Category: 574-98-1

On December 29, 2021, Kang, Kai; Loud, Nathan L.; DiBenedetto, Tarah A.; Weix, Daniel J. published an article.SDS of cas: 574-98-1 The title of the article was A General, Multimetallic Cross-Ullmann Biheteroaryl Synthesis from Heteroaryl Halides and Heteroaryl Triflates. And the article contained the following:

A new, general approach to biheteroaryls: the Ni- and Pd-catalyzed multimetallic cross-Ullmann coupling of heteroaryl halides with triflates. An array of 5-membered, 6-membered and fused heteroaryl bromides and chlorides, as well as aryl triflates derived from heterocyclic phenols proved to be viable substrates in this reaction (62 examples, 63 ± 17% average yield). The generality of this approach to biheteroaryls were further demonstrated in 96-well plate format at 10μmol scale. An array of 96 possible products provided >90% hit rate under a single set of conditions. Further, low-yielding combinations was rapidly optimized with a single “Toolbox Plate” of ligands, additives and reductants. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1

The Article related to pyridyl trifluoromethanesulfonate heteroaryl halide nickel palladium catalyst ullmann coupling, heteroaryl pyridine preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Wang, Lin; Fang, Zhijie published an article in 2020, the title of the article was Study on the synthesis and biological activities of N-alkylated deoxynojirimycin derivatives with a terminal tertiary amine.Electric Literature of 574-98-1 And the article contains the following content:

A series of N-alkylated deoxynojirimycin (DNJ) derivatives I (n = 1, 3; R = R1 = Me; RR1 = -(CH2)4-, -(CH2)5-, -(CH2)2O(CH2)2-) connected to a terminal tertiary amine at the alkyl chains of various lengths was prepared These novel synthetic compounds I were assessed for preliminary glucosidase inhibition and anticancer activities in vitro. Potent and selective inhibition was observed among them. Compound I (n = 1; RR1 = -(CH2)2O(CH2)2-) II (IC50 = 0.052μM) showed improved and selective inhibitory activity against β-glucosidase compared to DNJ (IC50 = 0.65μM). In addition, anal. of the kinetics of enzyme inhibition by using Lineweaver-Burk plots indicated that II inhibited β-glucosidase in a competitive manner, suggesting that II was expected to bind to the active site of β-glucosidase. Compounds I [n = 3; RR1 = -(CH2)4-, -(CH2)5-] were found to be moderate and selective inhibitors of α-glucosidase. Nevertheless, none of compounds inhibited the growth of B16F10 melanoma cells. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Electric Literature of 574-98-1

The Article related to tertiary amine alkyl deoxynojirimycin preparation glucosidase inhibition antitumor activity, Alkaloids: Alkaloids Containing One Nitrogen Atom In A Ring and other aspects.Electric Literature of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zeng, Leli; Ma, Gongcheng; Xu, Han; Mu, Jing; Li, Fan; Gao, Xiaoting; Deng, Zhuoting; Qu, Junle; Huang, Peng; Lin, Jing published an article in 2019, the title of the article was In Vivo Chemoselective Photoacoustic Imaging of Copper(II) in Plant and Animal Subjects.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione And the article contains the following content:

The detection of Cu2+ in living plants and animals is of great importance for environment monitoring and disease diagnosis. Here, a near-IR (NIR) turn-on photoacoustic (PA) probe (denoted as LET-2) is developed for Cu2+ detection in living subjects, such as soybean sprouts and mice. The absorbance band of LET-2 shifts from 625 to 715 nm after the interaction with Cu2+, thus producing strong PA signal output at 715 nm (PA715) as an indicator. The PA715 value is increased as a function of the concentration of Cu2+ (0 × 10-6-20 × 10-6M), with a calculated limit of detection of 10.8 × 10-9M. More importantly, both in vitro and in vivo studies in soybean sprouts and mice indicate that the as-prepared LET-2 PA probe is highly sensitive and selective for Cu2+ detection. These findings provide a solution for in vivo detection of metal ions by using chemoselective PA probes. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to photoacoustic imaging copper plant animal, animals, copper detection, in vivo, photoacoustic imaging, plants, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Application In Synthesis of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On December 15, 2021, 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 published an article.Category: bromides-buliding-blocks The title of the article was Discovery of a cryptic site at the interface 2 of TEAD – Towards a new family of YAP/TAZ-TEAD inhibitors. And the article contained the following:

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 experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Category: bromides-buliding-blocks

The Article related to pyrazole preparation tead2 inhibitor structure activity relationship, binding assays, hippo pathway, interface 2, tead cryptic binding pocket, tead inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 15, 2020, Sandfort, Frederik; Knecht, Tobias; Pinkert, Tobias; Daniliuc, Constantin G.; Glorius, Frank published an article.Name: 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Site-Selective Thiolation of (Multi)halogenated Heteroarenes. And the article contained the following:

A general and simple strategy for the site-selective thiolation of various pharmaceutically relevant electron-rich heteroarenes with thiols is reported. This mild and reliable photocatalytic protocol enables C-S coupling at the most electron-rich position of the (multi)halogenated substrates, complementing established methodologies. Exptl. and computational studies suggest a radical chain mechanism with the key step being a homolytic aromatic substitution of the heteroaryl halide by an electrophilic thiyl radical, highlighting an underdeveloped reactivity mode. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Name: 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to heteroarene thiol site selective thiolation photochem iridium, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Name: 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On January 31, 2020, Zhang, Xinwei; Zhang, Cunlong; Tang, Lin; Lu, Kuan; Zhao, Huan; Wu, Weibin; Jiang, Yuyang published an article.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Synthesis and biological evaluation of piperidyl benzimidazole carboxamide derivatives as potent PARP-1 inhibitors and antitumor agents. And the article contained the following:

A series of compounds based on a piperidyl benzimidazole carboxamide structure and tested their PARP-1 inhibitory activity, as well as cellular inhibitory activity. Some of them showed great potency as PARP-1 inhibitors and antitumor activity, which were valuable for further research. In addition, the predicted ADME properties and proposed binding mode with PARP-1 of the compounds were obtained via computational simulation. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to alkyl amidobenzimidazolyl piperidine preparation parp inhibition antitumor sar pharmacokinetics, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Reference of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 1, 2020, Kubasov, A. S.; Turishev, E. S.; Golubev, A. V.; Bykov, A. Yu.; Zhizhin, K. Yu.; Kuznetsov, N. T. published an article.Synthetic Route of 574-98-1 The title of the article was The method for synthesis of 2-sulfonium closo-decaborate anions derivatives with exo-polyhedral aminogroups. And the article contained the following:

A method for the preparation of sulfonium derivatives of the closo-decaborate anion with the exo-polyhedral amino groups [B10H9S((CH2)nNH2)2]- (n = 1-3) has been developed. The method is based on the alkylation of the [B10H9SH]2- anion with N-bromoalkyl phthalimides and subsequent removal of the phthalimide protection with hydrazine. We could show that the interaction between the [B10H9SH]2- anion with bromomethyl phthalimide groups allowed us to prepare selectively mono-S-substituted sulfanyl derivatives [B10H9SCH2N(CO)2C6H4]2-. Due to the high stability of the sulfonium derivatives of the closo-decaborate anion, it is possible to obtain perchlorinated analogs of these compounds by chlorination of the salts n-Bu4N[B10H9S((CH2)nN(CO)2C6H4)2] (n = 1-3) with sulfuryl chloride in acetonitrile. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Synthetic Route of 574-98-1

The Article related to crystal structure mol sulfonium decaborate anion polyhedral amino preparation, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Synthetic Route of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Lien, Vegard Torp; Kristiansen, Margrethe Konstanse; Pettersen, Solveig; Haugen, Mads Haugland; Olberg, Dag Erlend; Waaler, Jo; Klaveness, Jo published an article in 2019, the title of the article was Towards dual inhibitors of the MET kinase and WNT signaling pathway; design, synthesis and biological evaluation.Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione And the article contains the following content:

Both the kinase MET and the WNT signaling pathway are attractive targets in cancer therapy, and synergistic effects have previously been observed in animal models upon simultaneous inhibition. A strategy towards a designed multiple ligand of MET and WNT signaling is pursued based on the two hetero biaryl systems present in both the MET inhibitor tepotinib and WNT signaling inhibitor TC-E 5001. Initial screening was conducted to find the most suitable ring systems for further optimization, whereas a second screen explored modifications towards pyridazinones and triazolo pyridazines. Up to 54% reduction of WNT signaling activity at 10 microM concentration was achieved, however, only low affinities towards MET were observed Overall, the thiophene substituted pyridazinone 40 was the best dual MET and WNT signaling inhibitor, with a 17% and 19% reduction of activity, resp. Although further optimizations are needed to achieve more potent dual inhibitors, the strategy presented herein can be valuable towards the development of a dual inhibitor of MET and WNT signaling. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to met kinase wnt inhibitor anticancer agent signaling, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Safety of 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Min, Rui; Wu, Weibin; Wang, Mingzhong; Tang, Lin; Chen, Dawei; Zhao, Huan; Zhang, Cunlong; Jiang, Yuyang published an article in 2019, the title of the article was Discovery of 2-(1-(3-(4-chloroxyphenyl)-3-oxo- propyl)pyrrolidine-3-yl)-1H-benzo[d]imidazole-4-carboxamide: a potent poly(ADP-ribose) polymerase (PARP) inhibitor for treatment of cancer.SDS of cas: 574-98-1 And the article contains the following content:

A series of benzimidazole carboxamide derivatives have been synthesized and characterized by 1H-NMR, 13C-NMR and HRMS. PARP inhibition assays and cellular proliferation assays have also been carried out. Compounds 5cj and 5cp exhibited potential anticancer activities with IC50 values of about 4 nM against both PARP-1 and PARP-2, similar to the reference drug veliparib. The two compounds also displayed slightly better in vitro cytotoxicities against MDA-MB-436 and CAPAN-1 cell lines than veliparib and olaparib, with values of 17.4 microM and 11.4 microM, 19.8 microM and 15.5 microM, resp. The structure-activity relationship based on mol. docking was discussed as well. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).SDS of cas: 574-98-1

The Article related to breast cancer parp inhibitor, parp enzyme inhibition, benzimidazole carboxamide, poly(adp-ribose) polymerase, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On March 15, 2019, Miyake, Yuka; Itoh, Yukihiro; Hatanaka, Atsushi; Suzuma, Yoshinori; Suzuki, Miki; Kodama, Hidehiko; Arai, Yoshinobu; Suzuki, Takayoshi published an article.Formula: C10H8BrNO2 The title of the article was Identification of novel lysine demethylase 5-selective inhibitors by inhibitor-based fragment merging strategy. And the article contained the following:

Histone lysine demethylases (KDMs) have drawn much attention as targets of therapeutic agents. KDM5 proteins, which are Fe(II)/α-ketoglutarate-dependent demethylases, are associated with oncogenesis and drug resistance in cancer cells, and KDM5-selective inhibitors are expected to be anticancer drugs. However, few cell-active KDM5 inhibitors have been reported and there is an obvious need to discover more. In this study, we pursued the identification of highly potent and cell-active KDM5-selective inhibitors. Based on the reported KDM5 inhibitors, we designed several compounds by strategically merging two fragments for competitive inhibition with α-ketoglutarate and for KDM5-selective inhibition. Among them, compounds 10 and 13, which have a 3-cyano pyrazolo[1,5-a]pyrimidin-7-one scaffold, exhibited strong KDM5-inhibitory activity and significant KDM5 selectivity. In cellular assays using human lung cancer cell line A549, 10 and 13 increased the levels of trimethylated lysine 4 on histone H3, which is a specific substrate of KDM5s, and induced growth inhibition of A549 cells. These results should provide a basis for the development of cell-active KDM5 inhibitors to highlight the validity of our inhibitor-based fragment merging strategy. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Formula: C10H8BrNO2

The Article related to lysine demethylase kdm5 inhibitor drug design histone methylation epigenetics, epigenetics, histone methylation, inhibitor design, jhdm, kdm, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Formula: C10H8BrNO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary