Category: 76006-33-2

《New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase》 was published in ACS Medicinal Chemistry Letters in 2020. These research results belong to Tanaka, Yuta; Kurasawa, Osamu; Yokota, Akihiro; Klein, Michael G.; Saito, Bunnai; Matsumoto, Shigemitsu; Okaniwa, Masanori; Ambrus-Aikelin, Geza; Uchiyama, Noriko; Morishita, Daisuke; Kimura, Hiromichi; Imamura, Shinichi. HPLC of Formula: 76006-33-2 The article mentions the following:

In this work, a new chem. series possessing fused ring scaffolds designed from high-throughput screening hit compounds was synthesized, discovering a 5,6-dihydrothieno[2,3-c]pyridine derivative I [R = (R)-i-Bu] with potent inhibitory activity. Furthermore, the X-ray crystallog. anal. of the DHPS complex with I [R = (R)-i-Bu] demonstrated a distinct allosteric binding mode compared to a previously reported inhibitor. These findings could be significantly useful in the functional anal. of conformational changes in DHPS as well as the structure-based design of allosteric inhibitors. In the part of experimental materials, we found many familiar compounds, such as 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2HPLC of Formula: 76006-33-2)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. HPLC of Formula: 76006-33-2Some of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2018,Advanced Synthesis & Catalysis included an article by Han, Wen-Jing; Pu, Fan; Li, Chao-Jun; Liu, Zhong-Wen; Fan, Juan; Shi, Xian-Ying. SDS of cas: 76006-33-2. The article was titled 《Carboxyl-Directed Conjugate Addition of C-H Bonds to α,β-Unsaturated Ketones in Air and Water》. The information in the text is summarized as follows:

A simple ruthenium-catalyzed conjugate addition of C-H bonds to α,β-unsaturated ketones directed by a removable carboxyl group was developed as an effective protocol to synthesize ortho-alkylated benzoic acids in a greener manner. Without any additives, satisfactory to excellent yields of the targeted products were achieved in neat water, and the process characterizes in mild reaction conditions (in air and water), simple operations, and broad substrate scope. Noteworthy features of this method include mild reaction conditions (in air and water), operational simplicity and broad substrate scope. The versatility and utility of the addition products were demonstrated through further transformation into commonly inaccessible but highly useful motifs of meta-substituted alkylbenzenes and 3-substituted isochromanones. The results came from multiple reactions, including the reaction of 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2SDS of cas: 76006-33-2)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. SDS of cas: 76006-33-2Some of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2010,Pan, Shifeng; Wu, Xu; Jiang, Jiqing; Gao, Wenqi; Wan, Yongqin; Cheng, Dai; Han, Dong; Liu, Jun; Englund, Nathan P.; Wang, Yan; Peukert, Stefan; Miller-Moslin, Karen; Yuan, Jing; Guo, Ribo; Matsumoto, Melissa; Vattay, Anthony; Jiang, Yun; Tsao, Jeffrey; Sun, Fangxian; Pferdekamper, AnneMarie C.; Dodd, Stephanie; Tuntland, Tove; Maniara, Wieslawa; Kelleher, Joseph F. III; Yao, Yung-mae; Warmuth, Markus; Williams, Juliet; Dorsch, Marion published 《Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist》.ACS Medicinal Chemistry Letters published the findings.Synthetic Route of C8H7BrO2 The information in the text is summarized as follows:

The blockade of aberrant hedgehog (Hh) signaling has shown promise for therapeutic intervention in cancer. A cell-based phenotypic high-throughput screen was performed, and the lead structure (1) was identified as an inhibitor of the Hh pathway via antagonism of the Smoothened receptor (Smo). Structure-activity relation studies led to the discovery of a potent and specific Smoothened antagonist N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4′-(trifluoromethoxy)biphenyl-3-carboxamide (5m, NVP-LDE225), which is currently in clin. development. In the experiment, the researchers used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Synthetic Route of C8H7BrO2)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. Synthetic Route of C8H7BrO2 The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Liu, Wentao; Huang, Wei; Lin, Qian; Tsai, Mei-Hsuan; Zhang, Rui; Fan, Lijun; Scott, Jack D.; Liu, Guansai; Wan, Jinqiao published their research in Bioorganic & Medicinal Chemistry in 2021. The article was titled 《Development of DNA-compatible hydroxycarbonylation reactions using chloroform as a source of carbon monoxide》.Related Products of 76006-33-2 The article contains the following contents:

A robust palladium-catalyzed hydroxycarbonylation of aryl halides on DNA has been developed. Instead of Mo(CO)6 as a source of carbon monoxide as previously described in the literature, chloroform was used as a surrogate in this report for the purpose of avoiding to use a large excess of molybdenum reagent which is not totally soluble in aqueous reaction mixtures In the experiment, the researchers used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Related Products of 76006-33-2)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. The most pervasive is the naturally produced bromomethane.Related Products of 76006-33-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Recommanded Product: 76006-33-2In 2014 ,《Pyridyl Benzamides as a Novel Class of Potent Inhibitors for the Kinetoplastid Trypanosoma brucei》 appeared in Journal of Medicinal Chemistry. The author of the article were Ferrins, Lori; Gazdik, Michelle; Rahmani, Raphael; Varghese, Swapna; Sykes, Melissa L.; Jones, Amy J.; Avery, Vicky M.; White, Karen L.; Ryan, Eileen; Charman, Susan A.; Kaiser, Marcel; Bergstrom, Christel A. S.; Baell, Jonathan B.. The article conveys some information:

A whole-organism screen of approx. 87000 compounds against Trypanosoma brucei identified a number of promising compounds for medicinal chem. optimization. One of these classes of compounds the authors termed the pyridyl benzamides. While the initial hit had an IC50 of 12 μM, it was small enough to be attractive for further optimization, and the authors utilized three parallel approaches to develop the structure-activity relationships. The authors determined that the physicochem. properties for this class are generally favorable with particular positions identified that appear to block metabolism when substituted and others that modulate solubility The most active compound is 79, which has an IC50 of 0.045 μM against the human pathogenic strain Trypanosoma brucei rhodesiense and is more than 4000 times less active against the mammalian L6 cell line. In the experiment, the researchers used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Recommanded Product: 76006-33-2)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Recommanded Product: 76006-33-2Some of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

《Rhodium(III)-catalyzed tandem C-H olefination and oxidative cyclization of aromatic acids with acrylates for the synthesis of (E)-3-ylidenephthalides》 was written by Han, Wen-Jing; Pu, Fan; Fan, Juan; Liu, Zhong-Wen; Shi, Xian-Ying. Application In Synthesis of 3-Bromo-2-methylbenzoic acidThis research focused onylidenephthalide regioselective diastereoselective preparation; benzoic acid acrylate rhodium catalyst tandem olefination oxidative cyclization. The article conveys some information:

Intermol. tandem C-H olefination/C-O cyclization was achieved via a rhodium (III)-catalyzed C-H activation of carboxylic acids with acrylates. Direct and efficient construction of biol. relevant (E)-3-ylidenephthalide I [R = 4-Me, 4-Me-5-MeO, 4-Me-6-Cl, etc.; R1 = Me, Et, t-Bu, n-Bu] scaffolds with satisfactory to good yields was synthesized and characterized by stoichiometric reactants, exclusive stereoselectivity, com. available substrates, mild atm. conditions and short reaction time (less than 2 h). The experimental part of the paper was very detailed, including the reaction process of 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Application In Synthesis of 3-Bromo-2-methylbenzoic acid)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides. Application In Synthesis of 3-Bromo-2-methylbenzoic acid

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2003,Gohier, Frederic; Mortier, Jacques published 《ortho-Metalation of Unprotected 3-Bromo and 3-Chlorobenzoic Acids with Hindered Lithium Dialkylamides》.Journal of Organic Chemistry published the findings.Name: 3-Bromo-2-methylbenzoic acid The information in the text is summarized as follows:

Upon treatment of 3-chloro/bromobenzoic acids with hindered lithium dialkylamides (LDA or LTMP) at -50 °C, lithium 3-chloro/bromo-2-lithiobenzoates are generated. These dianions can be trapped as such to afford after electrophilic quenching a variety of simple 2-substituted-3-chloro/bromobenzoic acids. The 3-bromo-2-lithiobenzoate is less stable than the 3-chloro analog and partly eliminates lithium bromide, thus setting free lithium 2,3- and 3,4-dehydrobenzoates that can be intercepted in situ with the hindered base. After reading the article, we found that the author used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Name: 3-Bromo-2-methylbenzoic acid)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Name: 3-Bromo-2-methylbenzoic acid Alkyl bromides are mainly used as alkylating agents and also find application as a solvent to extract oil from seeds and wool.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2006,Xiao, Xiangshu; Antony, Smitha; Pommier, Yves; Cushman, Mark published 《Total Synthesis and Biological Evaluation of 22-Hydroxyacuminatine》.Journal of Medicinal Chemistry published the findings.Electric Literature of C8H7BrO2 The information in the text is summarized as follows:

A total synthesis of 22-hydroxyacuminatine, a cytotoxic alkaloid isolated from Camptotheca acuminata, is reported. The key step in the synthesis involves the reaction of 2,3-dihydro-1H-pyrrolo[3,4-b]quinoline with a brominated phthalide to generate a substituted pentacyclic 12H-5,11a-diazadibenzo[b,h]fluoren-11-one intermediate. Despite its structural resemblance to camptothecin and luotonin A, a biol. evaluation of 22-hydroxyacuminatine in a topoisomerase I-deficient cell line P388/CPT45 has confirmed that the observed cytotoxicity is not due to topoisomerase I inhibition, even though 22-hydroxyacuminatine has a hydroxyl group that can theor. hydrogen bond to Asp533. This result is consistent with the hypothesis that π-π stacking is more important than hydrogen-bonding interactions in determining topoisomerase I inhibitor binding in the ternary cleavage complex. In the experimental materials used by the author, we found 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Electric Literature of C8H7BrO2)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Electric Literature of C8H7BrO2 Moreover, several studies demonstrate that the average proportion of bromine in drugs is significantly higher than that in natural products.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Formula: C8H7BrO2In 2016 ,《Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL)》 appeared in Journal of Medicinal Chemistry. The author of the article were Borkin, Dmitry; Pollock, Jonathan; Kempinska, Katarzyna; Purohit, Trupta; Li, Xiaoqin; Wen, Bo; Zhao, Ting; Miao, Hongzhi; Shukla, Shirish; He, Miao; Sun, Duxin; Cierpicki, Tomasz; Grembecka, Jolanta. The article conveys some information:

Development of potent small mol. inhibitors of protein-protein interactions with optimized druglike properties represents a challenging task in lead optimization process. Here, we report synthesis and structure-based optimization of new thienopyrimidine class of compounds, which block the protein-protein interaction between menin and MLL fusion proteins that plays an important role in acute leukemias with MLL translocations. We performed simultaneous optimization of both activity and druglike properties through systematic exploration of substituents introduced to the indole ring of lead compound 1 (MI-136) to identify compounds suitable for in vivo studies in mice. This work resulted in the identification of compound 27 (MI-538), which showed significantly increased activity, selectivity, polarity, and pharmacokinetic profile over 1 and demonstrated a pronounced effect in a mouse model of MLL leukemia. This study, which reports detailed structure-activity and structure-property relationships for the menin-MLL inhibitors, demonstrates challenges in optimizing inhibitors of protein-protein interactions for potential therapeutic applications. After reading the article, we found that the author used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Formula: C8H7BrO2)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Some of these compounds are identical to man-made organobromine compounds, such as methyl bromide, bromoform, and bromophenols, but many others are entirely new moleclar entities, often possessing extraordinary and important biological properties. Formula: C8H7BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

SDS of cas: 76006-33-2In 2018 ,《Regioselective C-H Alkylation via Carboxylate-Directed Hydroarylation in Water》 appeared in Chemistry – A European Journal. The author of the article were Zhang, Guodong; Jia, Fan; Goossen, Lukas J.. The article conveys some information:

In the presence of catalytic [RuCl2(p-cym)]2 and using Li3PO4 as the base, benzoic acids react with olefins in water to afford the corresponding 2-alkylbenzoic acids in moderate to excellent yields. This C-H alkylation process is generally applicable to diversely substituted electron-rich and electron-deficient benzoic acids, along with α,β-unsaturated olefins including unprotected acrylic acid. The widely available carboxylate directing group can be removed or used for further derivatization. Mechanistic studies revealed that the transformation proceeds via a ruthenacycle intermediate. In the experiment, the researchers used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2SDS of cas: 76006-33-2)

3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Due to the reactivity of bromide, they are used as potential precursors or important intermediates in organic synthesis. SDS of cas: 76006-33-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary