Category: 14660-52-7

Wang, Bingbing; Peng, Pan; Ma, Wan; Liu, Zhao; Huang, Cheng; Cao, Yangmin; Hu, Ping; Qi, Xiaotian; Lu, Qingquan published their research in Journal of the American Chemical Society in 2021. The article was titled 《Electrochemical Borylation of Alkyl Halides: Fast, Scalable Access to Alkyl Boronic Esters》.HPLC of Formula: 14660-52-7 The article contains the following contents:

Herein, a fast, scalable, and transition-metal-free borylation of alkyl halides (X = I, Br, Cl) enabled by electroreduction is reported. This process provides an efficient and practical access to primary, secondary, and tertiary boronic esters at a high current. More than 70 examples, including the late-stage borylation of natural products and drug derivatives, are furnished at room temperature, thereby demonstrating the broad utility and functional-group tolerance of this protocol. Mechanistic studies disclosed that B2cat2 serves as both a reagent and a cathodic mediator, enabling electroreduction of difficult-to-reduce alkyl bromides or chlorides at a low potential. The experimental process involved the reaction of Ethyl 5-bromovalerate(cas: 14660-52-7HPLC of Formula: 14660-52-7)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.HPLC of Formula: 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhang, Mingming; Wei, Wei; Peng, Chengjun; Ma, Xiaodong; He, Xiao; Zhang, Heng; Zhou, Mingkang published their research in Bioorganic & Medicinal Chemistry Letters in 2021. The article was titled 《Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy》.Category: bromides-buliding-blocks The article contains the following contents:

The mTOR and HDAC dual suppression is meaningful for counteracting drug resistance resulted from kinase mutation and bypass mechanisms. Herein, we communicate our recent discovery of a novel structural series of mTOR/HDAC bi-functional inhibitors featuring the pyrazolopyrimidine core via pharmacophore-merging strategy. More than half of them exerted potent dual-target inhibitory activities. In particular, compound 50 exhibited IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, resp., along with remarkably enhanced anti-proliferative activity (IC50 = 1.74μM) against MV4-11 cell line than mTOR inhibitor MLN-0128 (IC50 = 5.84μM) and HDAC inhibitor SAHA (IC50 = 8.44μM). Its intracellular intervention of both mTOR signaling and HDAC was validated by the Western blot anal. Moreover, as the first disclosed mTOR/HDAC dual inhibitor with selectivity for some specific HDAC subtypes, it has the potential to alleviate the adverse effects resulted from pan-HDAC inhibition. Attributed to its favorable in vitro performance, compound 50 is valuable for further functional investigation as a polypharmacol. anti-cancer agent. The experimental process involved the reaction of Ethyl 5-bromovalerate(cas: 14660-52-7Category: bromides-buliding-blocks)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Takahashi, Yusuke; Seki, Masahiko published an article in 2021. The article was titled 《Finkelstein Reaction in Non-polar Organic Solvents: A Streamlined Synthesis of Organic Iodides》, and you may find the article in Organic Process Research & Development.Electric Literature of C7H13BrO2 The information in the text is summarized as follows:

The Finkelstein reaction of organic halides was found to proceed smoothly in non-polar organic solvents other than acetone when operated in the presence of a catalytic amount of tetra-n-butylammonium bromide and water. The new protocol was successfully applied to a preparation of Et 5-iodopentanoate from the corresponding bromide which was used directly for zinc reagent formation and Fukuyama coupling to enable the formation of the (+)-biotin side chain in a streamlined manner. Rate acceleration by microwave irradiation and an application to the synthesis of trimethylsilyl iodide was described as well. In the experiment, the researchers used Ethyl 5-bromovalerate(cas: 14660-52-7Electric Literature of C7H13BrO2)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Electric Literature of C7H13BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Tomasic, Tihomir; Rabbani, Said; Jakob, Roman P.; Reisner, Andreas; Jakopin, Ziga; Maier, Timm; Ernst, Beat; Anderluh, Marko published an article in 2021. The article was titled 《Does targeting Arg98 of FimH lead to high affinity antagonists?》, and you may find the article in European Journal of Medicinal Chemistry.Product Details of 14660-52-7 The information in the text is summarized as follows:

Bacterial resistance has become an important challenge in the treatment of urinary tract infections. The underlying resistance mechanisms can most likely be circumvented with an antiadhesive approach, antagonizing the lectin FimH located at the tip of fimbriae of uropathogenic E. coli. Here we report on a novel series of FimH antagonists based on the 1-(α-D-mannopyranosyl)-4-phenyl-1,2,3-triazole scaffold, designed to incorporate carboxylic acid or ester functions to interact with FimH Arg98. The most potent representative of the series, ester I, displayed a Kd value of 7.6 nM for the lectin domain of FimH with a general conclusion that all esters outperform carboxylates in terms of affinity. Surprisingly, all compounds from this new series exhibited improved binding affinities also for the R98A mutant, indicating another possible interaction contributing to binding. Our study on 1-(α-D-mannopyranosyl)-4-phenyl-1,2,3-triazole-based FimH antagonists offers proof that targeting Arg98 side chain by a “”chem. common sense””, i.e. by introduction of the acidic moiety to form ionic bond with Arg98 is most likely unsuitable approach to boost FimH antagonists’ potency. After reading the article, we found that the author used Ethyl 5-bromovalerate(cas: 14660-52-7Product Details of 14660-52-7)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Product Details of 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

COA of Formula: C7H13BrO2In 2022 ,《Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells》 appeared in European Journal of Medicinal Chemistry. The author of the article were Barreca, Marilia; Ingarra, Angela Maria; Raimondi, Maria Valeria; Spano, Virginia; De Franco, Michele; Menilli, Luca; Gandin, Valentina; Miolo, Giorgia; Barraja, Paola; Montalbano, Alessandra. The article conveys some information:

Searching for new small mols. as photosensitizing agents, the authors have developed a class of twenty-five pyrimido[5,4-g]indolizines I (R = H, COOEt, COOiPr, R1 = H, Ph, COMe, cyclohexyl, cyclopentyl, n = 1) and pyrimido[4,5-c]pyrrolo[1,2-a]azepines I (R = COOEt, COOiPr, R1 = H, Ph, cyclohexyl, cyclopentyl, n = 2) with a good substitution pattern defining a versatile synthetic pathway to approach the title ring systems. All compounds were evaluated for their photocytotoxicity on a triple neg. human breast cancer cell line (MDA-MB-231) in the dark and under UVA light (2.0 J/cm2). The most effective compounds exhibited a photoantiproliferative activity with IC50 values up to nanomolar ranges. Interestingly, these newly developed compounds showed high selectivity towards cancerous cells with respect to non-cancerous ones. Moreover, four representative derivatives were also phototoxic against an addnl. human HER2 pos. breast cancer cell line (HCC1954) and against the HER2 pos. vesical cancer cell line (T24) harboring Hras mutation. Mechanistic studies performed in triple neg. MDA-MB-231 cancer cells revealed the ability of the compounds to increase reactive oxygen species (ROS) production and to induce a thiol redox stress, thus triggering cancer cell death through apoptosis. Apoptotic cell death was also induced in highly aggressive and metastatic HER2 pos. Hras mutated T24-treated bladder cancer cells. Overall, data confirm that these new small photosensitizing agents may represent very promising candidates for phototherapy application against highly aggressive and resistant cancers. The results came from multiple reactions, including the reaction of Ethyl 5-bromovalerate(cas: 14660-52-7COA of Formula: C7H13BrO2)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.COA of Formula: C7H13BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Synthesis and biological evaluation of substituted amide derivatives of C4-ageratochromene dimer analog》 was written by Agarwal, Karishma; Gupta, Kratika; Sharma, Kriti; Khanka, Sonu; Singh, Shilpi; Singh, Jyoti; Trivedi, Laxmikant; Vasdev, Prema G.; Luqman, Suaib; Khan, Feroz; Singh, Divya; Gupta, Atul. Computed Properties of C7H13BrO2 And the article was included in Bioorganic & Medicinal Chemistry Letters in 2021. The article conveys some information:

Substituted amide derivatives of C4-ageratochromene dimer analog were synthesized through structural modification of precocene-I, isolated from the essential oil of Ageratum conyzoides L. The target compounds were evaluated for their bone-forming effect using osteoblast differentiation assay. Seven compounds presented good activity within 1 pM-1 nM concentration At 1 pM concentration, the most active compound (I) showed effective mineralization of osteoblast cells along with expression of osteogenic marker genes viz RUNX 2, BMP-2, and type 1 collagen (Type-1 col) without any toxicity towards osteoblast cells. Single crystal X-ray anal. of two compounds revealed that the core nucleus of these mols. bear Ph rings in a trans-stilbenoid system and had a good structural correlation with 17β-estradiol and diethylstilbestrol (DES). In-silico study about I showed its structural complementarities with the LBD of estrogen receptor (ER) which indicated possible ER-mediated activity of compounds After reading the article, we found that the author used Ethyl 5-bromovalerate(cas: 14660-52-7Computed Properties of C7H13BrO2)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents.Computed Properties of C7H13BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2022,Dallavalle, Sabrina; Musso, Loana; Cincinelli, Raffaella; Darwiche, Nadine; Gervasoni, Silvia; Vistoli, Giulio; Guglielmi, Mario B.; La Porta, Ilaria; Pizzulo, Maddalena; Modica, Elisa; Prosperi, Federica; Signorino, Giacomo; Colelli, Fabiana; Cardile, Francesco; Fucci, Alessandra; D’Andrea, Egildo Luca; Riccio, Assunta; Pisano, Claudio published an article in European Journal of Medicinal Chemistry. The title of the article was 《Antitumor activity of novel POLA1-HDAC11 dual inhibitors》.Category: bromides-buliding-blocks The author mentioned the following in the article:

Hybrid mols. targeting simultaneously DNA polymerase α (POLA1) and histone deacetylases (HDACs) were designed and synthesized to exploit a potential synergy of action. Among a library of screened mols., MIR002 and GEM144 showed antiproliferative activity at nanomolar concentrations on a panel of human solid and haematol. cancer cell lines. In vitro functional assays confirmed that these mols. inhibited POLA1 primer extension activity, as well as HDAC11. Mol. docking studies also supported these findings. Mechanistically, MIR002 and GEM144 induced acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. Oral administration of these inhibitors confirmed their antitumor activity in in vivo models. In human non-small cancer cell (H460) xenografted in nude mice MIR002 at 50 mg/kg, Bid (qd x 5 x 3w) inhibited tumor growth (TGI = 61%). More interestingly, in POLA1 inhibitor resistant cells (H460-R9A), the in vivo combination of MIR002 with cisplatin showed an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment. Moreover, in two human orthotopic malignant pleural mesothelioma xenografts (MM473 and MM487), oral treatments with MIR002 and GEM144 confirmed their significant antitumor activity (TGI = 72-77%). Consistently with recent results that have shown an inverse correlation between POLA1 expression and type I interferon levels, MIR002 significantly upregulated interferon-α in immunocompetent mice. In addition to this study using Ethyl 5-bromovalerate, there are many other studies that have used Ethyl 5-bromovalerate(cas: 14660-52-7Category: bromides-buliding-blocks) was used in this study.

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

The author of 《Oxazole-bridged combretastatin A-4 derivatives with tethered hydroxamic acids: structure-activity relations of new inhibitors of HDAC and/or tubulin function》 were Schmitt, Florian; Gosch, Lisa Chiara; Dittmer, Alexandra; Rothemund, Matthias; Mueller, Thomas; Schobert, Rainer; Biersack, Bernhard; Volkamer, Andrea; Hoepfner, Michael. And the article was published in International Journal of Molecular Sciences in 2019. Safety of Ethyl 5-bromovalerate The author mentioned the following in the article:

New inhibitors of tubulin polymerization and/or histone deacetylase (HDAC) activity were synthesized by attaching alkyl tethered hydroxamic acid appendages of varying length to oxazole-bridged combretastatin A-4 analogous caps. While their antiproliferative and microtubule disrupting effect was most pronounced for derivatives with short spacers, HDAC inhibition was strongest for those with longer spacers. These findings were further supported by computational methods such as structure-based docking experiments exploring the target interactions of the derivatives with varying linkers. For instance, compounds featuring short four-atom spacers between cap and hydroxamic acid inhibited the growth of various cancer cell lines and human endothelial hybrid cells with IC50 values in the low nanomolar range. In line with their ability to inhibit the microtubule assembly, four- and five-atom spacered hydroxamic acids caused an accumulation of 518A2 melanoma cells in G2/M phase, whereas a compound featuring a six-atom spacer and performing best in HDAC inhibition, induced a G1 arrest in these cells. All these beneficial anticancer activities together with their selectivity for cancer cells over non-malignant cells, point out the great potential of these novel pleiotropic HDAC and tubulin inhibitors as drug candidates for cancer therapy. In the part of experimental materials, we found many familiar compounds, such as Ethyl 5-bromovalerate(cas: 14660-52-7Safety of Ethyl 5-bromovalerate)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Safety of Ethyl 5-bromovalerate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2022,Bhumireddy, Archana; Bandaru, N. V. M. Rao; Raghurami Reddy, B.; Gore, Suraj T.; Mukherjee, Subhendu; Balasubramanian, Wesley Roy; Sumanth Kumar, V.; Alapati, Krishna Satya; Venkata Gowri Chandra Sekhar, Kondapalli; Nellore, Kavitha; Abbineni, Chandrasekhar; Samajdar, Susanta published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Design, synthesis, and biological evaluation of phenyl thiazole-based AR-V7 degraders》.Recommanded Product: Ethyl 5-bromovalerate The author mentioned the following in the article:

Multiple Splice variants of AR have been reported in the past few years. These splice variants are upregulated in most cases of CRPC resulting in poor prognosis. Most of these variants lack the ligand binding domain (LBD) but still bind to DNA resulting in constitutive activation of downstream targets. The AR-V7 splice variant has been characterized extensively and current clin. trials in CRPC are exploring the use of AR-V7 as a biomarker. New therapeutic mols. that selectively target AR-V7 are also being explored. However, there is a dearth of information available on the selectivity, phenotypic responses in AR-V7 dependent cell lines and pharmacokinetic properties of such mols. Using our proprietary computational algorithms and rational SAR optimization, we have developed a potent and selective AR-V7 degrader from a known AR DNA binding domain (DBD) binder. This mol. effectively degraded AR-V7 in a CRPC cell line and demonstrated good oral bioavailability in mouse PK studies. This tool compound can be used to evaluate the pharmacol. effects of AR-V7 degraders. Further exploration of SAR can be pursued to develop more optimized lead compoundsEthyl 5-bromovalerate(cas: 14660-52-7Recommanded Product: Ethyl 5-bromovalerate) was used in this study.

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Recommanded Product: Ethyl 5-bromovalerate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Product Details of 14660-52-7In 2021 ,《Identification of histone deacetylase inhibitors with (arylidene)aminoxy scaffold active in uveal melanoma cell lines》 was published in Journal of Enzyme Inhibition and Medicinal Chemistry. The article was written by Nencetti, Susanna; Cuffaro, Doretta; Nuti, Elisa; Ciccone, Lidia; Rossello, Armando; Fabbi, Marina; Ballante, Flavio; Ortore, Gabriella; Carbotti, Grazia; Campelli, Francesco; Banti, Irene; Gangemi, Rosaria; Marshall, Garland R.; Orlandini, Elisabetta. The article contains the following contents:

Uveal melanoma (UM) represents an aggressive type of cancer and currently, there is no effective treatment for this metastatic disease. In the last years, histone deacetylase inhibitors (HDACIs) have been studied as a possible therapeutic treatment for UM, alone or in association with other chemotherapeutic agents. Here we synthesized a series of new HDACIs based on the SAHA scaffold bearing an (arylidene)aminoxy moiety. Their HDAC inhibitory activity was evaluated on isolated human HDAC1, 3, 6, and 8 by fluorometric assay and their binding mode in the catalytic site of HDACs was studied by mol. docking. The most promising hit was the quinoline derivative , a nanomolar inhibitor of HDAC6, which exhibited a good antiproliferative effect on UM cell lines at micromolar concentration and a capability to modify the mRNA levels of HDAC target genes similar to that of SAHA. The experimental part of the paper was very detailed, including the reaction process of Ethyl 5-bromovalerate(cas: 14660-52-7Product Details of 14660-52-7)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Product Details of 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary