Tag: 200-300

Synthesis and biological evaluation of sulforaphane derivatives as potential antitumor agents was written by Hu, Kun;Qi, Yan-jie;Zhao, Juan;Jiang, He-fei;Chen, Xin;Ren, Jie. And the article was included in European Journal of Medicinal Chemistry in 2013.Safety of N-(5-Bromopentyl)phthalimide This article mentions the following:

A series of sulforaphane derivatives, S:C:NCH₂(CH₂)_nCH₂X(O)R [I, R = PhCH₂, Et, 2-furanylmethyl, cyclopentyl, etc., X = S(O), n = 1-4; R = PhCH₂, X = S, n = 2; R = PhCH₂, X = SO₂, n = 2], were synthesized and evaluated in vitro for their cytotoxicity against five cancer cell lines (HepG2, A549, MCF-7, HCT-116 and SH-SY5Y). The pharmacol. results showed that many of the derivatives displayed more potent cytotoxicity than sulforaphane (SFN). Furthermore, SFN and derivative I [R = PhCH₂, X = S(O), n = 2] (II) could induce cell cycle arrest at S or G2/M phase and cell apoptosis. SFN and II exhibited time- and dose-dependent activation on Nrf2 transcription factor, and II acted as a more potent Nrf2 inducer than SFN. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Safety of N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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–bromine bond is electrophilic in nature. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Safety of N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

An Intermolecular Hydroarylation of Highly Deactivated Styrenes Catalyzed by Re₂O₇/HReO₄ in Hexafluoroisopropanol was written by Hu, Liqun;Liu, Yibing;Fang, Xiong;zheng, Yuzhu;Liao, Rong-zhen;Li, Man;Xie, Youwei. And the article was included in ACS Catalysis in 2022.Application In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde This article mentions the following:

Here, authors describe an activation mode for unactivated alkenes on the basis of a synergy between Re₂O₇/HReO₄ and hexafluoroisopropanol (HFIP). Highly electron-deficient styrenes have been activated to effect a challenging intermol. hydroarylation with different arenes to give a variety of diarylalkanes in high efficiency. This method is characterized by mild reaction condition, broad substrate scope, high chem. yields, and minimal waste generation. The potential synthetic application of this methodol. was exemplified by the efficient synthesis of a retinoic acid receptor (RAR) agonist. DFT calculations and deuterium-labeling experiments were conducted to elucidate the reaction mechanism, and both confirmed the critical role of HFIP, which significantly reduced the energetical barriers for several key steps of this transformation via a network of hydrogen bonding to perrhenate anion with two equivalent of HFIP. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7Application In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde).

2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7) 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. 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 In Synthesis of 2-Bromo-4-(trifluoromethyl)benzaldehyde

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Chemo-proteomics exploration of HDAC degradability by small molecule degraders was written by Xiong, Yuan;Donovan, Katherine A.;Eleuteri, Nicholas A.;Kirmani, Nadia;Yue, Hong;Razov, Anthony;Krupnick, Noah M.;Nowak, Radoslaw P.;Fischer, Eric S.. And the article was included in Cell Chemical Biology in 2021.Quality Control of N-(5-Bromopentyl)phthalimide This article mentions the following:

Targeted protein degradation refers to the use of small mols. that recruit a ubiquitin ligase to a target protein for ubiquitination and subsequent proteasome-dependent degradation While degraders have been developed for many targets, key questions regarding degrader development and the consequences of acute pharmacol. degradation remain, specifically for targets that exist in obligate multi-protein complexes. Here, we synthesize a pan-histone deacetylase (HDAC) degrader library for the chemo-proteomic exploration of acute degradation of a key class of chromatin-modifying enzymes. Using chemo-proteomics, we not only map the degradability of the zinc-dependent HDAC family identifying leads for targeting HDACs 1-8 and 10 but also explore important aspects of degrading epigenetic enzymes. We discover cell line-driven target specificity and that HDAC degradation often results in collateral loss of HDAC-containing repressive complexes. These findings potentially offer a new mechanism toward controlling chromatin structure, and our resource will facilitate accelerated degrader design and development for HDACs. 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. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Quality Control of N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Optimization of Phenyl-Substituted Benzimidazole Carboxamide Poly(ADP-Ribose) Polymerase Inhibitors: Identification of (S)-2-(2-Fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a Highly Potent and Efficacious Inhibitor was written by Penning, Thomas D.;Zhu, Gui-Dong;Gong, Jianchun;Thomas, Sheela;Gandhi, Viraj B.;Liu, Xuesong;Shi, Yan;Klinghofer, Vered;Johnson, Eric F.;Park, Chang H.;Fry, Elizabeth H.;Donawho, Cherrie K.;Frost, David J.;Buchanan, Fritz G.;Bukofzer, Gail T.;Rodriguez, Luis E.;Bontcheva-Diaz, Velitchka;Bouska, Jennifer J.;Osterling, Donald J.;Olson, Amanda M.;Marsh, Kennan C.;Luo, Yan;Giranda, Vincent L.. And the article was included in Journal of Medicinal Chemistry in 2010.Product Details of 179232-29-2 This article mentions the following:

We have developed a series of phenylpyrrolidine- and phenylpiperidine-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase (PARP) inhibitors with excellent PARP enzyme potency as well as single-digit nanomolar cellular potency. These efforts led to the identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (22b, A-966492) (I). Compound 22b displayed excellent potency against the PARP-1 enzyme with a K_i of 1 nM and an EC₅₀ of 1 nM in a whole cell assay. In addition, 22b is orally bioavailable across multiple species, crosses the blood-brain barrier, and appears to distribute into tumor tissue. It also demonstrated good in vivo efficacy in a B16F10 s.c. murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2Product Details of 179232-29-2).

Methyl 4-bromo-2-fluorobenzoate (cas: 179232-29-2) 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. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Product Details of 179232-29-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Design and Synthesis of [(2,3-Dichlorophenyl)piperazin-1-yl]alkylfluorenylcarboxamides as Novel Ligands Selective for the Dopamine D₃ Receptor Subtype was written by Robarge, Michael J.;Husbands, Stephen M.;Kieltyka, Andrzej;Brodbeck, Robbin;Thurkauf, Andrew;Newman, Amy Hauck. And the article was included in Journal of Medicinal Chemistry in 2001.HPLC of Formula: 954-81-4 This article mentions the following:

The dopamine D₃ receptor subtype has been recently targeted as a potential neurochem. modulator of the behavioral actions of psychomotor stimulants, such as cocaine. However, definitive behavioral investigations have been hampered by the lack of highly selective D₃ agonists and antagonists. In an attempt to design a novel class of D₃ ligands with which to study this receptor system, a series of chem. divergent compounds that possessed various structural features that exist within several classes of reputed D₃ agents was screened and compared to the recently reported NGB 2904. On the basis of these results, a novel series of compounds was designed that included functional moieties that were required for high-affinity and selective binding to D₃ receptors. All the compounds in this series included an aryl-substituted piperazine ring, a varying alkyl chain linker (C₃-C₅), and a terminal aryl amide. The compounds were synthesized and evaluated in vitro for binding in CHO cells transfected with human D₂, D₃, or D₄ receptor cDNAs. D₃ binding affinities ranged from K_i = 1.4 to 1460 nM. The most potent analog in this series, I, demonstrated a D₃/D₂ selectivity of 64 and a D₃/D₄ selectivity of 1300. Structure-activity relationships for this class of ligands at D₃ receptors will provide new leads toward the development of highly selective and potent mol. probes that will prove useful in the elucidation of the role D₃ receptors play in the psychomotor stimulant and reinforcing properties of cocaine. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4HPLC of Formula: 954-81-4).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. 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. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.HPLC of Formula: 954-81-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Synthesis of aryl sulfonyl fluorides from aryl sulfonyl chlorides using sulfuryl fluoride (SO₂F₂) as fluoride provider was written by Song, Xuyan;He, Yunlu;Wang, Bo;Peng, Sanwen;Pan, Xi;Wei, Min;Liu, Qiang;Qin, Hua-Li;Tang, Haolin. And the article was included in Tetrahedron in 2022.Product Details of 454-65-9 This article mentions the following:

A highly efficient method for the synthesis of aryl sulfonyl fluorides ArSO₂F [Ar = 4-MeC₆H₄, 4-PhC₆H₄, 4-ClC₆H₄, etc.] was developed from aryl sulfonyl chlorides using SO₂F₂ as fluoride source in up to 98% isolated yield under mild conditions. Gram scale experiments were also conducted, revealing the good practicality of this new protocol. In the experiment, the researchers used many compounds, for example, 3-Bromobenzene-1-sulfonyl fluoride (cas: 454-65-9Product Details of 454-65-9).

3-Bromobenzene-1-sulfonyl fluoride (cas: 454-65-9) 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. 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.Product Details of 454-65-9

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Isomeric thermally activated delayed fluorescence emitters based on a quinolino[3,2,1-de]acridine-5,9-dione multiple resonance core and carbazole substituent was written by Liu, Jing-Feng;Zou, Sheng-Nan;Chen, Xing;Yang, Sheng-Yi;Yu, You-Jun;Fung, Man-Keung;Jiang, Zuo-Quan;Liao, Liang-Sheng. And the article was included in Materials Chemistry Frontiers in 2022.Related Products of 100189-84-2 This article mentions the following:

The color purity of the pixels is an essential indicator in organic light-emitting diode (OLED) com. displays. Since the two important parameters of high color purity and efficiency can be achieved simultaneously, multiple resonance thermally activated delayed fluorescence (MR-TADF) emitters have achieved rapid development. Recently, there has been a lot of research work on connecting various donor (D) moieties to the existing MR core, but few studies on how the linking moiety affects the efficiency of MR-TADF emitters. To figure out the influence of substituents on the MR-TADF system, we developed three isomers QAOCz1, QAOCz2, and QAOCz3, which are constructed with the same moieties of 3,11-diphenylquinolino[3,2,1-de]acridine-5,9-dione and 9-phenyl-9H-carbazole (PhCz) by different site connections. Through reasonable adjustments of the substitution site, the donor-acceptor (D-A) interaction of the isomers gradually weakened and mol. rigidity gradually increased. As a result, their singlet-triplet energy gap (ΔEST) gradually decreased and their photoluminescence quantum yield (PLQY) gradually rose. QAOCz3 with the weakest D-A interaction successfully achieves a much higher PLQY of 98.9% and a smaller ΔEST of 0.16 eV. The QAOCz3 based OLED not only realizes the best maximum external quantum efficiency (EQE) of 21.1% but also has the narrowest full-width at half maximum (FWHM) of 40 nm. This work shows that weakening the D-A interaction between the substituents and the MR core by a spacer group is of great significance for the construction of efficient MR-TADF emitters. In the experiment, the researchers used many compounds, for example, 2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2Related Products of 100189-84-2).

2,5-Dibromo-1,3-dimethylbenzene (cas: 100189-84-2) 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.Related Products of 100189-84-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

N-Phthalimidoalkyl derivatives of 2β-carbomethoxy-3β-(4′-iodophenyl)tropane (β-CIT): brain monoamine transporter affinity was written by Tamagnan, Gilles;Neumeyer, John L.;Gao, Yigong;Wang, Shaoyin;Kula Nora;Baldessarini, Ross J.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 1997.Recommanded Product: N-(5-Bromopentyl)phthalimide This article mentions the following:

A series of novel N-phthalimidoalkyl analogs I (n = 2-5, 8) for the stable phenyltropane β-CIT were synthesized and evaluated by selective radioligand binding assays for affinity to transporters for dopamine (DA), serotonin (5-HT) and norepinephrine (NE) in corpus striatum tissue from rat forebrain. β-CIT and I (n = 4, 5, 8) showed similarly greater affinity at 5-HT than DA transporters; this affinity was lost with I (n = 2, 3). These results are consistent with interference at a critical binding site for the tropane nitrogen on the transporter proteins and indicate that the tropane nitrogen atom can be substituted with large substituted alkyl moieties without loss of affinity or selectivity for amine transporters. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Recommanded Product: N-(5-Bromopentyl)phthalimide).

N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Recommanded Product: N-(5-Bromopentyl)phthalimide

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Intramolecular Direct Arylation of 1,3-Diketone-Derived Enol Ethers in a Synthesis of Tricyclic Oxoisochromene Derivatives was written by Muimhneachain, Eoin O.;Pardo, Leticia M.;Bateman, Lorraine M.;Rao Khandavilli, U. B.;Lawrence, Simon E.;McGlacken, Gerard P.. And the article was included in Advanced Synthesis & Catalysis in 2017.HPLC of Formula: 61150-57-0 This article mentions the following:

A synthesis of tricyclic oxoisochromene derivatives via an intramol. direct arylation of cycloalkyl-1,3-diketone-derived α,β-unsaturated ketone substrates is described. Interesting mechanistic insight has been gathered, based on deuterium migration studies, induced by palladium (Pd). In the experiment, the researchers used many compounds, for example, 2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0HPLC of Formula: 61150-57-0).

2-Bromo-4-fluorobenzylbromide (cas: 61150-57-0) belongs to organobromine compounds. 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. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.HPLC of Formula: 61150-57-0

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa was written by Batt, Douglas G.;Qiao, Jennifer X.;Modi, Dilip P.;Houghton, Gregory C.;Pierson, Deborah A.;Rossi, Karen A.;Luettgen, Joseph M.;Knabb, Robert M.;Jadhav, P. K.;Wexler, Ruth R.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2004.Application of 6515-58-8 This article mentions the following:

Structural features of the 5-amidinoindole inhibitor I of factor Xa, which displayed modest inhibition of factor IXa were varied to increase potency and improve selectivity for factor IXa. Several analogs of I with greatly diminished factor Xa selectivity were prepared and the structural features favorable for factor IXa activity were identified. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Application of 6515-58-8).

3-(Bromomethyl)benzoic acid (cas: 6515-58-8) 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–bromine bond is electrophilic in nature. 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 6515-58-8

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary