In-vitro and in-silico pharmacological profiling of 3-(4,5-diaryl-1H-imidazol-2-yl)quinoline-2-amine hybrids DOI Creative Commons
Nagarjuna Prakash Dalbanjan, Lokesh Bheemayya, Arihant Jayawant Kadapure

и другие.

Опубликована: Апрель 1, 2025

From Infection to Tumor: Exploring the Therapeutic Potential of Ciprofloxacin Derivatives as Anticancer Agents DOI Creative Commons

Hesham M. Hassan,

Roket Hassan,

Ranya Mohammed Elmagzoub

и другие.

Pharmaceuticals, Год журнала: 2025, Номер 18(1), С. 72 - 72

Опубликована: Янв. 9, 2025

Ciprofloxacin, a widely used second-generation fluoroquinolone for treating bacterial infections, has recently shown notable anticancer properties. This review explores progress in developing ciprofloxacin derivatives with properties, emphasizing key structural changes that improve their therapeutic effectiveness by modifying the basic group at position 7, carboxylic acid 3, or both. It further investigates mechanisms which these fight cancer, such as inducing apoptosis, arresting cell cycle, inhibiting topoisomerase I and II, preventing tubulin polymerization, suppressing interleukin 6, blocking thymidine phosphorylase, multidrug resistance proteins, hindering angiogenesis. Additionally, it outlines future directions, enhancing efficacy, selectivity, investigating potential synergy other chemotherapeutic agents, offering promising avenue new therapies cancer.

Язык: Английский

Процитировано

0

Biochemical and Computational Insights into the Therapeutic Potencies of Quinoline Appended Imidazole Compounds DOI
Nagarjuna Prakash Dalbanjan, Lokesh Bheemayya,

Karuna Korgaonkar

и другие.

ChemistrySelect, Год журнала: 2025, Номер 10(14)

Опубликована: Апрель 1, 2025

Abstract Diabetes is a complex metabolic disorder characterized by oxidative stress and chronic inflammation, necessitating the development of multifunctional therapeutic agents. This study evaluates in vitro silico antihyperglycemic, antioxidant, anti‐inflammatory activities four 3‐(4,5‐diaryl‐1 H ‐imidazol‐2‐yl)quinoline‐2‐amine derivatives (a–d) . Among them, compound (a) exhibited strong antihyperglycemic activity, with significant α‐amylase inhibition (IC 50 = 132.55 ± 4.12 µg/mL) enhanced glucose uptake yeast cells 126.32 3.48 µg/mL). Compound (d) showed superior antioxidant 42–44 properties. Molecular docking against PPAR‐γ confirmed binding interactions for all compounds, showing collectively better affinity (−10 kcal/mol −11.1 kcal/mol). Further, molecular dynamics normal mode analysis validated its stability functional potential. The ADMET predictions suggested favorable pharmacokinetics, especially compounds (b) findings suggest that has potential as lead molecule treatment moderate also shows promise, albeit slightly lower bioactivity. Despite these promising findings, none tested outperformed efficacy standard drugs any assays, indicating need further structural optimization to enhance their

Язык: Английский

Процитировано

0

In-vitro and in-silico pharmacological profiling of 3-(4,5-diaryl-1H-imidazol-2-yl)quinoline-2-amine hybrids DOI Creative Commons
Nagarjuna Prakash Dalbanjan, Lokesh Bheemayya, Arihant Jayawant Kadapure

и другие.

Опубликована: Апрель 1, 2025

Процитировано

0