Tag: 200-300

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

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 July 21, 2022, Garofalo, Albert W.; Schwarz, Jacob Bradley; Sabbatini, Fabio Maria; Migliore, Marco; Bernardi, Silvia; Budassi, Federica published a patent.Related Products of 1427433-22-4 The title of the patent was Preparation of indazoles and azaindazoles as LRRK2 inhibitors. And the patent contained the following:

The present invention is directed to indazole and azaindazole derivatives I and II [A = (un)substituted aryl, cycloalkyl, 5-14 membered heteroaryl, etc.; L = O or NH; ring B = Ph or 6-membered heteroaryl; ring C = Ph or 6-membered heteroaryl, wherein ring C is fused to ring D; X2 = N or CR2; X3 = N or CR3; X4 = N or CR4; wherein not more than two of X2, X3, and X4 are simultaneously N; each R1 and R5 = (independently) H, halo, alkyl, etc.; R2-R4 = (independently) H, halo, alkyl, etc.; n = 0-3; m = 0-1; p = 0-3; wherein in I: when ring B = Ph, then n = 1-3 and R1 = group other than H] or pharmaceutically acceptable salts thereof which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders such as Parkinson’s disease. E.g., a multi-step synthesis of III, starting from 6-bromo-1H-indazole and 1-cyclopropyl-4-iodopyrazole, was described. Exemplified compounds I and II were tested in the LRRK2 kinase activity assay (data given). Pharmaceutical composition comprising compound I or II was disclosed. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Related Products of 1427433-22-4

The Article related to indazole azaindazole preparation lrrk2 inhibitor cns disorder parkinson disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 19, 2018, Blagg, Brian S. J.; Kent, Caitlin Nicole; Mishra, Sanket Jaiprakash; Khandelwal, Anuj published a patent.Related Products of 39503-58-7 The title of the patent was Preparation of isoindolin-2-ylmethanone compounds as Hsp90b selective inhibitors for treatment of cancer. And the patent contained the following:

Provided are compounds of formula I as well as compositions including such compounds useful for the treatment of cancers such as non-small cell lung cancer, bladder cancer, or colon cancer. I [wherein each X independently = H, halo, sulfoxide, sulfone, etc.; R1 = H, OH, C1-3 alkyl, etc.; R2 = CH2X5 or OH; X5 = OH, halo, CN, etc.; R3 = alkyl, -CH(CH3)2, CF3, etc.] or a pharmaceutically acceptable salt and/or solvate thereof, are claimed and exemplified. Example compound II was prepared from a multistep procedure (preparation given). Exemplified I was evaluated for antiproliferative activity in cancer cell lines with II demonstrating IC50 values as low as 6.74 ± 1.1 μM in NCI-H23 non-small cell lung cancer cells. The experimental process involved the reaction of Methyl 5-bromo-2-methoxy-4-methylbenzoate(cas: 39503-58-7).Related Products of 39503-58-7

The Article related to isoindolinylmethanone compound preparation hsp90b inhibitor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 39503-58-7

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 15, 2011, Yeung, Kap-Sun; Parcella, Kyle E.; Bender, John A.; Beno, Brett R.; Grant-Young, Katharine A.; Han, Ying; Hewawasam, Piyasena; Kadow, John F.; Nickel, Andrew published a patent.Quality Control of 5-Bromo-2-methoxy-4-methylbenzoic acid The title of the patent was Preparation of benzofurancarboxamide derivatives and their preparation and use for the treatment of hepatitis C. And the patent contained the following:

The invention relates to benzofurancarboxamide derivatives of formula I, which are useful for treatment of hepatitis C. Compounds of formula I wherein R1 is NR5R6, alkoxy, Ph, etc.; R2 is H, halo, NO2, NH2, Ph and NR5R6; R3 is CN, alkoxycarbonyl, (cycloalkyl)oxycarbonyl, etc.; R4 is substituted Ph; R5 is H, alkyl and alkylsulfonyl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl and alkylsulfonyl; R20 and R21 are independently H, halo, alkyl and alkoxy; and pharmaceutically acceptable salts thereof, are disclosed. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their activity against HCV. From the assay, it was determined that compound II exhibited IC50 and EC50 values in the range 0.002 – 0.25 μM, resp. The experimental process involved the reaction of 5-Bromo-2-methoxy-4-methylbenzoic acid(cas: 90326-61-7).Quality Control of 5-Bromo-2-methoxy-4-methylbenzoic acid

The Article related to benzofurancarboxamide preparation treatment hepatitis c, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Quality Control of 5-Bromo-2-methoxy-4-methylbenzoic acid

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Yu, Xi-Hui; Cai, Xiong-Jie; Hong, Xiao-Qiao; Tam, Kin Yip; Zhang, Kun; Chen, Wen-Hua published an article in 2019, the title of the article was Synthesis and biological evaluation of aza-crown ether-squaramide conjugates as anion/cation symporters.Electric Literature of 574-98-1 And the article contains the following content:

Anion/cation symport across cellular membranes may lead to cell apoptosis and be developed as a strategy for new anticancer drug discovery. Four aza-crown ether-squaramide conjugates were synthesized and characterized. Their anion recognition, anion/cation symport, cytotoxicity and probable mechanism of action were investigated in details. These conjugates are able to form ion-pairing complexes with chloride anions and facilitate the transmembrane transport of anions via an anion/cation symport process. They can disrupt the cellular homeostasis of chloride anions and sodium cations and induce the basification of acidic organelles in live cells. These conjugates exhibit moderate cytotoxicity toward the tested cancer cells and trigger cell apoptosis by mediating the influx of chloride anions and sodium cations into live 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 aza ether squaramide anion cation cervical cancer antitumor agent, anion/cation symporter, anionophoric activity, antiproliferative activity, aza-crown ether, squaramide, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Electric Literature of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 7, 2021, You, Lijun; Yuan, Wei; He, Chuan published an article.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Intermolecular Dehydrogenative C-H/Si-H Cross-Coupling for the Synthesis of Arylbenzyl Bis(silanes). And the article contained the following:

An Ir-catalyzed intermol. dehydrogenative C-H/Si-H cross-coupling reaction for the synthesis of arylbenzyl bis(silanes) is developed. This hydrosilyl group steered intermol. C-H silylation process features high chemo- and regioselectivity, giving access to a wide range of multi-functionalized organosilanes in good yields from readily available starting materials with atom economy, efficiency, and environmental benignity. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to benzhydryldimethylsilane iridium catalyzed intermol dehydrogenative cross coupling phenyldimethylsilane, crystal structure arylbenzyl bissilane, mol structure, Organometallic and Organometalloidal Compounds: Silicon Compounds and other aspects.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

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

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 July 17, 2014, Boruah, Anima; Hosahalli, Subramanya; Panigrahi, Sunil Kumar published a patent.Related Products of 1261475-16-4 The title of the patent was Substituted 2-pyrazinone derivatives as kinase inhibitors. And the patent contained the following:

The present invention provides novel substituted 2-pyrazinone derivatives (I) as protein kinase inhibitors that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting kinase enzyme, more particularly BTK enzyme. The present invention also provides methods for synthesizing and administering the kinase inhibitor compounds The present invention also provides pharmaceutical formulations comprising at least one of the kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The experimental process involved the reaction of 1-Bromo-3-isocyanato-2-methyl-benzene(cas: 1261475-16-4).Related Products of 1261475-16-4

The Article related to btk kinase inhibitor pyrazinone derivative preparation cancer autoimmune inflammation, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Related Products of 1261475-16-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary