Tag: 200-300

On April 14, 2014, Vignaroli, Giulia; Mencarelli, Martina; Sementa, Deborah; Crespan, Emmanuele; Kissova, Miroslava; Maga, Giovanni; Schenone, Silvia; Radi, Marco; Botta, Maurizio published an article.Name: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the article was Exploring the Chemical Space around the Privileged Pyrazolo[3,4-d]pyrimidine Scaffold: Toward Novel Allosteric Inhibitors of T315I-Mutated Abl. And the article contained the following:

A library of pyrazolo[3,4-d]pyrimidines, endowed with a high level of mol. diversity, has been developed applying a synthetic sequence that allowed C3, N1, C4, and C6 substitution. The enzymic screening of this “privileged scaffold”-based compound collection, validated the use of a diversity-oriented approach in a field characteristically explored by target-oriented synthesis. In fact, several compounds showed high activity against the selected kinases (i.e., Src, Abl wt, and T315I mutated-form), furthermore and interestingly a new compound has emerged as an allosteric inhibitor of the T315I mutated-form of Abl, opening up new opportunities for the development of a novel class of noncompetitive inhibitors of Abl (T315I). The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Name: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

The Article related to diversity oriented synthesis library pyrazolopyrimidine inhibitor src abl kinase, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Name: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On May 15, 2019, Sun, Liangpeng; Wang, Peipei; Xu, Lili; Gao, Lixin; Li, Jia; Piao, Huri published an article.SDS of cas: 36640-53-6 The title of the article was Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors. And the article contained the following:

Two series of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, IIIv was found to have the best in vitro inhibition activity against PTP1B (IC50 = 0.67 ± 0.09 μM) and the best selectivity (9-fold) between PTP1B and T-cell protein tyrosine phosphatase (TCPTP). Mol. docking studies demonstrated that compounds IIIm, IIIv and IVg could occupy simultaneously at both the catalytic site and the adjacent pTyr binding site. These results provide novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).SDS of cas: 36640-53-6

The Article related to inhibition activity ptp1b inhibitor sar mol docking, 1,3-diphenyl-1h-pyrazole, ptp1b inhibitor, rhodanine-3-alkanoic acid, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.SDS of cas: 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On February 11, 1983, Cottam, Howard B.; Revankar, Ganapathi R.; Robins, Roland K. published an article.HPLC of Formula: 85426-79-5 The title of the article was A convenient synthesis of 6-amino-1-β-D-ribofuranosylpyrazolo[3,4-d]pyrimidin-4-one and related 4,6-disubstituted pyrazolopyrimidine nucleosides. And the article contained the following:

The glycosylation of 4,6-dichloropyrazolo[3,4-d]pyrimidine and 4-chloro-6-methylthiopyrazolo[3,4-d]pyrimidine via the corresponding trimethylsilyl intermediate and tetra-O-acetyl-β-D-ribofuranose in the presence of trimethylsilyl triflate as a catalyst, gave selective glycosylation at N-1 as the only nucleoside product. The intermediates 4,6-dichloro-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)pyrazolo[3,4-d]pyrimidine and 4-chloro-6-methylthio-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)pyrazolo[3,4-d]pyrimidine gave new and convenient synthetic routes to the inosine analog I, the guanosine analog II, the adenosine analog III, and the isoguanosine analog IV. Glycosylation of the trimethylsilyl derivative of 6-chloropyrazolo[3,4-d]pyrimidin-4-one unexpectedly gave the N-2 glycosyl isomer as the major product. A number of new 4,6-disubstituted pyrazolo[3,4-d]pyrimidine nucleosides were prepared from these glycosyl intermediates. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).HPLC of Formula: 85426-79-5

The Article related to pyrazolopyrimidine nucleoside, ribofuranosylpyrazolopyrimidinone, glycosylation pyrazolopyrimidine ribofuranose, Carbohydrates: Nucleosides and Nucleotides, Cobalamins, Riboflavin and other aspects.HPLC of Formula: 85426-79-5

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On August 13, 2009, Hirokawa, Takatsugu; Takemura, Shunji; Shibazaki, Manabu; Ishiwatari, Hiroyuki published a patent.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the patent was 3-naphthylpyrazole compounds, histamine H4 receptor antagonists containing them, their use for treatment for inflammatory disorders, and pharmaceutical compositions containing them. And the patent contained the following:

Claimed are title compounds I [ring A = C6-10 aryl; X = (CH2)n (n = 1-6), CH:N; Y = O, S, NR8; Z = direct bond, CHR7; R1-R7 = H, halo, OH, NO2, carboxy, carbamoyl, C1-6 alkyl, C2-6 acyl, C6-10-aryl-C1-6 alkyl, C5-10-heteroaryl-C2-6 alkenyl, etc.; R8 = H, OH, C1-6 alkyloxy], their salts, or their solvates [exclusive of (E)-2-[[3-(2-Naphthyl)-1-phenyl-1H-pyrazol-4-yl]methylene]hydrazinecarboxamide] and histamine H4 receptor antagonists containing I, their salts, or their solvates. Also claimed are prophylactic and/or therapeutic agents and pharmaceutical compositions containing I, their salts, or their solvates. Thus, (S)-2-amino-N-[[3-(2-naphthyl)-1-phenyl-1H-pyrazol-4-yl]methyl]-3-phenylpropanamide at 10 μM (preparation given) showed 86% inhibition against histamine binding to human recombinant H4 receptor expressed on CHO cells. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to naphthylpyrazole compound preparation histamine h4 receptor antagonist inflammation inhibitor, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 28, 2013, Wilson, Timothy R.; Koeppen, Hartmut; Merchant, Mark; Settleman, Jeffrey published a patent.SDS of cas: 924909-16-0 The title of the patent was Combinations comprising c-Met antagonists and B-raf antagonists for treatment of cancer. And the patent contained the following:

The invention provides combination therapies for treating a pathol. condition, such as cancer, wherein a c-met antagonist (e.g. crizotinib, tivantinib, anti-HGF antibody, onartuzumab) is combined with a B-raf antagonist (e.g. vemurafenib), thereby providing significant antitumor activity. C-met expression was inversely correlated with sensitivity to vemurafenib treatment. In one aspect, provided are methods for treating a cancer patient who has increased likelihood of developing resistance to B-raf antagonist comprising administering an effective amount (in combination) of B-raf antagonist and c-met antagonist. In addition, patients with B-raf mutant melanoma who had higher levels of circulating hepatocyte growth factor (HGF) showed substantially reduced progression free survival and overall survival when treated with B-raf antagonist, relative to patients with lower circulating HGF levels treated with B-raf antagonist. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).SDS of cas: 924909-16-0

The Article related to combination chemotherapy cmet antagonist braf inhibitor cancer treatment, gdc0712 preparation antitumor combination chemotherapy cmet braf drug target, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 13, 2007, Blake, James F.; Boyd, Steven Armen; Cohen, Frederick; De Meese, Jason; Fong, Kin Chiu; Gaudino, John J.; Kaplan, Tomas; Marlow, Allison L.; Seo, Jeongbeob; Thomas, Allen A.; Tian, Hongqi; Young, Wendy B. published a patent.Related Products of 924909-16-0 The title of the patent was Heterobicyclic pyrazole compounds as Met tyrosine kinase inhibitors and their preparation and use. And the patent contained the following:

The invention is related to the preparation of I and II [X = O, S, NH and derivatives; Z2, Z3 = independently CH and derivatives, N, wherein none or one of Z2, and Z3 = N; R1 = H, (un)substituted alk(en/yn)yl, (hetero)aryl, etc.; R2 = H, CF3, CN, SH and derivatives, SO2NH2 and derivatives, etc.; R3 = (un)substituted carbocyclyl, heterocyclyl, (hetero)/aryl] and their pharmaceutically acceptable salts which are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds I and II and their stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathol. conditions are disclosed. Thus, pyrazolopyridine III was prepared by a multi-step synthesis via 1-(4-methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol intermediate which was obtained from 1-(4-methoxybenzyl)-1H-pyrazol-5-amine and Meldrum’s acid. Certain I and II had IC50’s < 1 μM in a c-Met enzyme assay. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Related Products of 924909-16-0

The Article related to heterobicyclic pyrazole preparation tyrosine kinase inhibitor antiproliferative, pyrazolopyridine preparation met kinase inhibitor antitumor hyperproliferative disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On December 31, 2014, Goel, Neelima; Drabu, Sushma; Afzal, Obaid; Bawa, Sandhya published an article.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Antimicrobial screening and one-pot synthesis of 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives. And the article contained the following:

A series of 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives (4a-4k) were synthesized through direct reductive amination of 3-(naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde with various substituted aromatic amines using NaBH4 in the presence of I2 as reducing agent. The reaction was carried out in anhydrous methanol under neutral conditions at room temperature All 4-(substituted-anilinomethyl)-3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives (4a-4k) were tested in vitro for antifungal and antibacterial activities against different fungal and bacterial strains. Most of the compounds exhibited considerable antifungal activity, but poor antibacterial activity against the test strains. In the series compound 4e, 4g, 4j, and 4k, showed excellent antifungal activity against the fungal strain Aspergillus niger (MTCC) 281 and Aspergillus flavus MTCC 277 (% inhibition in the range of 47.7-58.9). The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to pyrazole naphthyl anilinomethyl preparation antibacterial antifungal, antimicrobial activity, naphthalene, pyrazole, reductive amination, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Xu, Li-Li; Zheng, Chang-Ji; Sun, Liang-Peng; Miao, Jing; Piao, Hu-Ri published an article in 2012, the title of the article was Synthesis of novel 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties as potential antibacterial agents.Electric Literature of 36640-53-6 And the article contains the following content:

In the present study, a series of 1,3-diarylpyrazole derivatives I [R = (un)substituted Ph, n = 1-5] bearing rhodanine-3-fatty acid moieties were synthesized and their antimicrobial activities were tested against various Gram-pos. and Gram-neg. bacteria. 1,3-Diaryl-4-formylpyrazoles were synthesized as key intermediates following a Vilsmeier-Haack strategy. Several compounds with an MIC of 2 μg/mL exhibited stronger antibacterial activity against the methicillin-resistant Staphylococcus aureus (MRSA) than the controls. None of the compounds showed any activity against Gram-neg. bacteria. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Electric Literature of 36640-53-6

The Article related to pyrazole aryl rhodanine derivative preparation antibacterial, thiazolidinone thioxodiarylpyrazolylmethylene preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Electric Literature of 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On April 20, 2017, Nicolaou, Kyriacos C.; Rhoades, Derek; Wang, Yanping; Totokotsopoulos, Sotirios published a patent.Category: pyrazoles-derivatives The title of the patent was Methods of synthesis, methods of treatment with, and drug conjugates of epothilone analogs. And the patent contained the following:

In one aspect, the present disclosure provides epothilone analogs I [wherein: X1 is absent, O or NRa; Ra is H, C≤8-alkyl, C≤8-cycloalkyl,(C≤6-alkyldiyl)-(C≤8-cycloalkyl), or a substituted version of either of these groups; provided that when X1 is absent, that the atoms to which it is attached are a part of a double bond;]. [X2, X3 and X4 are each independently O or NRb; wherein, Rb is H or C≤8-alkyl, C≤8-cycloalkyl, (C≤6-alkanediyl)-(C≤8-cycloalkyl), C≤b-aralkyl, or a substituted version of either of these groups;]. [Y1 and Y2 are each independently NH2, OH, or C≤8-alkoxy, C≤8-aralkoxy, C≤8-acyloxy, (C≤8-alkyl)amino, di(C≤8-alkyl)amino, C≤8-amido, or a substituted version of any of these groups, or ORc, wherein Rc is a hydroxy protecting group;]. [R1, R3, R4, R5, R6 and R7 are each independently H or C≤12-alkyl, C≤12-cycloalkyl, C≤12-alkenyl, C≤12-alkynyl, C≤12-aryl, or a substituted version of any of these groups; and,]. [R2 is C≤12-heteroaryl, C≤8-heteroarenediyl-Rd, or a substituted version of either of these groups; wherein Rd is C≤12-alkyl, C≤12-aryl, C≤12-aralkyl, C≤12-heteroaryl, C≤12-heteroaralkyl, or a substituted version of either of these groups;]. [Provided that R2 is not 2-methylthiazolyl, 2-(hydroxymethyl)thiazolyl, N-2-methyl-3- (methylthio)pyrazolyl or 2-(methylthio)thiazolyl;], or a pharmaceutically acceptable salt thereof. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Addnl., drug conjugates with cell targeting moieties of the compounds are also provided. Thus, epothilone B pyrazole analog II was prepared and tested for pharmacol. activity [EC50 = 19 μM for induction of tubulin assembly; GI50 = 14 nM vs. MCF-7 cell line; GI50 = 38 nM vs. OVCAR-8 cell line]. The experimental process involved the reaction of 5-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole(cas: 1187582-58-6).Category: pyrazoles-derivatives

The Article related to epothilone analogs preparation antitumor, antibody epothilone analog conjugate preparation cancer cell targeting, Biomolecules and Their Synthetic Analogs: Other Bacterial and Fungal Metabolites and other aspects.Category: pyrazoles-derivatives

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On June 30, 2015, Kamal, Raj; Kumar, Vipan; Bhardwaj, Vikas; Kumar, Vikas; Aneja, Kamal Rai published an article.Computed Properties of 36640-53-6 The title of the article was Synthesis, characterization and in vitro antimicrobial evaluation of some novel hydrazone derivatives bearing pyrimidinyl and pyrazolyl moieties as a promising heterocycles. And the article contained the following:

In the present investigation, ten new 2-((3-aryl-1-phenyl-1H-pyrazol-4-yl)methylene)-1-(4,6-dimethylpyrimidin-2-yl)hydrazines [I; Ar = (un)substituted Ph, 2-naphthyl] having pyrimidinyl and pyrazolyl moieties were synthesized. Structures of all compounds were confirmed by their spectral and elemental data. Most of the tested compounds were found to be significantly more effective against bacterial strains Staphylococcus aureus, Bacillus subtilis and Pseudomonas aeruginosa than the reference drug ciprofloxacin. All the newly synthesized compounds were found to be more potent antifungal agents than reference drug against Candida albicans, whereas except I (Ar = 4-nitrophenyl) all other compounds also shown good activity against Saccharomyces cerevisiae. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Computed Properties of 36640-53-6

The Article related to pyrimidinyl pyrazolyl hydrazone preparation bactericide fungicide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics