3‐Amino‐1<i>H</i>‐pyrazolopyridine Derivatives as a Maternal Embryonic Leucine Zipper Kinase Inhibitor

Park, Chul Min; Jadhav, Vithal B.; Song, Jong-Hwan; Lee, Jimin; Won, Hee Young; Choi, Sang Un; Son, You Hwa

doi:10.1002/bkcs.11129

Cited by 5 publications

(3 citation statements)

References 19 publications

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“…Thus, MELK can be considered as a crucial target for cancer treatment. In view of this, Park et al designed and synthesized piperidine-bearing pyrazolopyridine scaffolds as potent MELK inhibitors (Park et al, 2017). An excellent anti-MELK profile has been noticed for evaluated molecules.…”

Section: Pyridine/piperidine Derivativesmentioning

confidence: 99%

Pyrazolopyridine: An efficient pharmacophore in recent drug design and development

Dorababu¹

2022

Chem Biol Drug Des

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Among the various heterocyclic molecules employed for drug design and discovery, pyrazolopyridine is one of the promising pharmacophores. Pyrazolopyridine is a result of fusion of pyrazole and pyridine rings. The potent pharmacology of pyrazolopyridine may be the synergistic effect of pyrazole and pyridine moieties in a single framework. It has been used in drug design of a wide range of diseases such as anticancer, antimicrobial, anti‐inflammatory, and neuroprotection. Cancer has become a common disease among elderly people now a days that might be because of genetic inheritance to some extent, carcinogens, pollution, and some infectious diseases. Whatever may be the reason, cancer is one of the major causes of deaths worldwide. In addition, over‐usage and improper usage of antibiotics have led to drug resistance of microbes. Further, inflammation is a cause of various diseases such as arthritis, and other diseases. Thus, proinflammatory kinases are considered as primary target for inhibition of inflammation. In view of this, a work that compiles potent pharmacology of recently reported pyrazolopyridine analogs has been planned. The review is aimed to discuss pharmacology in brief along with structure–activity relationship (SAR). The review would emphasize importance of pyrazolopyridines in future drug design and discovery and may help in design of potent pharmacological agents.

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Section: Pyridine/piperidine Derivativesmentioning

confidence: 99%

Pyrazolopyridine: An efficient pharmacophore in recent drug design and development

Dorababu¹

2022

Chem Biol Drug Des

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“…Moreover, pyrazolopyridine-derived drug molecules exhibit anti-cancer properties (Huang et al, 2007;Ye et al, 2009). They are inhibitors of several important proteins, namely cyclinedependent kinase1, HIV reverse transcriptase, leucine zipper kinase, protein kinase, xanthine oxidase, interleukin-6 (IL-6), tumor necrosis factor alpha (TNF-), phosphodiesterase-4, NAD(P)H oxidases (Kumar et al, 2019;Gö khan-Kelekçi et al, 2007;Fathy et al, 2015;Park et al, 2017). A recent study reported that they could be promising inhibitors against the enzyme pantothenate synthetase from Mycobacterium tuberculosis (Amaroju et al, 2017).…”

Section: Chemical Contextmentioning

confidence: 99%

Crystal structure analysis of ethyl 6-(4-methoxyphenyl)-1-methyl-4-methylsulfanyl-3-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylate

2020

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“…For instance, 6-(3,5-dimethoxyphenyl)-3-(4-fluorophenyl)-1H-pyrazolo [3,4-b]pyridine (APcK110) is an extensively researched Kit kinase inhibitor [32][33][34]. More recently, various 1H-pyrazolo [3,4b]pyridine derivatives were reported as potent ALK-L1196M [35] and CDK8 inhibitors [36], PPARα agonists [37], and antimicrobial, anti-quorum-sensing, and anticancer agents [38], while 3-amino-1H-pyrazolo [3,4-b]pyridine core was identified as a novel scaffold for MELK kinase inhibitors [39]. 2-{[2-(1H-Pyrazolo [3,4-c]pyridin-3-yl)-6-(trifluoromethyl)pyrimidin-4-yl]amino}ethanol is a bacterial DNA ligase inhibitor [40], several compounds bearing 1H-pyrazolo [4,3-b]pyridin-3-amine scaffold act as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu 4 ) [41,42], 3-phenylpyrazolo [3,4-c]pyridines were reported to possess antiproliferative activity [43], and 1-(4-methoxybenzyl)-7-(4methylpiperazin-1-yl)-N-[4-(4-methylpiperazin-1-yl)phenyl]-3-phenyl-1H-pyrazolo [3,4c]pyridin-5-amine was suggested as potential angiogenesis inhibitor [44].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antiproliferative Activity of 2,4,6,7-Tetrasubstituted-2H-pyrazolo[4,3-c]pyridines

et al. 2021

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A library of 2,4,6,7-tetrasubstituted-2H-pyrazolo[4,3-c]pyridines was prepared from easily accessible 1-phenyl-3-(2-phenylethynyl)-1H-pyrazole-4-carbaldehyde via an iodine-mediated electrophilic cyclization of intermediate 4-(azidomethyl)-1-phenyl-3-(phenylethynyl)-1H-pyrazoles to 7-iodo-2,6-diphenyl-2H-pyrazolo[4,3-c]pyridines followed by Suzuki cross-couplings with various boronic acids and alkylation reactions. The compounds were evaluated for their antiproliferative activity against K562, MV4-11, and MCF-7 cancer cell lines. The most potent compounds displayed low micromolar GI50 values. 4-(2,6-Diphenyl-2H-pyrazolo[4,3-c]pyridin-7-yl)phenol proved to be the most active, induced poly(ADP-ribose) polymerase 1 (PARP-1) cleavage, activated the initiator enzyme of apoptotic cascade caspase 9, induced a fragmentation of microtubule-associated protein 1-light chain 3 (LC3), and reduced the expression levels of proliferating cell nuclear antigen (PCNA). The obtained results suggest a complex action of 4-(2,6-diphenyl-2H-pyrazolo[4,3-c]pyridin-7-yl)phenol that combines antiproliferative effects with the induction of cell death. Moreover, investigations of the fluorescence properties of the final compounds revealed 7-(4-methoxyphenyl)-2,6-diphenyl-2H-pyrazolo[4,3-c]pyridine as the most potent pH indicator that enables both fluorescence intensity-based and ratiometric pH sensing.

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3‐Amino‐1H‐pyrazolopyridine Derivatives as a Maternal Embryonic Leucine Zipper Kinase Inhibitor

Cited by 5 publications

References 19 publications

Pyrazolopyridine: An efficient pharmacophore in recent drug design and development

Pyrazolopyridine: An efficient pharmacophore in recent drug design and development

Crystal structure analysis of ethyl 6-(4-methoxyphenyl)-1-methyl-4-methylsulfanyl-3-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylate

Synthesis and Antiproliferative Activity of 2,4,6,7-Tetrasubstituted-2H-pyrazolo[4,3-c]pyridines

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