Discovery of novel pyrazole and pyrazolo[1,5‐a]pyrimidine derivatives as cyclooxygenase inhibitors (COX‐1 and COX‐2) using molecular modeling simulation
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200395
Abstract: Searching for effective and selective anti‐inflammatory agents, our study involved designing and synthesizing new pyrazole and pyrazolo[1,5‐a]pyrimidine derivatives 4–11. The structures of the synthesized derivatives were confirmed using different spectroscopic techniques. Virtual screening was achieved… read more here.
Keywords: pyrazole pyrazolo; cox; pyrazolo pyrimidine; cox cox ... See more keywords
Pyrazolo[3,4‐d]pyrimidine scaffold: A review on synthetic approaches and EGFR and VEGFR inhibitory activities
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DOI: 10.1002/ardp.202200424
Abstract: The pyrazolo[3,4‐d]pyrimidine core has received a lot of interest from the medicinal chemistry community as a promising framework for drug design and discovery. It is an isostere of the adenine ring of adenosine triphosphate, which… read more here.
Keywords: scaffold review; pyrimidine scaffold; pyrazolo pyrimidine; review synthetic ... See more keywords
Design, synthesis, and biological evaluation of a potent PLK4 inhibitor WY29 with 1H‐pyrazolo[3,4‐d]pyrimidine scaffold
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200490
Abstract: Centriole duplication occurs once per cell cycle and is regulated by Polo‐like kinase 4 (PLK4). Overexpression of PLK4 in somatic cells can lead to the excessive formation of centrioles, directly causing chromosome segregation errors and… read more here.
Keywords: compound; wy29; pyrazolo pyrimidine; plk4 ... See more keywords
In vitro enzymatic evaluation of some pyrazolo[1,5‐a]pyrimidine derivatives: Design, synthesis, antioxidant, anti‐diabetic, anti‐Alzheimer, and anti‐arthritic activities with molecular modeling simulation
Sign Up to like & getrecommendations! Published in 2022 at "Drug Development Research"
DOI: 10.1002/ddr.22008
Abstract: The strategy of utilizing nitrogen compounds in various biological applications has recently emerged as a powerful approach to exploring novel classes of therapeutics to face the challenge of diseases. A series of pyrazolo[1,5‐a]pyrimidine‐based compounds 3a–l… read more here.
Keywords: anti alzheimer; pyrazolo pyrimidine; anti diabetic; diabetic anti ... See more keywords
Synthesis of androsteno[17,16-d]pyrazoles and androsteno[17,16-d]-2′-pyrazolines with pyrazolo[3,4-d]pyrimidine fragments
Sign Up to like & getrecommendations! Published in 2018 at "Russian Chemical Bulletin"
DOI: 10.1007/s11172-018-2185-5
Abstract: Reactions of pyrazolo[3,4-d]pyrimidine-containing hydrazines with pregnenolone derivatives were studied. The reaction of 16α,17α-epoxy-3β-hydroxy-5-pregnen-20-one and its 3-O-acetyl derivative with 6-hydrazino-3,4-dimethyl-1H-pyrazolo[3,4-d]pyrimidine and 4-hydrazino-3-methyl-6-phenyl-1H-pyrazolo[3,4-d]pyrimidine afforded new androsteno[17,16-d]pyrazoles with pyrazolo[3,4-d]pyrimidine fragments. The reaction of 3β-hydroxypregna-5,16-dien-20-one and its 3-O-acetyl derivative… read more here.
Keywords: pyrimidine; pyrimidine fragments; pyrazolo pyrimidine; androsteno pyrazoles ... See more keywords
Synthesis and biological evaluation of 7-(aminoalkyl)pyrazolo[1,5-a]pyrimidine derivatives as cathepsin K inhibitors.
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DOI: 10.1016/j.bioorg.2018.11.029
Abstract: A series of novel 7-aminoalkyl substituted pyrazolo[1,5-a]pyrimidine derivatives were synthesized and tested for inhibition of cathepsin K. The synthetic methodology comprises cyclization of 5-aminopyrazoles with N-Boc-α-amino acid-derived ynones followed by transformation of the ester and… read more here.
Keywords: biological evaluation; pyrimidine derivatives; pyrimidine; pyrazolo pyrimidine ... See more keywords
Acid Derivatives of Pyrazolo[1,5-a]pyrimidine as Aldose Reductase Differential Inhibitors.
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DOI: 10.1016/j.chembiol.2018.07.008
Abstract: Aldose reductase (AKR1B1), the key enzyme of the polyol pathway, plays a crucial role in the development of long-term complications affecting diabetic patients. Nevertheless, the expedience of inhibiting this enzyme to treat diabetic complications has… read more here.
Keywords: reductase; differential inhibitors; aldose reductase; pyrazolo pyrimidine ... See more keywords
Floro-pyrazolo[3,4-d]pyrimidine derivative as a novel plant activator induces two-pathway immune system.
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DOI: 10.1016/j.phytochem.2021.112657
Abstract: Plants are known to develop a multi-faceted innate immune system for pathogenic defense. Systemic acquired resistance (SAR) and induced systemic resistance (ISR) are the two main pathways. Many chemical inducers known as plant activators that… read more here.
Keywords: immune system; resistance; pyrazolo pyrimidine; plant ... See more keywords
A novel solid-phase synthetic method for production of N-alkyl-4-alkylamino-1-aryl-1H-pyrazolo[3,4-d]pyrimidine-6-carboxamide library
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DOI: 10.1016/j.tet.2017.08.044
Abstract: Abstract This work describes a solid-phase synthetic method for building a compound library of N -alkyl-4-alkylamino-1-aryl-1 H -pyrazolo[3,4- d ]pyrimidine-6-carboxamide derivatives, that are based on the biologically active 1-aryl-1 H -pyrazolo[3,4- d ]pyrimidine scaffold. In… read more here.
Keywords: aryl pyrazolo; phase; pyrazolo pyrimidine; solid phase ... See more keywords
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-a]pyrimidine-Based Macrocycles.
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DOI: 10.1021/acs.jmedchem.2c00173
Abstract: Serine/threonine kinase 17A (death-associated protein kinase-related apoptosis-inducing protein kinase 1─DRAK1) is a part of the death-associated protein kinase (DAPK) family and belongs to the so-called dark kinome. Thus, the current state of knowledge of the… read more here.
Keywords: threonine kinase; pyrazolo pyrimidine; kinase 17a; kinase ... See more keywords
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b00359
Abstract: Inhibition of the protein-protein interaction between B-cell lymphoma 6 (BCL6) and corepressors has been implicated as a therapeutic target in diffuse large B-cell lymphoma (DLBCL) cancers and profiling of potent and selective BCL6 inhibitors are… read more here.
Keywords: lymphoma bcl6; pyrazolo pyrimidine; bcl6 binders; cell ... See more keywords