Category: 14660-52-7

In 2019,Bioorganic Chemistry included an article by Karamitri, Angeliki; Sadek, Mirna S.; Journe, Anne-Sophie; Gbahou, Florence; Gerbier, Romain; Osman, Mai B.; Habib, Samy A. M.; Jockers, Ralf; Zlotos, Darius P.. Recommanded Product: 14660-52-7. The article was titled 《O-linked melatonin dimers as bivalent ligands targeting dimeric melatonin receptors》. The information in the text is summarized as follows:

A series of dimeric melatonin analogs 3a-e obtained by connecting two melatonin mols. through the methoxy oxygen atoms with spacers spanning 16-24 atoms and the agomelatine dimer 7 were synthesized and characterized in 2-[125-I]-iodomelatonin binding assays, bioluminescence resonance energy transfer (BRET) experiments, and in functional cAMP and β-arrestin recruitment assays at MT1 and MT2 receptors. The binding affinity of 3a-e generally increased with increasing linker length. Bivalent ligands 3a-e increased BRET signals of MT1 dimers up to 3-fold compared to the monomeric control ligand indicating the simultaneous binding of the two pharmacophores to dimeric receptors. Bivalent ligands 3c and 7 exhibited important changes in functional properties on the Gi/cAMP pathway but not on the β-arrestin pathway compared to their monomeric counterparts. Interestingly, 3c (20 atoms spacer) shows inverse agonistic properties at MT2 on the Gi/cAMP pathway. In conclusion, these findings indicate that O-linked melatonin dimers are promising tools to develop signaling pathway-based bivalent melatonin receptor ligands. The experimental process involved the reaction of Ethyl 5-bromovalerate(cas: 14660-52-7Recommanded Product: 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.Recommanded Product: 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Structure-Activity Relationship of Antischistosomal Ozonide Carboxylic Acids》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Wu, Jianbo; Wang, Xiaofang; Chiu, Francis C. K.; Haberli, Cecile; Shackleford, David M.; Ryan, Eileen; Kamaraj, Sriraghavan; Bulbule, Vivek J.; Wallick, Alexander I.; Dong, Yuxiang; White, Karen L.; Davis, Paul H.; Charman, Susan A.; Keiser, Jennifer; Vennerstrom, Jonathan L.. Reference of Ethyl 5-bromovalerate The article mentions the following:

Semisynthetic artemisinins and other bioactive peroxides are best known for their powerful antimalarial activities, and they also show substantial activity against schistosomes-another Hb-degrading pathogen. Building on this discovery, we now describe the initial structure-activity relationship (SAR) of antischistosomal ozonide carboxylic acids OZ418 (2) and OZ165 (3). Irresp. of lipophilicity, these ozonide weak acids have relatively low aqueous solubilities and high protein binding values. Ozonides with para-substituted carboxymethoxy and N-benzylglycine substituents had high antischistosomal efficacies. It was possible to increase solubility, decrease protein binding, and maintain the high antischistosomal activity in mice infected with juvenile and adult Schistosoma mansoni by incorporating a weak base functional group in these compounds In some cases, adding polar functional groups and heteroatoms to the spiroadamantane substructure increased the solubility and metabolic stability, but in all cases decreased the antischistosomal activity. In the part of experimental materials, we found many familiar compounds, such as Ethyl 5-bromovalerate(cas: 14660-52-7Reference of Ethyl 5-bromovalerate)

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.Reference of Ethyl 5-bromovalerate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2019,Journal of Organic Chemistry included an article by Ding, Shao-Lei; Ji, Yang; Su, Yan; Li, Rui; Gu, Peiming. Synthetic Route of C7H13BrO2. The article was titled 《Schmidt Reaction of ω-Azido Valeryl Chlorides Followed by Intermolecular Trapping of the Rearrangement Ions: Synthesis of Assoanine and Related Pyrrolophenanthridine Alkaloids》. The information in the text is summarized as follows:

The Schmidt reaction of ω-azido valeryl chlorides in the presence of an addnl. nucleophile was explored. The arenes, alcs., and amines were demonstrated as the intermol. trapping reagents for isocyanate ion and N-acyliminium ion from the Schmidt rearrangement, affording the corresponding products with moderate to excellent yields. Two 2-oxoindoles from the reaction were successfully converted into four natural alkaloids, namely, assoanine, anhydrolycorine, oxoassoanine, and anhydrolycorinone. The results came from multiple reactions, including the reaction of Ethyl 5-bromovalerate(cas: 14660-52-7Synthetic Route 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.Synthetic Route of C7H13BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Application of 14660-52-7In 2020 ,《Multitarget Compounds for Bipolar Disorder: From Rational Design to Preliminary Pharmacokinetic Evaluation》 appeared in ChemMedChem. The author of the article were Di Martino, Rita Maria Concetta; Bottegoni, Giovanni; Seghetti, Francesca; Russo, Debora; Penna, Ilaria; De Simone, Alessio; Ottonello, Giuliana; Mandrup Bertozzi, Sine; Armirotti, Andrea; Bandiera, Tiziano; Belluti, Federica; Cavalli, Andrea. The article conveys some information:

Due to the complex and multifactorial nature of bipolar disorder (BD), single-target drugs have traditionally provided limited relief with no disease-modifying effects. In line with the polypharmacol. paradigm, we attempted to overcome these limitations by devising two series of multitarget-directed ligands endowed with both a partial agonist profile at dopamine receptor D3 (D3R) and inhibitory activity against glycogen synthase kinase 3 beta (GSK-3β). These are two structurally unrelated targets that play independent, yet connected, roles in cognition and mood regulation. Two compounds (7 and 10) emerged as promising D3R/GSK-3β multitarget-directed ligands with nanomolar activity at D3R and low-micromolar inhibition of GSK-3β, thereby confirming, albeit preliminarily, the feasibility of our strategy. Furthermore, 7 showed promising drug-like properties in stability and pharmacokinetic studies. In the experiment, the researchers used Ethyl 5-bromovalerate(cas: 14660-52-7Application 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.Application of 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Related Products of 14660-52-7In 2019 ,《Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases》 appeared in Journal of Medicinal Chemistry. The author of the article were Zhang, Kehui; Lai, Fangfang; Lin, Songwen; Ji, Ming; Zhang, Jingbo; Zhang, Yan; Jin, Jing; Fu, Rong; Wu, Deyu; Tian, Hua; Xue, Nina; Sheng, Li; Zou, Xiaowen; Li, Yan; Chen, Xiaoguang; Xu, Heng. The article conveys some information:

Polypharmacol. is a promising paradigm in modern drug discovery. Herein, we have discovered a series of novel PI3K and HDAC dual inhibitors in which the hydroxamic acid moiety as the zinc binding functional group was introduced to a quinazoline-based PI3K pharmacophore through an appropriate linker. Systematic structure-activity relationship studies resulted in lead compounds 23 (shown in graphical abstract and duplicated as I) and 36 (II) that simultaneously inhibited PI3K and HDAC with nanomolar potencies and demonstrated favorable antiproliferative activities. Compounds 23 and 36 efficiently modulated the expression of p-AKT and Ac-H3, arrested the cell cycle, and induced apoptosis in HCT116 cancer cells. Following pharmacokinetic studies, 23 was further evaluated in HCT116 and HGC-27 xenograft models to show significant in vivo anticancer efficacies with tumor growth inhibitions of 45.8% (po, 150 mg/kg) and 62.6% (i.p., 30 mg/kg), resp. Overall, this work shows promise in discovering new anticancer therapeutics by the approach of simultaneously targeting PI3K and HDAC pathways with a single mol. In the experimental materials used by the author, we found Ethyl 5-bromovalerate(cas: 14660-52-7Related Products 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.Related Products of 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia》 was written by Liang, Jinhao; Huang, Yi-You; Zhou, Qian; Gao, Yuqi; Li, Zhe; Wu, Deyan; Yu, Si; Guo, Lei; Chen, Zhen; Huang, Ling; Liang, Steven H.; He, Xixin; Wu, Ruibo; Luo, Hai-Bin. Category: bromides-buliding-blocks And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:

To validate PDE4 inhibitors as novel therapeutic agents against vascular dementia (VaD), 25 derivatives were discovered from the natural inhibitor α-mangostin (IC50 = 1.31μM). Hit-to-lead optimization identified a novel and selective PDE4 inhibitor 4e (IC50 = 17 nM), which adopted a different binding pattern from PDE4 inhibitors roflumilast and rolipram. Oral administration of 4e at a dose of 10 mg/kg exhibited remarkable therapeutic effects in a VaD model and did not cause emesis to beagle dogs, indicating its potential as a novel anti-VaD agent. In the experiment, the researchers used many compounds, for example, Ethyl 5-bromovalerate(cas: 14660-52-7Category: bromides-buliding-blocks)

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

Hwang, Nicky; Sun, Liren; Noe, Daisy; Lam, Patrick Y. S.; Zhou, Tianlun; Block, Timothy M.; Du, Yanming published an article in 2021. The article was titled 《Hepatoselective Dihydroquinolizinone Bis-acids for HBsAg mRNA Degradation》, and you may find the article in ACS Medicinal Chemistry Letters.Reference of Ethyl 5-bromovalerate The information in the text is summarized as follows:

Chronic hepatitis B (CHB) is characterized by high levels of hepatitis B virus (HBV) surface antigen (HBsAg) in blood circulation. A major goal of CHB interventions is reducing or eliminating this antigenemia; however, there are currently no approved methods that can do this. A novel family of compounds with a dihydroquinolizinone (DHQ) scaffold has been shown to reduce circulating levels of HBsAg in animals, representing a first for a small mol. Reductions of HBsAg were a result of the compound’s effect on HBsAg mRNA levels. However, com. development by Roche of a DHQ lead compound, RG-7834, was stopped due to undisclosed toxicity issues. Herein we report our effort to convert the systemic RG7834 compound to a hepatoselective DHQ analog to limit its distribution to the bloodstream and thus to other body tissues. The experimental process involved the reaction of Ethyl 5-bromovalerate(cas: 14660-52-7Reference 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.Reference of Ethyl 5-bromovalerate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhang, Kezhuo; Huang, Jiaxin; Zhao, Wanxiang published an article in 2022. The article was titled 《Rh-Catalyzed Coupling of Aldehydes with Allylboronates Enables Facile Access to Ketones》, and you may find the article in Chemistry – A European Journal.SDS of cas: 14660-52-7 The information in the text is summarized as follows:

A novel strategy for the preparation of ketones R1C(O)CHR2CH2CH2R3 (R1 = n-pentyl, cyclohexyl, Ph, 2-thienyl, 4-pyridinyl, etc., R2 = R3 = H; R1 = Ph, R2 = Ph, 4-MeC6H4, 2-naphthyl, 3-furyl, etc., R3 = H; R1 = Ph, R2 = H, R3 = Et, Ph; etc.) from aldehydes R1CHO and allylic boronic esters R2CH:CHCHR3Bpin is presented. This reaction involves the allylation of aldehydes with allylic boronic esters and the Rh-catalyzed chain-walking of homoallylic alcs. The key to this successful development is the protodeboronation of alkenyl boryl ether intermediate via a tetravalent borate anion species in the presence of KHF2 and MeOH. This approach features mild reaction conditions, broad substrate scope, and excellent functional group tolerance. Mechanistic studies also supported that the tandem allylation and chain-walking process are involved.Ethyl 5-bromovalerate(cas: 14660-52-7SDS of cas: 14660-52-7) was used in this study.

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.SDS of cas: 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

HPLC of Formula: 14660-52-7In 2021 ,《Novel Nonsecosteroidal Vitamin D Receptor Modulator Combined with Gemcitabine Enhances Pancreatic Cancer Therapy through Remodeling of the Tumor Microenvironment》 appeared in Journal of Medicinal Chemistry. The author of the article were Kang, Zisheng; Wang, Cong; Tong, Yu; Li, Yanyi; Gao, Yi; Hou, Siyuan; Hao, Meixi; Han, Xiaolin; Wang, Bin; Wang, Qianqian; Zhang, Can. The article conveys some information:

In a pancreatic tumor microenvironment, activated pancreatic stellate cells (PSCs) produce extracellular matrix (ECM) to form a barrier to drug penetration. Moreover, the interaction between cancer cells and activated PSCs promotes the tumor growth. Vitamin D receptor (VDR), as a key regulator to promote the recovery of PSCs to the resting state, is an attractive therapeutic target for pancreatic cancer. Herein, we reported the design and synthesis of 57 nonsecosteroidal VDR modulators based on the skeleton of phenyl-pyrrolyl pentane. Among them, compounds C4, I5, and I8 exhibited excellent VDR affinity and effective inhibition of the activation of PSCs, as well as potent suppression of the interaction between cancer cells and PSCs in vitro. In vivo, compound I5 combined with gemcitabine achieved efficacious antitumor activity without causing hypercalcemia. In conclusion, the compounds designed in our study can remodel the tumor microenvironment and are expected to be candidates for the treatment of pancreatic cancer. 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. 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.HPLC of Formula: 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Application of 14660-52-7In 2019 ,《Design, synthesis, and biological evaluation of quinazoline derivatives as dual HDAC1 and HDAC6 inhibitors for the treatment of cancer》 appeared in Chemical Biology & Drug Design. The author of the article were Chen, Jinying; Sang, Zitai; Jiang, Youjun; Yang, Chao; He, Linhong. The article conveys some information:

Fifty-eight quinazoline-based compounds were designed and synthesized based on the structural optimizations from the lead compound 23bb in an attempt to search for more potent dual HDAC1 and HDAC6 inhibitors. Among them, 32c (HDAC1, IC50 = 31.10 ± 0.37 nM; HDAC6, IC50 = 16.15 ± 0.62 nM) and 32d (HDAC1, IC50 = 37.00 ± 0.24 nM; HDAC6, IC50 = 35.00 ± 0.71 nM) were not only identified as potent dual-acting HDAC1 and HDAC6 inhibitors with over 10-fold selectivity to the other HDACs, but also displayed activities in tubulin acetylation and histone H3 acetylation induction. Importantly, both of them displayed strong antiproliferative activities against various tumor cell lines in vitro with IC50 values <40 nM, especially for hematol. tumors cells (U266 and RPMI8226, IC50 < 1 nM), which were even better than 23bb and SAHA. Furthermore, 32c showed a significant tumor growth inhibition (antitumor rate = 63.98%, p < 0.05) in the resistant MCF-7/ADR xenograft model without any obvious body weight changes and abnormal behaviors. The authors' findings validate that 32c is a potent dual inhibitor of HDAC1/6 that can be an efficacious treatment for breast cancer with Adriamycin resistance. In the experiment, the researchers used Ethyl 5-bromovalerate(cas: 14660-52-7Application 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.Application of 14660-52-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary