Novel pyrazolo[3,4‐b]pyridine derivatives: Synthesis, structure–activity relationship studies, and regulation of the AMPK/70S6K pathway
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DOI: 10.1002/ardp.202100465
Abstract: A series of novel pyrazolo[3,4‐b]pyridine derivatives were designed, synthesized, and biologically evaluated for anti‐lung cancer activity. Structure–activity relationship and AutoGPA models were constructed based on the in vitro antiproliferative potency of the compounds against a… read more here.
Keywords: novel pyrazolo; structure activity; pyrazolo pyridine; pyridine derivatives ... See more keywords
Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111714
Abstract: In our continuing efforts to find novel anti-HIV compounds, we have synthesized sixteen novel pyrazolo[4,3-c]pyridin-4-one derivatives. All the synthesized compounds were screened for anti-HIV activity against HIV-1VB59 (R5, subtype C). Compounds 12a-12c and 12e were… read more here.
Keywords: pyrazolo pyridin; one derivatives; hiv; pyridin one ... See more keywords
Discovery of Novel Pyrazolo-Pyridone DCN1 Inhibitors Controlling Cullin Neddylation.
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DOI: 10.1021/acs.jmedchem.9b00410
Abstract: Chemical control of cullin neddylation is attracting increased attention based largely on the successes of the NEDD8-activating enzyme (E1) inhibitor Pevonedistat. Recently reported chemical probes enable selective and time-dependent inhibition of downstream members of the… read more here.
Keywords: pyrazolo pyridone; cullin neddylation; discovery novel; dcn1 ... See more keywords
Design, synthesis and antitumor evaluation of novel pyrazolo[3,4-d]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibitors
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DOI: 10.1080/14756366.2022.2142786
Abstract: Abstract The present study aimed to investigate the antitumor effect of simultaneous inhibition of dihydrofolate reductase (DHFR) enzyme. We designed some novel pyrazolo[3,4-d]pyrimidines bearing different amino acid conjugates as efficient antifolate agents attributable to their… read more here.
Keywords: novel pyrazolo; compound; antitumor; amino acid ... See more keywords
A Novel Pyrazolo[3,4-d]pyrimidine Induces Heme Oxygenase-1 and Exerts Anti-Inflammatory and Neuroprotective Effects
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DOI: 10.14348/molcells.2021.0074
Abstract: The anti-oxidant enzyme heme oxygenase-1 (HO-1) is known to exert anti-inflammatory effects. From a library of pyrazolo[3,4-d]pyrimidines, we identified a novel compound KKC080096 that upregulated HO-1 at the mRNA and protein levels in microglial BV-2… read more here.
Keywords: kkc080096 upregulated; novel pyrazolo; pyrazolo pyrimidine; anti inflammatory ... See more keywords
Synthesis, Characterization, and Biological Evaluation of Some Novel Pyrazolo[5,1-b]thiazole Derivatives as Potential Antimicrobial and Anticancer Agents
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DOI: 10.3390/molecules26175383
Abstract: The pharmacological activities of thiazole and pyrazole moieties as antimicrobial and anticancer agents have been thoroughly described in many literature reviews. In this study, a convenient synthesis of novel pyrazolo[5,1-b]thiazole-based heterocycles was carried out. The… read more here.
Keywords: antimicrobial anticancer; anticancer agents; pyrazolo thiazole; novel pyrazolo ... See more keywords