WELPSA: A Green Catalyst Mediated Microwave Assisted Efficient Synthesis of Novel 5‐Aminopyrazole‐4‐Carbonitrile Derivatives as Anticancer Agents (MCF‐7, A‐549) and In Silico Studies DOI
Aravind R. Nesaragi, Vinuta Kamat, Sharanappa Chapi

et al.

Archiv der Pharmazie, Journal Year: 2025, Volume and Issue: 358(4)

Published: April 1, 2025

ABSTRACT Malononitrile, modified hydrazine, and quinoline aldehyde were combined in a one‐pot reaction under microwave irradiation to create the medicinally significant family of heterocyclic scaffolds, quinoline, coumarin, thiazole, pyrazole 4‐carbonitrile derivatives with help green solvent as water. WELPSA (water extract lemon peel‐soaked ash) is used speed up solvent‐free environment, according more environmentally friendly protocols. This methodology offers several advantages like short duration, synthesis, high yield, no need for chromatographic techniques, catalyst recyclability five cycles, so on. Synthesized evaluated anticancer potential against lung (A549) breast cancer cell lines. Among tested compounds, 4i 4j exhibited remarkable activities. Further investigations using Annexin V staining flow cytometry revealed that both compounds effectively induced apoptosis A549 cells. Compound was subjected molecular docking dynamic studies understand basis their activity, which demonstrated strong interaction target protein 1m17, providing insights into its mechanism action. These findings highlight promising candidates drug development.

Language: Английский

Imidazole‐Centred Oxadiazole Sensor for Detecting Al3+ and Fe3+ Cations in Living Cells: A Zebrafish Bioimaging Approach DOI
Aravind R. Nesaragi,

Bi Bi Ayisha Mulla,

Sharanappa Chapi

et al.

Applied Organometallic Chemistry, Journal Year: 2025, Volume and Issue: 39(4)

Published: March 9, 2025

ABSTRACT This study introduces a novel organic fluorescent chemosensor, designated as imidazole 4‐(1‐(4‐(5‐(4‐( tert ‐butyl)phenyl)‐1,3,4‐oxadiazol‐2‐yl)phenyl)‐1 H ‐phenanthro[9,10‐ d ]imidazol‐2‐yl)‐N,N‐diphenylaniline ( TIMTB ). Engineered specifically for detecting aluminium (Al 3+ ) and iron (Fe ions, demonstrates exceptional selectivity, rapid response times, efficacy in complex matrices such biological fluids environmental samples. Comprehensive evaluations through UV absorption, fluorescence spectroscopy, pH‐dependent studies confirm 's high sensitivity selectivity towards Al Fe . Further, the was supported by Density Functional Theory (DFT) studies. , synthesized with an imidazole‐oxadiazole core, exhibited significantly low cytotoxicity (14 ± 0.15 μM). In aqueous ethanol medium, probe achieved notably detection limits of 2 nM 2.19 μM Minimal observed both in‐vitro (MDA‐MB‐231 cells) in‐vivo (zebrafish, Danio rerio studies, paving way its application tracing intracellular ions zebrafish embryos. robust performance underscores potential invaluable tool monitoring biomedical applications.

Language: Английский

Citations

1
WELPSA: A Green Catalyst Mediated Microwave Assisted Efficient Synthesis of Novel 5‐Aminopyrazole‐4‐Carbonitrile Derivatives as Anticancer Agents (MCF‐7, A‐549) and In Silico Studies DOI
Aravind R. Nesaragi, Vinuta Kamat, Sharanappa Chapi

et al.

Archiv der Pharmazie, Journal Year: 2025, Volume and Issue: 358(4)

Published: April 1, 2025

ABSTRACT Malononitrile, modified hydrazine, and quinoline aldehyde were combined in a one‐pot reaction under microwave irradiation to create the medicinally significant family of heterocyclic scaffolds, quinoline, coumarin, thiazole, pyrazole 4‐carbonitrile derivatives with help green solvent as water. WELPSA (water extract lemon peel‐soaked ash) is used speed up solvent‐free environment, according more environmentally friendly protocols. This methodology offers several advantages like short duration, synthesis, high yield, no need for chromatographic techniques, catalyst recyclability five cycles, so on. Synthesized evaluated anticancer potential against lung (A549) breast cancer cell lines. Among tested compounds, 4i 4j exhibited remarkable activities. Further investigations using Annexin V staining flow cytometry revealed that both compounds effectively induced apoptosis A549 cells. Compound was subjected molecular docking dynamic studies understand basis their activity, which demonstrated strong interaction target protein 1m17, providing insights into its mechanism action. These findings highlight promising candidates drug development.

Language: Английский

Citations

0