Tag: 200-300

Photochromic dihetarylethenes 3. Synthesis and photochromic properties of 1,2-bis[2-methyl-5-(benzoxazol-2-yl)thien-3-yl]hexafluorocyclopentene was written by Krayushkin, M. M.;Stoyanovich, F. M.;Zolotarskaya, O. Yu.;Martynkin, A. Yu.;Ivanov, V. L.;Uzhinov, B. M.. And the article was included in Russian Chemical Bulletin (Translation of Izvestiya Akademii Nauk, Seriya Khimicheskaya) in 1999.Application of 29421-99-6 This article mentions the following:

The title compound, i.e., 2,2′-[(3,3,4,4,5,5-hexafluoro-1-cyclopentene-1,2-diyl)di-(2-methyl-3,5-thiophenediyl)]bis[benzoxazole] was prepared and its photochromic properties were studied. The compound thus prepared did not exhibit fluorescent properties in either open or cyclic form. In the experiment, the researchers used many compounds, for example, 4-Bromo-5-methylthiophene-2-carboxylic acid (cas: 29421-99-6Application of 29421-99-6).

4-Bromo-5-methylthiophene-2-carboxylic acid (cas: 29421-99-6) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.Application of 29421-99-6

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Thiazolidinedione “Magic Bullets” Simultaneously Targeting PPAR绾?and HDACs: Design, Synthesis, and Investigations of their In Vitro and In Vivo Antitumor Effects was written by Tilekar, Kalpana;Hess, Jessica D.;Upadhyay, Neha;Bianco, Alessandra Lo;Schweipert, Markus;Laghezza, Antonio;Loiodice, Fulvio;Meyer-Almes, Franz-Josef;Aguilera, Renato J.;Lavecchia, Antonio;C S, Ramaa. And the article was included in Journal of Medicinal Chemistry in 2021.Recommanded Product: 615-55-4 This article mentions the following:

Monotargeting anticancer agents suffer from resistance and target nonspecificity concerns, which can be tackled with a multitargeting approach. The combined treatment with HDAC inhibitors and PPAR绾?agonists has displayed potential antitumor effects. Based on these observations, this work involves design and synthesis of mols. I (Ar = Ph, pyridin-2-yl, benzo[d]thiazol-2-yl, etc.) that can simultaneously target PPAR绾?and HDAC. Several out of 25 compounds inhibited HDAC4, and six compounds acted as dual-targeting agents. Compound I (Ar = 2-bromo-4,6-difluorophenyl) was the most potent, with activity toward PPAR绾?EC₅₀ = 0.245娓璏 and HDAC4 IC₅₀ = 1.1娓璏. Addnl., compounds I (Ar = 4-methylphenyl, 2-bromo-4,6-difluorophenyl) were cytotoxic to CCRF-CEM cells (CC₅₀ = 2.8 and 9.6娓璏, resp.), induced apoptosis, and caused DNA fragmentation. Furthermore, compound I (Ar = 4-methylphenyl) modulated the expression of c-Myc, cleaved caspase-3, and caused in vivo tumor regression in CCRF-CEM tumor xenografts. Thus, this study provides a basis for the rational design of dual/multitargeting agents that could be developed further as anticancer therapeutics. In the experiment, the researchers used many compounds, for example, 3,4-Dibromoaniline (cas: 615-55-4Recommanded Product: 615-55-4).

3,4-Dibromoaniline (cas: 615-55-4) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. 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: 615-55-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design of novel carbamate acetylcholinesterase inhibitors based on the multiple sites of acetylcholinesterase was written by Zhao, Qianfei;Yang, Guoquan;Mei, Xiangdong;Yuan, Huizhu;Ning, Jun. And the article was included in Journal of Pesticide Science (Tokyo, Japan) in 2008.Quality Control of N-(5-Bromopentyl)phthalimide This article mentions the following:

This work describes the design, synthesis, AChE inhibitory activity, and structure-activity relationship of compounds related to a recently discovered series of AChE inhibitors: phthalimide alkyloxyphenyl N-methylcarbamates. The influence of structural variations on inhibitory potency was carefully investigated by modifying different alkyloxy chain lengths and positions between phthalimide and Ph N-methylcarbamate. The biol. properties of the series were investigated in some detail by considering their activity on isolated enzymes. All of the newly synthesized derivatives, when tested on isolated AChE from the brain of the housefly (Musca domestica), were more active than Ph N-methylcarbamate. In particular, compound I1 displayed the best AChE inhibition (352-fold higher than Ph N-methylcarbamate, and 29-fold higher than metolcarb), which suggested that the phthalimide group of I1 bound strongly to the residues lining the gorge, and Ph N-methylcarbamate bound at the catalytic sites. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Quality Control of N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Quality Control of N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells was written by Valente, Sergio;Lepore, Ilaria;Dell’Aversana, Carmela;Tardugno, Maria;Castellano, Sabrina;Sbardella, Gianluca;Tomassi, Stefano;Di Maro, Salvatore;Novellino, Ettore;Di Santo, Roberto;Costi, Roberta;Altucci, Lucia;Mai, Antonello. And the article was included in Biochimie in 2012.Related Products of 108940-96-1 This article mentions the following:

Chem. manipulations undertaken on some bis(bromo- and dibromo-phenol) compounds previously reported by us as wide-spectrum epigenetic inhibitors let us to identify bis (bromo- and dibromo-methoxyphenyl) derivatives highly selective for PR-SET7 and EZH2 (compounds 4, 5, 9, and 10). Western blot analyses were carried out in U937 cells to determine the effects of such compounds on the Me marks related to the tested enzymes (H3K4me1, H3K9me2, H4H20me1, and H3K27me3). The 1,5-bis(3-bromo-4-methoxyphenyl)penta-1,4-dien-3-one 4 (EC₅₀ vs EZH2 = 74.9 娓璏), tested in U937 cells at 50 娓璏, induced massive cell death and 28% of granulocytic differentiation, highlighting the potential use of EZH2 inhibitors in cancer. In the experiment, the researchers used many compounds, for example, 3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1Related Products of 108940-96-1).

3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Related Products of 108940-96-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis of Substituted 6-Anilinouracils and Their Inhibition of DNA Polymerase IIIC and Gram-Positive Bacterial Growth was written by Zhi, Chengxin;Long, Zheng-Yu;Gambino, Joseph;Xu, Wei-Chu;Brown, Neal C.;Barnes, Marjorie;Butler, Michelle;LaMarr, William;Wright, George E.. And the article was included in Journal of Medicinal Chemistry in 2003.Related Products of 615-55-4 This article mentions the following:

Certain substituted 6-anilinouracils are potent and selective inhibitors of Gram+ bacterial DNA polymerase IIIC (pol IIIC). In addition, analogs with 3-substituents in the uracil ring have potent antibacterial activity against Gram+ organisms in culture. In an attempt to find optimal anilino substituents for pol IIIC binding and optimal 3-substituents for antibacterial activity, several series of 3-substituted-6-aminouracils were prepared and assayed their activity against pol IIIC from Bacillus subtilis and a panel of Gram+ and Gram- bacteria in culture. The 6-(3-ethyl-4-methylanilino) group and closely related substituent patterns maximized pol IIIC inhibition potency. Among a series of 3-(substituted-butyl)-6-(3-ethyl-4-methylanilino)uracils, basic amino substituents increased pol IIIC inhibition, but decreased antibacterial activity. The most potent antibacterials were simple hydroxybutyl and methoxybutyl derivatives, and hydrophobically substituted piperidinylbutyl derivatives In the experiment, the researchers used many compounds, for example, 3,4-Dibromoaniline (cas: 615-55-4Related Products of 615-55-4).

3,4-Dibromoaniline (cas: 615-55-4) 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. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Related Products of 615-55-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Binding Mode and Potency of N-Indolyloxopyridinyl-4-aminopropanyl-Based Inhibitors Targeting Trypanosoma cruzi CYP51 was written by Vieira, Debora F.;Choi, Jun Yong;Calvet, Claudia M.;Siqueira-Neto, Jair Lage;Johnston, Jonathan B.;Kellar, Danielle;Gut, Jiri;Cameron, Michael D.;McKerrow, James H.;Roush, William R.;Podust, Larissa M.. And the article was included in Journal of Medicinal Chemistry in 2014.Computed Properties of C8H6BrFO2 This article mentions the following:

Chagas disease is a chronic infection in humans caused by Trypanosoma cruzi and manifested in progressive cardiomyopathy and/or gastrointestinal dysfunction. Limited therapeutic options to prevent and treat Chagas disease put 8 million people infected with T. cruzi worldwide at risk. CYP51, involved in the biosynthesis of the membrane sterol component in eukaryotes, is a promising drug target in T. cruzi. We report the structure-activity relationships (SAR) of an N-arylpiperazine series of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors designed to probe the impact of substituents in the terminal N-Ph ring on binding mode, selectivity and potency. Depending on the substituents at C-4, two distinct ring binding modes, buried and solvent-exposed, have been observed by X-ray structure anal. (resolution of 1.95-2.48 鑴?. The 5-chloro-substituted analogs 9 and 10 with no substituent at C-4 demonstrated improved selectivity and potency, suppressing 閳?9.8% parasitemia in mice when administered orally at 25 mg/kg, b.i.d., for 4 days. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2Computed Properties of C8H6BrFO2).

Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon鑱砨romine bond is electrophilic in nature. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Computed Properties of C8H6BrFO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design, synthesis and antibacterial activity of novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain was written by Song, Qiu-Ling;Guo, Bao-Qin;Zhang, Wen;Lan, Ping;Sun, Ping-Hua;Chen, Wei-Min. And the article was included in Journal of Antibiotics in 2011.Application of 954-81-4 This article mentions the following:

A set of 17 novel ketolides bearing an aryltetrazolyl-substituted alkyl side chain were synthesized and evaluated for their antibacterial activities, which the aryltetrazolyl group was selected to replace the hetero-aryl moiety of the side chain in telithromycin for designing new compounds The synthesis of aryltetrazolyl alkylamines was reported in detail. The antibacterial activities of new ketolides were evaluated against a number of pathogens including macrolide-resistant organisms by using telithromycin as the reference Many of the evaluated compounds exhibited remarkable activities against both erythromycin-susceptible and erythromycin-resistant organisms such as Staphylococcus aureus (except S. aureus AD-08), Pseudomonas aeruginosa and Escherichia coli. Among these, the compound 11e exhibited excellent antibacterial potency against all the strains in comparison with others. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Application of 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Application of 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

An improved total synthesis of spermatinamine, an inhibitor of isoprenylcysteine carboxy methyltransferase was written by Ullah, Nisar;Haladu, Shamsuddeen A.;Mosa, Basem A.. And the article was included in Tetrahedron Letters in 2011.Name: 3,5-Dibromo-4-methoxybenzaldehyde This article mentions the following:

An improved total synthesis of spermatinamine (I), an inhibitor of the anticancer target isoprenylcysteine carboxy methyltransferase (no biol. testing data presented), was accomplished starting from the com. available 3,4-dibromo-4-hydroxybenzaldehyde via a high yielding reaction sequence in an overall yield of 31%. In the experiment, the researchers used many compounds, for example, 3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1Name: 3,5-Dibromo-4-methoxybenzaldehyde).

3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. 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.Name: 3,5-Dibromo-4-methoxybenzaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Fries reaction of m-halophenylacetate was written by Chen, F.-C.;Chang, K. T.. And the article was included in Taiwan Yaoxue Zazhi in 1952.Category: bromides-buliding-blocks This article mentions the following:

m-BrC₆H₄OAc (I) (10 g.) heated with 20 g. AlCl₃ (II), 2 hrs. at 80鎺? followed by steam distillation, gave 3 g. yellow crystals (III), m. 42-3鎺? and 0.4 g. yellow crystals (IV), m. 85-90鎺? from the distillate and the residue, resp. I (10 g.) treated with 18 g. II, 1 hr. at 45鎺? gave 1 g. IV. Assuming that the o-isomer predominates at elevated temperature, III and IV are apparently 4-bromo-2-hydroxy- and 2-bromo-4-hydroxyacetophenones, resp. III with BzH gave a chalcone (V), yellow needles, m. 115-16鎺? cyclization of V with H₃PO₄ gave a flavanone (VI), m. 77-8鎺? dehydrogenation of VI with N-bromosuccinimide gave a flavone, m. 162-3鎺? Heating 7 g. m-IC₆H₄OAc (VII) in 35 ml. PhNO₂ (VIII) with 20 g. II 4 hrs. at 90-5鎺? followed by steam distillation, gave 0.1 g. crystals (IX), m. 53-4鎺? and 0.1 g. crystals (X), m. 128-36鎺? from the distillate and the residue, resp. VII (5 g.) in 25 ml. VIII heated with 17 g. II 3 hrs. at 100-120鎺?gave 0.15 g. IX. IX and X are apparently 2-hydroxy-4-iodo- and 4-hydroxy-2-iodoacetophenones, resp. In the experiment, the researchers used many compounds, for example, 3-Bromophenyl acetate (cas: 35065-86-2Category: bromides-buliding-blocks).

3-Bromophenyl acetate (cas: 35065-86-2) 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. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis and Bioevaluation of Novel [¹⁸F]FDG-Conjugated 2-Nitroimidazole Derivatives for Tumor Hypoxia Imaging was written by Yang, Xianteng;Wang, Fan;Zhu, Hua;Yang, Zhi;Chu, Taiwei. And the article was included in Molecular Pharmaceutics in 2019.Product Details of 954-81-4 This article mentions the following:

Hypoxia imaging can guide tumor treatment and monitor changes in hypoxia during treatment. However, there is still no ideal hypoxia imaging agent for clin. applications. In this study, two novel 2-nitromidazole derivatives were synthesized and directly radiolabeled by [¹⁸F]FDG in high radiochem. yield and excellent radiochem. purity. Cell experiments, biodistribution, and positron emission tomog. (PET) imaging studies were also conducted in mice-bearing S180 or OS732 tumors. [¹⁸F]FDG-2NNC2ON [(2R,3S,4R,E)-2-¹⁸F-fluoro-3,4,5,6-tetrahydroxyhexanal O-3-(2-(2-nitro-1H-imidazole-1-yl)ethylamino)-2-oxopropyl oxime] and [¹⁸F]FDG-2NNC5ON [(2R,3S,4R,E)-2-¹⁸F-fluoro-3,4,5,6-tetrahydroxyhexanal-O-3-(5-(2-nitro-1H-imidazole-1-yl)pentylamino)-2-oxopropyl oxime] can be cleared from the blood quickly and specifically target hypoxic tumor cells. The uptake of the probes by hypoxic cells gradually increases with time. After 4 h, the uptake value of [¹⁸F]FDG-2NNC2ON in hypoxic cells is 3.2 times higher than that in normoxia cells. In contrast, there is no difference in the uptake of [¹⁸F]FDG between hypoxic cells and normoxia cells. Biodistribution resulting from two tumor models indicate that the uptake values of the two radiotracers in the tumor are higher at 1 h than those at 2 and 4 h. At 1 and 2 h, the tumors are clearly observed on the PET images and the imaging features of [¹⁸F]FDG-2NNC5ON and [¹⁸F]FDG-2NNC2ON are distinct from those of [¹⁸F]FDG. Compared with [¹⁸F]FDG-2NNC5ON, [¹⁸F]FDG-2NNC2ON has a higher proportion of renal excretion, lower digestive tract uptake, and better imaging contrast because of its higher hydrophilicity. At 2 h, [¹⁸F]FDG-2NNC2ON shows a good tumor-to-blood (T/B) ratio, tumor-to-muscle ratio based on biodistribution (Bio-T/M ratio), and tumor-to-muscle ratio based on regions of interest on the PET images [region of interest (ROI)-T/M ratio] in the two tumor models (T/B, Bio-T/M, and ROI-T/M ratios are 3.2, 2.6, and 3.9 in the S180 tumor model and are 3.4, 4.2, and 4.6 in the OS732 tumor model, resp.). The imaging features visualized with autoradiog. mostly coincided with the pos. areas of HIF1浼?staining by immunofluorescence. Meanwhile, the biodistribution study and PET imaging revealed that the uptake of the radiotracers in the tumor cannot be competed by 5% glucose, confirming that [¹⁸F]FDG-2NNC2ON targets the hypoxic regions of the tumors instead of targeting tumors through the glucose metabolism pathway. These results suggest that the new 2-nitroimidazole derivative conjugated with [¹⁸F]FDG, [¹⁸F]FDG-2NNC2ON, has potential as an imaging agent for hypoxia. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Product Details of 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Product Details of 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary