Tag: M.W=200-250

Zhu, Gui-Dong; Gong, Jianchun; Claiborne, Akiyo; Woods, Keith W.; Gandhi, Viraj B.; Thomas, Sheela; Luo, Yan; Liu, Xuesong; Shi, Yan; Guan, Ran; Magnone, Shayna R.; Klinghofer, Vered; Johnson, Eric F.; Bouska, Jennifer; Shoemaker, Alexander; Oleksijew, Anatol; Stoll, Vincent S.; De Jong, Ron; Oltersdorf, Tilman; Li, Qun; Rosenberg, Saul H.; Giranda, Vincent L. published the artcile< Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity>, Synthetic Route of 552331-06-3, the main research area is isoquinoline pyridine derivative preparation Akt kinase inhibitor.

The structure-activity relationships of a series of isoquinoline-pyridine-based protein kinase B/Akt antagonists have been investigated in an effort to improve the major shortcomings of the lead compound (I), including poor pharmacokinetic profiles in several species (e.g., mouse iv t1/2 = 0.3 h, po F = 0%). Chlorination at C-1 position of the isoquinoline improved its pharmacokinetic property in mice (iv t1/2 = 5.0 h, po F = 51%) but resulted in >500-fold drop in potency. In a mouse MiaPaCa-2 xenograft model, an amino analog (II) significantly slowed the tumor growth, however was accompanied by toxicity.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 552331-06-3 belongs to class isoquinoline, and the molecular formula is C9H5BrClN, Synthetic Route of 552331-06-3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Mansour, Oula C.; Evison, Benny J.; Sleebs, Brad E.; Watson, Keith G.; Nudelman, Abraham; Rephaeli, Ada; Buck, Damian P.; Collins, J. Grant; Bilardi, Rebecca A.; Phillips, Don R.; Cutts, Suzanne M. published the artcile< New Anthracenedione Derivatives with Improved Biological Activity by Virtue of Stable Drug-DNA Adduct Formation>, Category: isoquinoline, the main research area is anthracenedione amino derivative DNA adduct formation.

Mitoxantrone is an anticancer agent that acts as a topoisomerase II poison, however, it can also be activated by formaldehyde to form DNA adducts. Pixantrone, a 2-aza-anthracenedione with terminal primary amino groups in its side chains, forms formaldehyde-mediated adducts with DNA more efficiently than mitoxantrone. Mol. modeling studies indicated that extension of the “”linker”” region of anthracenedione side arms would allow the terminal primary amino greater flexibility and thus access to the guanine residues on the opposite DNA strand. New derivatives based on the pixantrone and mitoxantrone backbones were synthesized, and these incorporated primary amino groups as well as extended side chains. The stability of DNA adducts increased with increasing side chain length of the derivatives A mitoxantrone derivative bearing extended side chains (I) formed the most stable adducts with ∼100-fold enhanced stability compared to mitoxantrone. This finding is of great interest because long-lived drug-DNA adducts are expected to perturb DNA-dependent functions at all stages of the cell cycle.

Journal of Medicinal Chemistry published new progress about Acute promyelocytic leukemia. 144511-13-7 belongs to class isoquinoline, and the molecular formula is C13H5F2NO2, Category: isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Krapcho, A. Paul; Petry, Mary E.; Getahun, Zelleka; Landi, John J. Jr.; Stallman, John; Polsenberg, Johanna F.; Gallagher, Cynthia E.; Maresch, Martin J.; Hacker, Miles P. published the artcile< 6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A Novel Class of Chromophore-Modified Antitumor Anthracene-9,10-diones: Synthesis and Antitumor Evaluations>, Recommanded Product: 6,9-Difluorobenzo[g]isoquinoline-5,10-dione, the main research area is anthracenedione preparation antitumor; benzoisoquinoline preparation antitumor.

Synthetic procedures have been developed which lead to the 2-aza congeners I (R = amine groups or N-containing heterocyclic groups) and several related N-oxides (II, R = NH2 or NMe2). I exhibited a wide range of in vitro cytotoxicity against L1210 leukemia, the human colon adenocarcinoma cell line LoVo, and the doxorubicin resistant LoVo/DX cell line. Selected analogs of I showed significant P388 antileukemic activity in mice with I (R = NH2, n = 2) exhibiting high activity. This activity was also retained in the related N-oxide II (R = NH2, n = 2). These heterocyclic bioisosteric models are representative of the first anthracene-9,10-diones which display antileukemic activity comparable to mitoxantrone.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 144511-13-7 belongs to class isoquinoline, and the molecular formula is C13H5F2NO2, Recommanded Product: 6,9-Difluorobenzo[g]isoquinoline-5,10-dione.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Liang, Jun; Van Abbema, Anne; Balazs, Mercedesz; Barrett, Kathy; Berezhkovsky, Leo; Blair, Wade S.; Chang, Christine; Delarosa, Donnie; De Voss, Jason; Driscoll, Jim; Eigenbrot, Charles; Goodacre, Simon; Ghilardi, Nico; MacLeod, Calum; Johnson, Adam; Bir Kohli, Pawan; Lai, Yingjie; Lin, Zhonghua; Mantik, Priscilla; Menghrajani, Kapil; Nguyen, Hieu; Peng, Ivan; Sambrone, Amy; Shia, Steven; Smith, Jan; Sohn, Sue; Tsui, Vickie; Ultsch, Mark; Williams, Karen; Wu, Lawren C.; Yang, Wenqian; Zhang, Birong; Magnuson, Steven published the artcile< Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model>, Computed Properties of 552331-06-3, the main research area is imidazopyridine derivative preparation TYK2 inhibitor psoriasis; IL-23; Imidazopyridine; Kinase; Psoriasis; TYK2.

Herein we report identification of an imidazopyridine class of potent and selective TYK2 inhibitors, exemplified by prototype 6, through constraint of the rotatable amide bond connecting the pyridine and aryl rings of compound 1. Further optimization led to generation of compound 30 that potently inhibits the TYK2 enzyme and the IL-23 pathway in cells, exhibits selectivity against cellular JAK2 activity, and has good pharmacokinetic properties. In mice, compound 30 demonstrated dose-dependent reduction of IL-17 production in a PK/PD model as well as in an imiquimod-induced psoriasis model. In this efficacy model, the IL-17 decrease was accompanied by a reduction of ear thickness indicating the potential of TYK2 inhibition as a therapeutic approach for psoriasis patients.

Bioorganic & Medicinal Chemistry Letters published new progress about Antipsoriatic agents. 552331-06-3 belongs to class isoquinoline, and the molecular formula is C9H5BrClN, Computed Properties of 552331-06-3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Isoquinoline’s properties: Isoquinoline is a colorless hygroscopic liquid at temperatures above its melting point with a penetrating, 1532-97-4, formula is C9H6BrN, Name is 4-Bromoisoquinoline. unpleasant odor. Impure samples can appear brownish, as is typical for nitrogen heterocycles. Formula: C9H6BrN.

Yang, Xu-Wen;Li, Dong-Hui;Song, A-Xiang;Liu, Feng-Shou research published 《 ”Bulky-Yet-Flexible” α-Diimine Palladium-Catalyzed Reductive Heck Cross-Coupling: Highly Anti-Markovnikov-Selective Hydroarylation of Alkene in Air》, the research content is summarized as follows. To pursue a highly regioselective and efficient reductive Heck reaction, a series of moisture- and air-stable α-diimine palladium precatalysts was rationally designed, readily synthesized, and fully characterized. The relationship between the structures of the palladium complexes and the catalytic properties was investigated. It was revealed that the “bulky-yet-flexible” palladium complexes allowed highly anti-Markovnikov-selective hydroarylation of alkenes with (hetero)aryl bromides under aerobic conditions. Further, synthetic application of the present protocol could provide rapid and straightforward access to functional and biol. active mols.

Formula: C9H6BrN, 4-Bromoisoquinoline, also known as 4-Bromoisoquinoline, is a useful research compound. Its molecular formula is C9H6BrN and its molecular weight is 208.05 g/mol. The purity is usually 95%.

4-Bromoisoquinoline is an aryl halide that can be used in the cross-coupling reaction with other aryl halides. It has been shown to have anticancer activity and to inhibit the growth of tumour cell lines in vitro. This compound is also efficient for inhibiting leukemia cells. 4-Bromoisoquinoline has been shown to have an inhibitory effect on cancer cells through the inhibition of DNA synthesis and RNA transcription, as well as by inducing apoptosis. The mechanism of action may be due to its ability to bind to aromatic hydrocarbons and halides, which leads to thermodynamic changes and vibrational energy transfer., 1532-97-4.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

In a broader sense, the term isoquinoline is used to make reference to isoquinoline derivatives. 1-Benzylisoquinoline is the structural backbone in naturally occurring alkaloids including papaverine. 1532-97-4, formula is C9H6BrN, Name is 4-Bromoisoquinoline. The isoquinoline ring in these natural compound derives from the aromatic amino acid tyrosine. Product Details of C9H6BrN.

Xu, Dan;Zhao, Hong;Dong, Zhengping;Ma, Jiantai research published 《 Catalytically Active Co-N_x Species Stabilized on Nitrogen-doped Porous Carbon for Efficient Hydrogenation and Dehydrogenation of N-heteroarenes》, the research content is summarized as follows. A highly dispersed cobalt catalyst stabilized on the mesoporous N-doped carbon layers was prepared by adsorption and pyrolysis of cobalt complex on dendritic fibrous silica nanospheres (KCC-1@Co-N-C-T)was studied. The characterizations of HAADF-STEM, XRD and XPS together with the KSCN poisoning tests determine the absence of Co⁰ or CoO_x nanoparticles and the Co-N_x species were the active sites. The formation of Co-N_x species resulted from the properties of N-rich cobalt-phenanthroline complex and dendritic fibrous silica supports, increased the original spatial distance between Co atoms and thus prevented them from aggregation. The KCC-1@Co-N-C-800 catalyst showed excellent activity and selectivity for the oxidative dehydrogenation (ODH) of saturated N-heterocycles and base-free catalytic transfer hydrogenation (CTH) of unsaturated N-heterocycles.

Product Details of C9H6BrN, 4-Bromoisoquinoline, also known as 4-Bromoisoquinoline, is a useful research compound. Its molecular formula is C9H6BrN and its molecular weight is 208.05 g/mol. The purity is usually 95%.

4-Bromoisoquinoline is an aryl halide that can be used in the cross-coupling reaction with other aryl halides. It has been shown to have anticancer activity and to inhibit the growth of tumour cell lines in vitro. This compound is also efficient for inhibiting leukemia cells. 4-Bromoisoquinoline has been shown to have an inhibitory effect on cancer cells through the inhibition of DNA synthesis and RNA transcription, as well as by inducing apoptosis. The mechanism of action may be due to its ability to bind to aromatic hydrocarbons and halides, which leads to thermodynamic changes and vibrational energy transfer., 1532-97-4.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

In a broader sense, the term isoquinoline is used to make reference to isoquinoline derivatives. 1-Benzylisoquinoline is the structural backbone in naturally occurring alkaloids including papaverine. 1532-97-4, formula is C9H6BrN, Name is 4-Bromoisoquinoline. The isoquinoline ring in these natural compound derives from the aromatic amino acid tyrosine. Synthetic Route of 1532-97-4.

Xu, Pin;Chen, Peng-Yu;Xu, Hai-Chao research published 《 Scalable Photoelectrochemical Dehydrogenative Cross-Coupling of Heteroarenes with Aliphatic C-H Bonds》, the research content is summarized as follows. Heteroarenes are structural motifs found in many bioactive compounds and functional materials. Dehydrogenative cross-coupling of heteroarenes with aliphatic C-H bonds provides straightforward access to functionalized heteroarenes from readily available materials. Established methods employ stoichiometric chem. oxidants under conditions of heating or light irradiation By merging electrochem. and photochem., we have achieved efficient photoelectrochem. dehydrogenative cross-coupling of heteroarenes and C(sp³)-H donors through H₂ evolution, without the addition of metal catalysts or chem. oxidants. Mechanistically, the C(sp³)-H donor is converted to a nucleophilic carbon radical through H-atom transfer with chlorine atom, which is produced by light irradiation of anodically generated Cl₂ from Cl^–. The carbon radical then undergoes radical substitution to the heteroarene to afford alkylated heteroarene products.

Synthetic Route of 1532-97-4, 4-Bromoisoquinoline, also known as 4-Bromoisoquinoline, is a useful research compound. Its molecular formula is C9H6BrN and its molecular weight is 208.05 g/mol. The purity is usually 95%.

4-Bromoisoquinoline is an aryl halide that can be used in the cross-coupling reaction with other aryl halides. It has been shown to have anticancer activity and to inhibit the growth of tumour cell lines in vitro. This compound is also efficient for inhibiting leukemia cells. 4-Bromoisoquinoline has been shown to have an inhibitory effect on cancer cells through the inhibition of DNA synthesis and RNA transcription, as well as by inducing apoptosis. The mechanism of action may be due to its ability to bind to aromatic hydrocarbons and halides, which leads to thermodynamic changes and vibrational energy transfer., 1532-97-4.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

In a broader sense, the term isoquinoline is used to make reference to isoquinoline derivatives. 1-Benzylisoquinoline is the structural backbone in naturally occurring alkaloids including papaverine. 1532-97-4, formula is C9H6BrN, Name is 4-Bromoisoquinoline. The isoquinoline ring in these natural compound derives from the aromatic amino acid tyrosine. Application of C9H6BrN.

Yadav, Lalit;Tiwari, Mohit K.;Shyamlal, Bharti Rajesh Kumar;Chaudhary, Sandeep research published 《 Organocatalyst in Direct C(_sp²)-H Arylation of Unactivated Arenes: [1-(2-Hydroxyethyl)-piperazine]-Catalyzed Inter-/Intra-molecular C-H Bond Activation》, the research content is summarized as follows. In the presence of 10 mol% 1-piperazineethanol, aryl iodides and bromides underwent arylation with benzene mediated by KOt-Bu to yield biaryls. N-Aryl 2-bromobenzamides underwent cyclization mediated by KOt-Bu in the presence of 40 mol% 1-piperazineethanol and 40 mol% 4-dimethylaminopyridine in mesitylene to yield phenanthridinones. Study of the reaction mechanism using kinetics and kinetic isotope effects and inhibition studies are consistent with the formation of aryl radical anions and a single electron transfer mechanism.

Application of C9H6BrN, 4-Bromoisoquinoline, also known as 4-Bromoisoquinoline, is a useful research compound. Its molecular formula is C9H6BrN and its molecular weight is 208.05 g/mol. The purity is usually 95%.

4-Bromoisoquinoline is an aryl halide that can be used in the cross-coupling reaction with other aryl halides. It has been shown to have anticancer activity and to inhibit the growth of tumour cell lines in vitro. This compound is also efficient for inhibiting leukemia cells. 4-Bromoisoquinoline has been shown to have an inhibitory effect on cancer cells through the inhibition of DNA synthesis and RNA transcription, as well as by inducing apoptosis. The mechanism of action may be due to its ability to bind to aromatic hydrocarbons and halides, which leads to thermodynamic changes and vibrational energy transfer., 1532-97-4.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Isoquinoline’s properties: Isoquinoline is a colorless hygroscopic liquid at temperatures above its melting point with a penetrating, 1532-97-4, formula is C9H6BrN, Name is 4-Bromoisoquinoline. unpleasant odor. Impure samples can appear brownish, as is typical for nitrogen heterocycles. Name: 4-Bromoisoquinoline.

Zhang, Dong;Cai, Jinlin;Du, Jinze;Wang, Qingdong;Yang, Jinming;Geng, Rongqing;Fang, Zheng;Guo, Kai research published 《 Electrochemical-Oxidation-Promoted Direct N-ortho-Selective Difluoromethylation of Heterocyclic N-Oxides》, the research content is summarized as follows. An efficient and green electrochem. N-ortho-selective difluoromethylation method of various quinoline and isoquinoline N-oxides has been developed. In this method sodium difluoromethanesulfinate (HCF₂SO₂Na) was used as the source of difluoromethyl moiety and various N-ortho-selective difluoromethylation quinolines and isoquinolines N-oxides were obtained in good to excellent yield under constant current. In addition, the reaction was easy to scale up and maintains good yields. Preliminary mechanism studies suggested that the reaction has underwent a free radical addition and hydrogen elimination pathway.

Name: 4-Bromoisoquinoline, 4-Bromoisoquinoline, also known as 4-Bromoisoquinoline, is a useful research compound. Its molecular formula is C9H6BrN and its molecular weight is 208.05 g/mol. The purity is usually 95%.

4-Bromoisoquinoline is an aryl halide that can be used in the cross-coupling reaction with other aryl halides. It has been shown to have anticancer activity and to inhibit the growth of tumour cell lines in vitro. This compound is also efficient for inhibiting leukemia cells. 4-Bromoisoquinoline has been shown to have an inhibitory effect on cancer cells through the inhibition of DNA synthesis and RNA transcription, as well as by inducing apoptosis. The mechanism of action may be due to its ability to bind to aromatic hydrocarbons and halides, which leads to thermodynamic changes and vibrational energy transfer., 1532-97-4.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Isoquinoline is a heterocyclic aromatic organic compound. 1532-97-4, formula is C9H6BrN, Name is 4-Bromoisoquinoline. It is a structural isomer of quinoline. Isoquinoline and quinoline are benzopyridines, which are composed of a benzene ring fused to a pyridine ring. HPLC of Formula: 1532-97-4.

Zhao, Jianhong;Qian, Kun;Tong, Mengchao;Yuan, Qiyang;Zhang, Yongqiang research published 《 Mild and Metal-Free Cross-Dehydrogenative Coupling of Nitrogen Heteroarenes with Aldehydes Enabled by Structural Hybridization of Promoting Reagents》, the research content is summarized as follows. A mild and metal-free cross-dehydrogenative coupling reaction of nitrogen heteroarenes with aldehydes has been developed by the structural hybridization of promoting reagents. The procedure is environmentally benign, cost-effective and industrially scalable, which allows the direct acylation of electron-deficient nitrogen heteroarenes in moderate to good yields. Furthermore, the synthetic utility of this new method in the synthesis of a variety of pharmaceutically relevant isoquinoline alkaloids has been also demonstrated.

1532-97-4, 4-Bromoisoquinoline, also known as 4-Bromoisoquinoline, is a useful research compound. Its molecular formula is C9H6BrN and its molecular weight is 208.05 g/mol. The purity is usually 95%.

4-Bromoisoquinoline is an aryl halide that can be used in the cross-coupling reaction with other aryl halides. It has been shown to have anticancer activity and to inhibit the growth of tumour cell lines in vitro. This compound is also efficient for inhibiting leukemia cells. 4-Bromoisoquinoline has been shown to have an inhibitory effect on cancer cells through the inhibition of DNA synthesis and RNA transcription, as well as by inducing apoptosis. The mechanism of action may be due to its ability to bind to aromatic hydrocarbons and halides, which leads to thermodynamic changes and vibrational energy transfer., HPLC of Formula: 1532-97-4

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem