Month: November 2022

On February 15, 2021, Yang, Ling; Tan, Dong-Hang; Fan, Wen-Xin; Liu, Xu-Ge; Wu, Jia-Qiang; Huang, Zhi-Shu; Li, Qingjiang; Wang, Honggen published an article.Safety of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Photochemical Radical C-H Halogenation of Benzyl N-Methyliminodiacetyl (MIDA) Boronates: Synthesis of α-Functionalized Alkyl Boronates. And the article contained the following:

Benzylboronates ArCH2B(MIDA) were halogenated in α-position by reaction with NBS either initiated with benzyl peroxide or photochem., giving α-haloboronates ArCHXB(MIDA). Fluorination and chlorination were performed by reactions with Selectfluor and NCS, resp., under 9-fluorenone catalysis. α-Haloboronates are useful organic synthons that can be converted to a diverse array of α-substituted alkyl borons. Methods to α-haloboronates are limiting and often suffer from harsh reaction conditions. Reported herein is a photochem. radical C-H halogenation of benzyl N-methyliminodiacetyl (MIDA) boronates. Fluorination, chlorination, and bromination reactions were effective by using this protocol. Upon reaction with different nucleophiles, the C-Br bond in the brominated product could be readily transformed to a series of C-C, C-O, C-N, C-S, C-P, and C-I bonds, some of which are difficult to forge with α-halo sp2-B boronate esters. An activation effect of B(MIDA) moiety was found. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Safety of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to bmida methyliminodiacetyl boronate photochem halogenation preparation haloboronate, halogenation, ketone catalysis, organoboron, photochemistry, radical reaction, Organometallic and Organometalloidal Compounds: Boron Compounds and other aspects.Safety of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On February 8, 2022, Li, Yingying; Jiang, Zhimin; Duan, Xiaoqun; Wei, Riming; Chen, Yijie; Fan, Xinxin; Liu, Jieyu; Su, Huilin published a patent.Formula: C24H27Br2P The title of the patent was Artesunate derivatives as antitumor agents and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

The invention relates to the tech. field of medicine, and specifically discloses artesunate derivatives I•Br- and II•Br- (n is 6-20; R1 is C1-6 alkyl) and preparation method and application thereof. Compounds I and II were prepared by using alkylation and esterification as the key steps. All the invention compounds were evaluated for their antitumor activity. The artesunate derivatives provided by the present invention have novel skeleton structure and excellent antitumor activity, and can be used for the preparation of antitumor drugs. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Formula: C24H27Br2P

The Article related to artesunate derivative preparation antitumor treatment cancer, Terpenes and Terpenoids: Sesquiterpenes (C15), Including Ionones and other aspects.Formula: C24H27Br2P

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 2, 2015, Kang, Byeong Heon; Lee, Chang Uk; Yoo, Ja Hyeong; Park, Hye Gyeong published a patent.HPLC of Formula: 83152-22-1 The title of the patent was Mitochondria-targeting antitumor compositions. And the patent contained the following:

The title antitumor composition has excellent inhibitory effect on mol. chaperones (e.g. Hsp90 and TRAP1) in tumor cells, by connecting triphenylphosphate into mitochondria-penetrating moiety, by using 8-(6-iodo-benzo[1,3]dioxol-5-ylsulfanyl)adenine as mol. chaperone inhibitor. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).HPLC of Formula: 83152-22-1

The Article related to mitochondria targeting antitumor therapy, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.HPLC of Formula: 83152-22-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On April 8, 2015, Lee, Changwook; Park, Hye-Kyung; Jeong, Hanbin; Lim, Jaehwa; Lee, An-Jung; Cheon, Keun Young; Kim, Chul-Su; Thomas, Ajesh P.; Bae, Boram; Kim, Nam Doo; Kim, Seong Heon; Suh, Pann-Ghill; Ryu, Ja-Hyoung; Kang, Byoung Heon published an article.Formula: C24H27Br2P The title of the article was Development of a Mitochondria-Targeted Hsp90 Inhibitor Based on the Crystal Structures of Human TRAP1. And the article contained the following:

The mitochondrial pool of Hsp90 and its mitochondrial paralog, TRAP1, suppresses cell death and reprograms energy metabolism in cancer cells; therefore, Hsp90 and TRAP1 have been suggested as target proteins for anticancer drug development. Here, the authors report that the actual target protein in cancer cell mitochondria is TRAP1, and current Hsp90 inhibitors cannot effectively inactivate TRAP1 because of their insufficient accumulation in the mitochondria. To develop mitochondrial TRAP1 inhibitors, the authors determined the crystal structures of human TRAP1 complexed with Hsp90 inhibitors. The iso-Pr amine of the Hsp90 inhibitor PU-H71 was replaced with the mitochondria-targeting moiety triphenylphosphonium to produce SMTIN-P01. SMTIN-P01 showed a different mode of action from the nontargeted PU-H71, as well as much improved cytotoxicity to cancer cells. In addition, the authors determined the structure of a TRAP1-adenylyl-imidodiphosphate (AMP-PNP) complex. On the basis of comparative anal. of TRAP1 structures, the authors propose a mol. mechanism of ATP hydrolysis that is crucial for chaperone function. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Formula: C24H27Br2P

The Article related to mitochondria hsp inhibitor crystal structure trap, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Formula: C24H27Br2P

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

On January 16, 2014, Stockwell, Brent R.; Welsch, Matthew; Yang, Wan Seok published a patent.HPLC of Formula: 1019442-22-8 The title of the patent was Quinazolinone-based oncogenic-ras-selective lethal compounds and their use. And the patent contained the following:

The present invention provides compounds for treating or ameliorating the effects of a cancer having a cell that harbors an oncogenic RAS mutation, for modulating a lipoxygenase in a ferroptosis cell death pathway, and for depleting reduced glutathione (GSH) in a cell harboring an oncogenic RAS mutation are further provided. The experimental process involved the reaction of 5-Bromo-2-isopropoxyaniline(cas: 1019442-22-8).HPLC of Formula: 1019442-22-8

The Article related to antitumor quinazolinone preparation oncogenic ras mutation cancer therapy, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.HPLC of Formula: 1019442-22-8

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 25, 2015, Stockwell, Brent R.; Welsch, Matthew; Yang, Wan Seok published a patent.Application In Synthesis of 5-Bromo-2-isopropoxyaniline The title of the patent was Quinazolinone-based oncogenic-ras-selective lethal compounds and their use. And the patent contained the following:

The present invention provides, inter alia, compounds having the structure (1) compositions containing such compounds are also provided. Methods for using such compounds or compositions for treating or ameliorating the effects of a cancer having a cell that harbors an oncogenic RAS mutation, for modulating a lipoxygenase in a ferroptosis cell death pathway, and for depleting reduced glutathione (GSH) in a cell harboring an oncogenic RAS mutation are further provided. The experimental process involved the reaction of 5-Bromo-2-isopropoxyaniline(cas: 1019442-22-8).Application In Synthesis of 5-Bromo-2-isopropoxyaniline

The Article related to antitumor quinazolinone preparation oncogenic ras mutation cancer therapy, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application In Synthesis of 5-Bromo-2-isopropoxyaniline

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

On September 28, 2020, Kim, Jong Seung; Sunwoo, Gyeong; Verwilst, Peter; Won, Mi Ae published a patent.COA of Formula: C24H27Br2P The title of the patent was Modified antibiotics for non-nuclear genotoxic chemotherapy and pharmaceutical composition for anti-cancer containing the same. And the patent contained the following:

The present invention relates to a modified antibiotic compound for the treatment of cancer with minimal nuclear gene damage and an anticancer pharmaceutical composition comprising same. Since the repurposed antibiotic compound has a therapeutic effect in a manner that targets only the mitochondria of cancer cells, the modified antibiotic compound does not cause gene degeneration unlike conventional chemotherapy which damages nuclear DNAs to kill cancer cells, , thereby preventing the recurrence of cancer. In addition, a mitochondria targeted therapy using the compound according to the present invention can effectively treat malignant tumors that are difficult to treat due to acquiring drug resistance by general anticancer treatment. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).COA of Formula: C24H27Br2P

The Article related to nonnuclear genotoxic chemotherapy mitochondria targeting antimetastatic repurposed antibiotic, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.COA of Formula: C24H27Br2P

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On September 24, 2020, Kim, Jong Seung; Sunwoo, Kyoung; Verwilst, Peter; Won, Miae published a patent.Formula: C24H27Br2P The title of the patent was Repurposed antibiotics for non-nuclear genotoxic chemotherapy and pharmaceutical composition for anti-cancer containing the same. And the patent contained the following:

The present invention relates to a repurposed antibiotic compound for the treatment of cancer with minimal nuclear gene damage and an anticancer pharmaceutical composition comprising same. Since the repurposed antibiotic compound has a therapeutic effect in a manner that targets only the mitochondria of cancer cells, the modified antibiotic compound does not cause gene degeneration unlike conventional chemotherapy which damages nuclear DNAs to kill cancer cells, , thereby preventing the recurrence of cancer. In addition, a mitochondria targeted therapy using the compound according to the present invention can effectively treat malignant tumors that are difficult to treat due to acquiring drug resistance by general anticancer treatment. The experimental process involved the reaction of (6-Bromohexyl)triphenylphosphonium bromide(cas: 83152-22-1).Formula: C24H27Br2P

The Article related to nonnuclear genotoxic chemotherapy mitochondria targeting antimetastatic repurposed antibiotic, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Formula: C24H27Br2P

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary