Category: 539-74-2

《Synthesis, labeling and biological evolution of new thiopyrano[2,3-b]pyridine derivatives as potential anticancer agents》 was written by Sofan, Mamdouh Abdel-Monem; Hamama, Wafaa Salama; El-Hawary, Ibrahim Ibrahim; Ibrahim, Ismail Taha; Zoorob, Hanafi Hassan. Product Details of 539-74-2This research focused onthiopyranopyridine preparation anticancer. The article conveys some information:

The new thiopyrano[2,3-b]pyridines could be synthesized from the nicotinonitrile derivative The cytotoxicity activity of the selected compounds I, II and III was tested against MCF-7 and HCT-116 cell lines. The compound I (TP5) exhibited significant inhibitory activity and displayed the most potent activity, more than II and III. The compound I with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent. In the light of this result, the labeled 125I-compound I (125I-TP5) was prepared and its cytotoxicity against ascites tumor in mice has been evaluated. The results show that compound I (TP5) may be potentially used as a radiopharmaceutical for tumor diagnosis when labeled with 125I. In addition to this study using Ethyl 3-bromopropanoate, there are many other studies that have used Ethyl 3-bromopropanoate(cas: 539-74-2Product Details of 539-74-2) was used in this study.

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Due to the reactivity of bromide, they are used as potential precursors or important intermediates in organic synthesis. Product Details of 539-74-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Liu, Qi; Wang, Leqi; Hu, Xinping; Zhou, Chuhang; Tang, Yingwei; Ma, Yining; Wang, Xiaoxiao; Liu, Yan published their research in Journal of Chinese Pharmaceutical Sciences in 2021. The article was titled 《Fabrication of deoxycholic acid-modified polymeric micelles and their transmembrane transport》.Related Products of 539-74-2 The article contains the following contents:

Oral administration is the best way for the most patients due to the good compliance, and intestinal epithelium is the main barrier of oral drug absorption. In order to overcome the small intestine epithelial barrier to orally deliver water-insoluble drugs, deoxycholic acid (DA), a substrate of the intestinal bile acid transporters, conjugated poly (2-ethyl-2-oxazoline)-poly (D, L-lactide) (DA-PEOz-PLA) was designed and synthesized, and deoxycholic acid-modified polymeric micelles composed of DA-PEOz-PLA and mPEG-PLA were fabricated to encapsulate model drug coumarin 6 (C6) based on intestinal bile acid pathway. The structure of DA-PEOz-PLA was confirmed using 1H NMR and TLC, and the mol. weight measured by GPC was 10034 g/mol with a PDI of 1.51. The C6-loaded polymeric micelles with drug loading content of 0.085% were characterized to have 40.11 nm in diameter and uniform spherical morphol. observed by TEM. Furthermore, the deoxycholic acid-modified polymeric micelles were demonstrated to further enhance the transmembrane transport efficiency. The mechanic study evidenced that anchorage of deoxycholic acid onto the micelles surface enriched their transcellular transport pathway. Therefore, the designed deoxycholic acid-modified polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs. The results came from multiple reactions, including the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Related Products of 539-74-2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Related Products of 539-74-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2022,Liu, Yulin; Uras, Giuseppe; Onuwaje, Itse; Li, Wenlong; Yao, Hong; Xu, Shengtao; Li, Xinuo; Li, Xinnan; Phillips, James; Allen, Stephanie; Gong, Qi; Zhang, Haiyan; Zhu, Zheying; Liu, Jie; Xu, Jinyi published an article in European Journal of Medicinal Chemistry. The title of the article was 《Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer’s disease》.Recommanded Product: Ethyl 3-bromopropanoate The author mentioned the following in the article:

A series of sulfone analogs of donepezil I (R1 = H, F; R2 = H, 4-F, 3-Cl, etc.) were designed and synthesized as novel acetylcholinesterase (AChE) inhibitors with the potent inhibiting Aβ aggregation and providing neuroprotective effects as potential modalities for Alzheimer’s disease (AD). Most of the target compounds displayed effective inhibition of AChE, especially compound II which displayed powerful inhibitory activity (IC50 = 2.4 nM). Kinetic and docking studies indicated that compound II was a mixed-type inhibitor. Furthermore, in glyceraldehyde (GA)-exposed SH-SY5Y differentiated neuronal cells, compound II could potently inhibit AChE, reduce tau phosphorylation at S396 residue, provide neuroprotection by rescuing neuronal morphol. and increasing cell viability. It was also found to reduce amyloid aggregation in the presence of AChE. In addition, compound II showed evident protections from mitochondrial membrane dysfunction and oxidative stress in okadaic acid-induced pharmacol. models. Moreover, compound II exhibited more effective treatment prospects in vivo than donepezil, including a moderate blood-brain barrier permeability, a more potent AChE inhibitory activity and behavioral improvement in scopolamine-induced cognition-impaired mice model at a much lower dose. Collectively, compound II is a promising lead compound for further investigation to discovery and development of new anti-AD agents. The experimental process involved the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Recommanded Product: Ethyl 3-bromopropanoate)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds. 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: Ethyl 3-bromopropanoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Luo, Guoshun; Lin, Xin; Ren, Shengnan; Wu, Shuangjie; Wang, Xin; Ma, Luyu; Xiang, Hua published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer》.Category: bromides-buliding-blocks The article contains the following contents:

Concomitant inhibition of estrogen receptor alpha (ERα) and histone deacetylase (HDAC) signaling has been proven effective in endocrine-resistant ER+ breast cancers. Herein, a series of tetrahydroisoquinoline (THIQ)-hydroxamate conjugates were rationally designed and synthesized as dual SERDs/HDAC inhibitors by incorporating the hydroxamate, a known HDAC pharmacophore, into a privileged THIQ scaffold of selective ERα degraders (SERDs). Some of these THIQ-hydroxamate conjugates displayed remarkable HDAC6 inhibition and improved antiproliferative activity against MCF-7 cells. Particularly, the most potent HDAC inhibitor 19k also exhibits potent ERα binding affinity, good ERα degradation efficacy and the best antiproliferative activity. Besides, 19k displayed superior antitumor efficacy than the drug combination (Fulvestrant + SAHA) through promoting ERα degradation and histone acetylation in an MCF-7 xenograft model, without causing observable toxicity. Collectively, this study validates the therapeutic potential of a dual-acting compound with potent ERα degradation efficacy and HDAC6 inhibition in breast cancer. In the part of experimental materials, we found many familiar compounds, such as Ethyl 3-bromopropanoate(cas: 539-74-2Category: bromides-buliding-blocks)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides. Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Related Products of 539-74-2In 2021 ,《Synthesis of novel pyrazolo[3,4-b]quinolinebisphosphonic acids and an unexpected intramolecular cyclization and phosphonylation reaction》 appeared in Organic & Biomolecular Chemistry. The author of the article were Teixeira, Fatima C.; Lucas, Carla; Curto, M. Joao M.; Andre, Vania; Duarte, M. Teresa; Teixeira, Antonio P. S.. The article conveys some information:

Novel pyrazolo[3,4-b]quinoline α-ketophosphonic and hydroxymethylenebisphosphonic acid compounds were synthesized using different methodologies, starting from 2-chloro-3-formylquinoline 1. New phosphonic acid compounds were obtained as N-1 derivatives with a side chain with 1 or 3 (n = 1 or 3) methylene groups. All phosphonic acid compounds and their corresponding ester and carboxylic acid precursors were fully characterized, and their structures elucidated by spectroscopic data, using NMR techniques and IR and high-resolution mass spectroscopy. During the process to obtain the N-1 substituted derivative with two methylene groups (n = 2) in the side chain, an unexpected addition-cyclization cascade reaction was observed, involving the phosphonylation of an aromatic ring and the formation of a new six-member lactam ring to afford a tetracyclic ring system. This was an unexpected result since other pyrazolo[3,4-b]quinoline derivatives and all corresponding pyrazolo[3,4-b]pyridine derivatives already prepared, under similar exptl. conditions, did not undergo this reaction. This domino reaction occurs with different phosphite reagents but only affords the six-member ring. The spectroscopic data allowed the identification of the new synthesized tetracyclic compounds and the x-ray diffraction data of compound 11 enabled the confirmation of the proposed structures. The results came from multiple reactions, including the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Related Products of 539-74-2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. In contrast, terrestrial plants account only for a few bromine-containing compounds.Related Products of 539-74-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhai, Shiyang; Zhang, Huimin; Chen, Rui; Wu, Jiangxia; Ai, Daiqiao; Tao, Shunming; Cai, Yike; Zhang, Ji-Quan; Wang, Ling published an article in 2021. The article was titled 《Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma》, and you may find the article in European Journal of Medicinal Chemistry.Synthetic Route of C5H9BrO2 The information in the text is summarized as follows:

Hepatocellular carcinoma (HCC) is a major contributor to global cancer incidence and mortality. Many pathways are involved in the development of HCC and various proteins including mTOR and HDACs have been identified as potential drug targets for HCC treatment. In the present study, two series of novel hybrid mols. targeting mTOR and HDACs were designed and synthesized based on parent inhibitors (MLN0128 and PP121 for mTOR, SAHA for HDACs) by using a fusion-type mol. hybridization strategy. In vitro antiproliferative assays demonstrated that these novel hybrids with suitable linker lengths exhibited broad cytotoxicity against various cancer cell lines, with significant activity against HepG2 cells. Notably, DI06, an MLN0128-based hybrid, exhibited antiproliferative activity against HepG2 cells with an IC50 value of 1.61μM, which was comparable to those of both parent drugs (MLN0128, IC50 = 2.13μM and SAHA, IC50 = 2.26μM). In vitro enzyme inhibition assays indicated that DI06, DI07 and DI17 (PP121-based hybrid) exhibited nanomolar inhibitory activity against mTOR kinase and HDACs (e.g., HDAC1, HDAC2, HDAC3, HADC6 and HADC8). Cellular studies and western blot analyses uncovered that in HepG2 cells, DI06 and DI17 induced cell apoptosis by targeting mTOR and HDACs, blocked the cell cycle at the G0/G1 phase and suppressed cell migration. The potential binding modes of the hybrids (DI06 and DI17) with mTOR and HDACs were investigated by mol. docking. DI06 displayed better stability in rat liver microsomes than DI07 and DI17. Collectively, DI06 as a novel mTOR and HDACs inhibitor presented here warrants further investigation as a potential treatment of HCC. In the experiment, the researchers used Ethyl 3-bromopropanoate(cas: 539-74-2Synthetic Route of C5H9BrO2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Due to the reactivity of bromide, they are used as potential precursors or important intermediates in organic synthesis. Synthetic Route of C5H9BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Iwami, Hikaru; Okamura, Masaya; Kondo, Mio; Masaoka, Shigeyuki published their research in Angewandte Chemie, International Edition in 2021. The article was titled 《Electrochemical Polymerization Provides a Function-Integrated System for Water Oxidation》.Electric Literature of C5H9BrO2 The article contains the following contents:

Water oxidation is a key reaction in natural and artificial photosynthesis. In nature, the reaction is efficiently catalyzed by a metal-complex-based catalyst surrounded by hole-transporting amino acid residues. However, in artificial systems, there is no example of a water oxidation system that has a catalytic center surrounded by hole transporters. Herein, we present a facile strategy to integrate catalytic centers and hole transporters in one system. Electrochem. polymerization of a metal-complex-based precursor afforded a polymer-based material (Poly-1). Poly-1 exhibited excellent hole-transporting ability and catalyzed water oxidation with high performance. It was also revealed that the catalytic activity was almost completely suppressed in the absence of the hole-transporting moieties. The present study provides a novel strategy for constructing efficient mol.-based systems for water oxidation In the part of experimental materials, we found many familiar compounds, such as Ethyl 3-bromopropanoate(cas: 539-74-2Electric Literature of C5H9BrO2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals.Electric Literature of C5H9BrO2 The most pervasive is the naturally produced bromomethane.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Quality Control of Ethyl 3-bromopropanoateIn 2021 ,《Discovery of a cryptic site at the interface 2 of TEAD – Towards a new family of YAP/TAZ-TEAD inhibitors》 appeared in European Journal of Medicinal Chemistry. The author of the article were Sturbaut, Manon; Bailly, Fabrice; Coevoet, Mathilde; Sileo, Pasquale; Pugniere, Martine; Liberelle, Maxime; Magnez, Romain; Thuru, Xavier; Chartier-Harlin, Marie-Christine; Melnyk, Patricia; Gelin, Muriel; Allemand, Frederic; Guichou, Jean-Francois; Cotelle, Philippe. The article conveys some information:

The Hippo pathway is involved in organ size control and tissue homeostasis by regulating cell growth, proliferation and apoptosis. It controls the phosphorylation of the transcription co-activator YAP (Yes associated protein) and TAZ (Transcriptional coactivator with PDZ-binding motif) in order to control their nuclear import and their interaction with TEAD (Transcriptional Enhanced Associated Domain). YAP, TAZ and TEADs are dysregulated in several cancers making YAP/TAZ-TEAD interaction a new emerging anti-cancer target. We report the synthesis of a set of trisubstituted pyrazoles which bind to hTEAD2 at the interface 2 revealing for the first time a cryptic pocket created by the movement of the phenol ring of Y382. Compound I disrupts YAP/TAZ-TEAD interaction in HEK293T cells and inhibits TEAD target genes and cell proliferation in MDA-MB-231 cells. Compound I is therefore the first inhibitor of YAP/TAZ-TEAD targeting interface 2. This mol. could serve with other pan-TEAD inhibitors such as interface 3 ligands, for the delineation of the relative importance of VGLL vs YAP/TAZ in a given cellular model. The results came from multiple reactions, including the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Quality Control of Ethyl 3-bromopropanoate)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Quality Control of Ethyl 3-bromopropanoate Due to the reactivity of bromide, they are used as potential precursors or important intermediates in organic synthesis.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2022,Galster, Florian; Postges, Timo; Hanekamp, Walburga; Lehr, Matthias published an article in Archiv der Pharmazie (Weinheim, Germany). The title of the article was 《ω-(5-Phenyl-2H-tetrazol-2-yl)alkyl-substituted hydrazides and related compounds as inhibitors of amine oxidase copper containing 3 (AOC3)》.Synthetic Route of C5H9BrO2 The author mentioned the following in the article:

Recently, 6-(5-phenyl-2H-tetrazol-2-yl)hexan-1-amine was found to be a tight-binding substrate of AOC3. To obtain novel inhibitors of the enzyme, the amino group of this substrate was replaced with functional groups that occur in known AOC3 inhibitors, such as hydrazide or glycine amide moieties. In addition, derivatives of the compounds I [R = NHNH2, OEt, NH(CH2)2NH2, NH(CH2)3NH2, 3-(tert-butoxycarbonylamino)propylamino; n = 1, 2, 5, 6, etc.], II [R2 = HNC(O)CH2NH2, HNC(O)OPh, 2-(aminomethyl)imidazol-1-yl, etc.] obtained in this way were prepared The obtained hydrazide I [R = NHNH2; n = 6] which proved to be the most effective, was subjected to further structural modifications. Selected hydrazides I [R = NHNH2; n = 1, 6] were evaluated for selectivity toward some other amine oxidases. The results came from multiple reactions, including the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Synthetic Route of C5H9BrO2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds. 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. Synthetic Route of C5H9BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Bhukya, Balakishan; Kaushal, Tanu; Kumar, Deepak; Singh, Diksha; Parveen, Shahnaz; Khan, Sana; Luqman, Suaib; Konwar, Rituraj; Chanda, Debabrata; Khan, Feroz; Kumar, Shailesh; Meena, Abha; Negi, Arvind S. published their research in Indian Journal of Heterocyclic Chemistry in 2021. The article was titled 《Antiproliferative activity of diarylnaphthofurans through microtubule destabilization》.Quality Control of Ethyl 3-bromopropanoate The article contains the following contents:

The present communication deals with pharmacophore designing based on ”Fragment-Based Drug Discovery” approach. Two series of compounds diaryl naphthofurans I (R = (3-nitrophenyl)carbonyl, 4-fluorophenyl, 5-formylfuran-2-yl, etc.) and II (R1 = H, 2-ethoxy-2-oxoethyl, 3-ethoxy-3-oxopropyl, 4-ethoxy-4-oxobut-2-en-1-yl, etc.) were synthesized and evaluated against human cancer cell lines by sulforhodamine assay, target studies through tubulin kinetics, in silico predictions of binding pocket, and drugability and safety studies by acute oral toxicity in mice model. Out of 24 varied analogs, seven compounds exhibited significant antiproliferative activity against both hormone-dependent and hormone-independent breast cancer cell lines. Among these, two of the most active representative compounds I (R = 3-carboxyphenyl) and II (R1 = H) showed potential antiproliferative activity against MDA-MB-231 with IC50 at 10.04μM and 10.70μM and significant anti-tubulin effect at their half IC50 and IC50. In mol. docking studies, both the compounds occupied colchicine binding pocket at β-tubulin with high binding energies of -8.3 Kcal/mol and -7.9 Kcal/mol, resp. Both the identified investigational leads were found to be safe and non-toxic in rodent model up to 1000 mg/kg oral dose. Optimization of these lead compounds may yield some better candidates in future. In the experimental materials used by the author, we found Ethyl 3-bromopropanoate(cas: 539-74-2Quality Control of Ethyl 3-bromopropanoate)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. In contrast, terrestrial plants account only for a few bromine-containing compounds.Quality Control of Ethyl 3-bromopropanoate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary