_L, and Mcl-1 measured. Encouragingly, 22 compounds exhibited binding affinities in the micromolar range (K_i<20 μM) to at least one target protein. Moreover, some compounds were observed to be highly selective binders to Mcl-1 with no detectable binding to Bcl-2 or Bcl-x_L, among which the most potent one, I, has a K_i value of 0.18 μM for Mcl-1. Binding modes of four selected compounds to Mcl-1 and Bcl-x_L were derived through mol. docking and mol. dynamics simulations. It seems that the binding affinity and selectivity of these compounds can be reasonably interpreted with these models. Our study demonstrated the possibility for obtaining selective Mcl-1 inhibitors with relatively simple chem. scaffolds. The active compounds identified by us could be used as lead compounds for developing even more potent selective Mcl-1 inhibitors with potential pharmaceutical applications.

ChemMedChem published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Kosmalski, Tomasz published the artcileNew heterocyclic oxime ethers of 1-(benzofuran-2-yl)ethan-1-one and their antimicrobial activity, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene, the publication is Acta Poloniae Pharmaceutica (2015), 72(2), 289-295, database is CAplus.

A series of benzofurans I (R = 4-CF₃, 4-Br-2-F, 2,6-F₂, etc.) were synthesized starting from 2-acetylbenzofuran. Antimicrobial activities of the compounds were examined and notable activity was observed

Acta Poloniae Pharmaceutica published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Zhang, Qiang published the artcileDesign and synthesis of benzyl aminocoumarin and its anti-Alzheimer′s activity, Formula: C7H5Br2F, the publication is New Journal of Chemistry (2021), 45(37), 17287-17300, database is CAplus.

Benzylaminocoumarin is a kind of compound with coumarin skeleton and benzylamino side chain structure at positions 3 and 4. Our group has previously explored the AD activity of 3-(4-aminophenyl) coumarin and obtained benzylaminocoumarin by further structural modification of benzamide side chains. A total of 29 benzylaminocoumarins were synthesized, and the compounds were tested for anti-AD-related activities, and compounds M3, M11, M21 and M26 were found to show good AChE inhibitory activity by in vitro activity experiments, with compound M11 (IC50 = 0.068 ± 0.04) showing better AChE inhibitory activity than the pos. drug donepezil (IC50 = 0.079 ± 0.008). The compound showed good MAO inhibitory activity against M3 and M11, of which compound M11 (IC50 = 6.312 ± 0.03) showed the best MAO-B inhibitory activity, but was weaker than the pos. drug donepezil (IC50 = 1.697 ± 0.01). The exptl. results showed that compounds M21 and M26 could selectively inhibit the AChE activity, and their probability of producing toxic side effects was low. Compound M11 shows dual AChE and MAO inhibitory activity and can be used as a potential therapeutic agent for the treatment of AD. In anti-AD multitarget drug research, multitarget inhibitors have low limitations and are able to produce better therapeutic effects on the entire disease system.

New Journal of Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C9H22OSi, Formula: C7H5Br2F.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Ward, Simon E. published the artcileIntegration of Lead Optimization with Crystallography for a Membrane-Bound Ion Channel Target: Discovery of a New Class of AMPA Receptor Positive Allosteric Modulators, Synthetic Route of 76283-09-5, the publication is Journal of Medicinal Chemistry (2011), 54(1), 78-94, database is CAplus and MEDLINE.

A novel series of AMPAR pos. modulators is described that were identified by high throughput screening. The mols. of the series have been optimized from a high quality starting point hit to afford excellent developability, tolerability, and efficacy profiles, leading to identification of a clin. candidate. Unusually for an ion channel target, this optimization was integrated with regular generation of ligand-bound crystal structures and uncovered a novel chemotype with a unique and highly conserved mode of interaction via a trifluoromethyl group.

Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C14H10O4S2, Synthetic Route of 76283-09-5.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary