Novel thiazole-based cyanoacrylamide derivatives: DNA cleavage, DNA/BSA binding properties and their anticancer behaviour against colon and breast cancer cells

BMC Chemistry, Journal Year: 2024, Volume and Issue: 18(1)

Published: Sept. 20, 2024

Language: Английский

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Bioactive Fused Pyrazoles Inspired by the Adaptability of 5-Aminopyrazole Derivatives: Recent Review

Molecules, Journal Year: 2025, Volume and Issue: 30(2), P. 366 - 366

Published: Jan. 17, 2025

Heterocyclic compounds, especially those containing the pyrazole moiety, are highly significant in organic chemistry and possess remarkable diverse biological properties. The 5-aminopyrazole derivatives key starting materials for synthesis of numerous bioactive compounds such as pyrazolopyridine, pyrazolopyrimidine, pyrazoloquinazoline, pyrazolotriazine derivatives. Many inspired by a wide spectrum activities medicinal applications antioxidants, anticancer agents, enzyme inhibitors, antimicrobials, anti-tuberculosis activities. This review summarizes recently reported methods fused pyrazole-based based on within last 5 years (2020 to present). One important goals this is illustrate future strategies design, development, utilization products potent drugs.

Language: Английский

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Bruceine a exerts antitumor effect against colon cancer by accumulating ROS and suppressing PI3K/Akt pathway

Frontiers in Pharmacology, Journal Year: 2023, Volume and Issue: 14

Published: March 28, 2023

Bruceine A (BA), a quassic ester from bruceine javanica, regulates diverse intracellular signal transduction pathways and manifests variety of biological activities, however, its pharmacological mechanism in treating colon cancer (CC) is unclear. In this study, we investigated the anticancer effects BA on CC cells underlying mechanisms. The network pharmacology research indicated that Akt1 Jun PI3K/Akt are predominant targets critical signaling pathways, respectively, for treatment CC. Meanwhile, molecular docking results implied could conjugate to pivotal proteins pathway. remarkably suppressed proliferation HCT116 CT26 with 48-h IC50 26.12 229.26 nM, expression p-PI3K/p-Akt was restrained by at level as verified Western blot assay. Further mechanistic studies revealed impacted cell cycle-related regulating P27 (a protein bridging pathway proteins), arresting cycle G2 phase, inhibiting CT26, facilitated apoptosis activating mitochondria-associated Bax accumulating reactive oxygen species, addition apparently inhibited migration cells. Taken together, our demonstrated might be promising chemotherapy drug

Language: Английский

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Design, Synthesis and Characterization of New Fused Pyrazole Systems: In Vitro Anti-bacterial, Anti-fungal, Antioxidant Evaluation, In Silico DFT and Molecular Docking Studies

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 142163 - 142163

Published: March 1, 2025

Language: Английский

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One‐Pot Synthesis of Styryl‐Linked Polycyclic‐Fused Pyridine Derivatives by a Multicomponent Strategy

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(17)

Published: April 28, 2025

Abstract In the present study, new styryl‐linked pyridine derivatives fused with pyrazole were synthesized by one‐pot reaction of α, β‐ unsaturated aldehyde, cyclic‐1,3‐diketone, and 5‐aminopyrazole in DMSO at 100 °C an open air. All products characterized FTIR, 1 H NMR, 13 C HRMS. Single crystal XRD one product 4i was done to confirm structure. 2C─C 1C─N bonds are formed one‐pot. Various bioactive moieties such as pyridine, pyrazole, styryl our hybrid heterocyclic scaffold. This methodology is also applicable gram‐scale synthesis. Operational simplicity, greener condition, good yields products, easy purification process notable features this methodology.

Language: Английский

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Silver(I) triflate-catalyzed post-Ugi synthesis of pyrazolodiazepines

Beilstein Journal of Organic Chemistry, Journal Year: 2025, Volume and Issue: 21, P. 915 - 925

Published: May 8, 2025

A silver(I) triflate-catalyzed post-Ugi assembly of novel pyrazolo[1,5- a ][1,4]diazepine scaffolds is reported offering high yields (up to 98%) under mild conditions. The synthetic sequence involves the Ugi four-component reaction (U4CR) pyrazole-3-carbaldehydes, primary amines, 3-substituted propiolic acids, and isocyanides, followed by intramolecular heteroannulation resulting pyrazole-tethered propargylamides occurring in 7- endo - dig fashion. approach scalable tolerates diverse range substitution patterns.

Language: Английский

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Synthesis, activity, docking and dynamic simulation studies of novel pyrazolo-pyrano[2,3-d]-pyrimidine analogues as anti-diabetic agents

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1305, P. 137720 - 137720

Published: Feb. 7, 2024

Language: Английский

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Synthesis, in vitro α‐Glucosidase Inhibition, DFT Calculations, and Molecular Docking Studies of Some New Substituted 2,5‐Bis(pyrazolyl)‐1,3,4‐oxadiazoles

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(9)

Published: Feb. 28, 2024

Abstract A pivotal feature of present research study is the synthesis some new 2,5‐bis(pyrazolyl)‐1,3,4‐oxadiazoles as promising α‐glucosidase inhibitors. In this regard, a facile reaction scheme was designed to afford 1,3,4‐oxadiazole ring. search most favourable condition, model first carried out between 1,3‐diphenyl‐1 H ‐pyrazole‐4‐carbohydrazide ( 3 ) and ‐pyrazole‐4‐carboxylic acid 4 using phosphorous oxychloride (POCl ). The results emanated from were utilized prepare other derivatives highlight scope current synthetic approach structures prepared molecules characterized spectroscopic techniques. These further investigated for their inhibitory potentials. 2,5‐Bis(1,3‐diphenyl‐1 ‐pyrazol‐4‐yl)‐1,3,4‐oxadiazole 5 2‐(3‐(4‐bromophenyl)‐1‐phenyl‐1 ‐pyrazol‐4‐yl)‐5‐(1,3‐diphenyl‐1 c displayed strong in vitro activities with IC 50 73.1±1.13 μM 87.3±1.12 respectively least toxicity profiles. Molecular docking computational studies including geometry optimization synthesized molecular systems, calculations orbital energies, electrostatic potential (MEP) surface maps helped establish structural electronic properties contributing towards bioactivity. electrophilicity index significantly quantifies biological activity. experimental data altogether facilitated understanding therapeutic attributes these versatile scaffolds relation inhibition.

Language: Английский

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Structure–Activity Relationship Studies on Highly Functionalized Pyrazole Hydrazones and Amides as Antiproliferative and Antioxidant Agents

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(9), P. 4607 - 4607

Published: April 23, 2024

Aminopyrazoles represent interesting structures in medicinal chemistry, and several derivatives showed biological activity different therapeutic areas. Previously reported 5-aminopyrazolyl acylhydrazones amides relevant antioxidant anti-inflammatory activities. To further extend the structure–activity relationships this class of derivatives, a novel series pyrazolyl was designed prepared through divergent approach. The compounds shared phenylamino pyrazole nucleus that differently decorated at positions 1, 3, 4. antiproliferative, antiaggregating, properties obtained 10–22 were evaluated vitro assays. Derivative 11a antitumor against selected tumor cell lines (namely, HeLa, MCF7, SKOV3, SKMEL28) with micromolar IC50 values. In platelet assay, pyrazoles higher ROS formation inhibition than reference drugs acetylsalicylic acid N-acetylcysteine. Furthermore, radical scavenging screening confirmed good acylhydrazone molecules. Overall, collected data allowed us to previously pharmaceutical attractiveness aminopyrazole derivatives.

Language: Английский

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Synthesis and Characterization of New Bases Derived from Nitrophenylpyrazoles, Coordination to Palladium and Antifungal Activity and Catalytic Activity in Mizoroki–Heck Reactions

Catalysts, Journal Year: 2024, Volume and Issue: 14(6), P. 387 - 387

Published: June 16, 2024

In this study, we report the synthesis of eight Schiff bases (3–10) type N-heterocycle (N-het) using conventional refluxing conditions as well different eco-friendly techniques such grinding, thermal fusion, microwave irradiation (MWI) and ultrasound, all them in presence a catalytic amount acetic acid. These procedures had additional advantage being environmentally friendly high-yield, making these protocols an alternative for Schiff-base syntheses. The obtained were coordinated to palladium, generating new complexes [Pd2Cl4(N-het)2]. Complexes [Pd2Cl4(5)2] [Pd2Cl4(9)2] showed high activity selectivity model Mizoroki–Heck C-C coupling reaction styrene with iodobenzene bromobenzaldehydes. All compounds evaluated antifungal against clinically important fungi Candida albicans Cryptococcus neoformans. Although low both fungi, some their palladium [Pd2Cl4(3)2], [Pd2Cl4(5)2], [Pd2Cl4(8)2] [Pd2Cl4(10)2] comparatively higher effects mainly C. product Mizoroki–Heck-type reactions, 4-styrylbenzaldehyde, was isolated purified be later used four nitrophenylpyrazole derivatives styrylimine, which also displayed activity, especially

Language: Английский

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