Developing our knowledge of the quinolone scaffold and its value to anticancer drug design

Singh, Yogesh; Bhatia, Neha; Biharee, Avadh; Kulkarni, Swanand; Thareja, Suresh; Monga, Vikramdeep

doi:10.1080/17460441.2023.2246366

Expert Opinion on Drug Discovery

2023

DOI: 10.1080/17460441.2023.2246366

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Developing our knowledge of the quinolone scaffold and its value to anticancer drug design

Yogesh Singh,

Neha Bhatia,

Avadh Biharee

et al.

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2024

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Cited by 3 publications

References 63 publications

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Pyrazole, Pyrazoline, and Fused Pyrazole Derivatives: New Horizons in EGFR‐Targeted Anticancer Agents

Hosamani,

Pal

et al. 2024

Chemistry & Biodiversity

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Pyrazole and its derivatives remain popular heterocycles in drug design, and development. Pyrazole derivatives been extensively studied by the scientific community and as they possess a wide range of biological activity, especially anti‐EGFR properies. Overexpression of EGFR signaling promotes tumor growth by inhibiting apoptosis. EGFR dysfunction has been described in several cancer. Therefore, EGFR represents a prospective target for cancer treatment. Several anti‐EGFR drugs are thriving the market, notably dacomitinib, afatinib, erlotinib etc. However, almost all drugs have limited therapeutic effectiveness due to a lack of selectivity as well as substantial side effects. To address this, innovative therapeutic anti‐EGFR drugs with high effectiveness and low toxicity are needed. To combat therapeutic resistance to EGFR inhibitors, pyrazole, and pyrazole‐based derivatives have been explored as a promising pharmacophore for developing novel compounds with higher potency, lower toxicity, and desirable pharmacokinetic profiles. The current review outlines the investigation of advancements towards anti‐ EGFR via pyrazole, pyrazoline, and fused pyrazole‐based compounds and represents inclusive data on pyrazole‐based marketed drugs as well as therapeutic candidates undergoing preclinical and clinical development. We have also summarised structure‐activity relationship (SAR), mechanistic studies to afford ideas for the design and development of new anti‐EGFR derivatives.

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Pyrazole, Pyrazoline, and Fused Pyrazole Derivatives: New Horizons in EGFR‐Targeted Anticancer Agents

Hosamani,

Pal

et al. 2024

Chemistry & Biodiversity

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Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance

Zang,

Wang,

Battini

et al. 2024

European Journal of Medicinal Chemistry

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Quinolone Derivatives as Anticancer Agents: Importance in Medicinal Chemistry

Azzman,

Anwar,

Syazani Mohamed

et al. 2024

CTMC

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Abstract:: Quinolone is a heterocyclic compound containing carbonyl at the C-2 or C-4 positions with nitrogen at the C-1 position. The scaffold was first identified for its antibacterial properties, and the derivatives were known to possess many pharmacological activities, including anticancer. In this review, the quinolin-2(H)-one and quinolin-4(H)-one derivatives were identified to inhibit several various proteins and enzymes involved in cancer cell growth, such as topoisomerase, mi-crotubules, protein kinases, phosphoinositide 3-kinases (PI3K) and histone deacetylase (HDAC). Hybrids of quinolone with curcumin or chalcone, 2-phenylpyrroloquinolin-4-one and 4-quinolone derivatives have demonstrated strong potency against cancer cell lines. Additionally, quinolones have been explored as inhibitors of protein kinases, including EGFR and VEGFR. Therefore, this review aims to consolidate the medicinal chemistry of quinolone derivatives in the pipeline and discuss their similarities in terms of their pharmacokinetic profiles and potential target sites to provide an understanding of the structural requirements of anticancer quinolones.

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Developing our knowledge of the quinolone scaffold and its value to anticancer drug design

Cited by 3 publications

References 63 publications

Pyrazole, Pyrazoline, and Fused Pyrazole Derivatives: New Horizons in EGFR‐Targeted Anticancer Agents

Pyrazole, Pyrazoline, and Fused Pyrazole Derivatives: New Horizons in EGFR‐Targeted Anticancer Agents

Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance

Quinolone Derivatives as Anticancer Agents: Importance in Medicinal Chemistry

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