Synthesis and in vitro evaluation of novel tetralin‐pyrazolo[3,4‐<i>b</i>]pyridine hybrids as potential anticancer agents

Hamza, Eman; Hamdy, Nehal A.; Zarie, Eman S.; Fakhr, I. M. I.; Elwahy, Ahmed H. M.; Awad, Hanem M.

doi:10.1002/jhet.3764

Cited by 13 publications

(2 citation statements)

References 54 publications

(41 reference statements)

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“…Compounds 139(a-d) showed activity against HCT116 and compounds 140(a-d) showed activity against MCF-7 cancer cell lines. The structure of pyrazolo [3,4] pyridine hybrids is shown in Figure 127 and the in vitro IC50 (μM) of compounds [139(a-d),140(a-d)] against cancer cell lines is shown in Table 114 [204]. [3,4] pyridine hybrids as potential anticancer agents.…”

Section: Compoundmentioning

confidence: 99%

Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids

et al. 2022

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Cancer is a complex disease, and its treatment is a big challenge, with variable efficacy of conventional anticancer drugs. A two-drug cocktail hybrid approach is a potential strategy in recent drug discovery that involves the combination of two drug pharmacophores into a single molecule. The hybrid molecule acts through distinct modes of action on several targets at a given time with more efficacy and less susceptibility to resistance. Thus, there is a huge scope for using hybrid compounds to tackle the present difficulties in cancer medicine. Recent work has applied this technique to uncover some interesting molecules with substantial anticancer properties. In this study, we report data on numerous promising hybrid anti-proliferative/anti-tumor agents developed over the previous 10 years (2011–2021). It includes quinazoline, indole, carbazole, pyrimidine, quinoline, quinone, imidazole, selenium, platinum, hydroxamic acid, ferrocene, curcumin, triazole, benzimidazole, isatin, pyrrolo benzodiazepine (PBD), chalcone, coumarin, nitrogen mustard, pyrazole, and pyridine-based anticancer hybrids produced via molecular hybridization techniques. Overall, this review offers a clear indication of the potential benefits of merging pharmacophoric subunits from multiple different known chemical prototypes to produce more potent and precise hybrid compounds. This provides valuable knowledge for researchers working on complex diseases such as cancer.

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Section: Compoundmentioning

confidence: 99%

Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids

et al. 2022

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“…Hamza et al synthesized novel tetralin-pyrazolo[3,4- b ]pyridine hybrids and tested their in vitro cytotoxicity against HCT116 and MCF7 cells using MTT assay [ 117 ]. Compound 97 displayed the highest inhibition of MCF7 cells with an IC 50 value of 16.1 µM, while compound 98 demonstrated the most potent anticancer activity against HCT116 cells with an IC 50 value of 6.4 µM, compared to doxorubicin (IC 50 = 9.5 and 65.6 µM, respectively).…”

Section: Pyrazole Derivatives With Undefined Mechanismsmentioning

confidence: 99%

Recent Advances in the Development of Pyrazole Derivatives as Anticancer Agents

Zhang

et al. 2023

IJMS

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Pyrazole derivatives, as a class of heterocyclic compounds, possess unique chemical structures that confer them with a broad spectrum of pharmacological activities. They have been extensively explored for designing potent and selective anticancer agents. In recent years, numerous pyrazole derivatives have been synthesized and evaluated for their anticancer potential against various cancer cell lines. Structure–activity relationship studies have shown that appropriate substitution on different positions of the pyrazole ring can significantly enhance anticancer efficacy and tumor selectivity. It is noteworthy that many pyrazole derivatives have demonstrated multiple mechanisms of anticancer action by interacting with various targets including tubulin, EGFR, CDK, BTK, and DNA. Therefore, this review summarizes the current understanding on the structural features of pyrazole derivatives and their structure-activity relationships with different targets, aiming to facilitate the development of potential pyrazole-based anticancer drugs. We focus on the latest research advances in anticancer activities of pyrazole compounds reported from 2018 to present.

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Efficient synthesis and biological evaluation of some new series of pyridine derivatives: Promising and potent new class of anticancer agents

Abbas

Zeina

Radwan

et al. 2022

Journal of Heterocyclic Chem

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In an attempt to develop potent anticancer agents, we have synthesized some substituted pyridine derivatives. Alkylation of the pyridine-3-carbonitrile 1a by chloroacetonitrile or methyl iodide and ethyl iodide produced the O-alkylated nicotinonitrile derivatives (2-4), respectively. The reaction of nicotinonitrile 1a with acetic anhydride furnished the N-acetyl derivative 5. In addition, the reaction of 1a with concentrated sulfuric acid yielded compound 6 whereas its reaction with chloroacetone gave the corresponding 2-alkoxy-pyridine derivative 7 which then refluxed with sodium methoxide to give compound 8. Furthermore, alkylation of 1a-c with methyl bromoacetate and ethyl bromoacetate produced the corresponding methyl, ethyl ester derivatives 9,

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Synthesis and in vitro evaluation of novel tetralin‐pyrazolo[3,4‐b]pyridine hybrids as potential anticancer agents

Cited by 13 publications

References 54 publications

Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids

Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids

Recent Advances in the Development of Pyrazole Derivatives as Anticancer Agents

Efficient synthesis and biological evaluation of some new series of pyridine derivatives: Promising and potent new class of anticancer agents

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