Synthesis, biological evaluation, and in silico studies of phenyl naphthalene-2-sulfonate derived thiosemicarbazones as potential carbonic anhydrase inhibitors

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 155, P. 108118 - 108118

Published: Jan. 4, 2025

Language: Английский

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Novel benzenesulfonamide derivatives as potential selective carbonic anhydrase IX, XII inhibitors with anti-proliferative activity: Design, synthesis and in silico studies

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 153, P. 107881 - 107881

Published: Oct. 10, 2024

Language: Английский

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Synthesis of tetra-substituted thiophene derivatives as potential Hits combating antibiotic resistant bacteria ESKAPE

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 155, P. 108101 - 108101

Published: Jan. 8, 2025

Language: Английский

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Discovery of 5-Phenylthiazol-2-amine Derivatives as Novel PI4KIIIβ Inhibitors with Efficacious Antitumor Activity by Inhibiting the PI3K/AKT Axis

Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: March 6, 2025

To develop novel PI4KIIIβ inhibitors and explore their antitumor activity, a series of 5-phenylthiazol-2-amine derivatives were synthesized by structural modifications PIK93. Biological assay results indicated that compounds 16 43 exhibited superior selective inhibitory antiproliferative activity than Mechanistic studies revealed the two inhibit PI3K/AKT pathway more effectively, thereby inducing cancer cell apoptosis, cycle arrest in G2/M phase autophagy. Importantly, vivo toxicity pharmacodynamics showed safety to commercially available axis inhibitor alpelisib, obviously small lung H446 xenograft models. Overall, this work highlights therapeutic potential treatment tumors, provides candidates viable drug development strategies for inhibitors.

Language: Английский

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Insight Study For Repurposing Of Certain Anti‐Inflammatory Drugs Based On Aspirin and Salicylic Acid Scaffolds For The Treatment of Cancer as CDKs Inhibitors: Cheminformatics and Anticancer Studies

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(15)

Published: April 1, 2025

Abstract The highly increased and global mortality due to cancer has created an urgent need discover promising targets for its treatment. Where drug repurposing was considered as attractive approach that can facilitate the lead generation optimization phases of discovery by existing agents target diseases other than their primary uses. Cheminformatics studies represented in molecular docking well dynamic simulation salicylic acid / aspirin analogues sulindac indomethacin anti‐inflammatory drugs were carried out be used cyclin‐dependent kinases (CDKs) namely CDK2, CDK6, CDK12 inhibitors. Sulindac displayed best binding ligand all receptors. CDKs inhibition effects three sulindac, anthranilic demonstrated good inhibitory activity against ranging from 0.48 1.78 µM. Likewise, cytotoxicity revealed potent anticancer 0.155 1.278 µM cell lines: HCT‐116, MCF‐7, HeLa cells. As a result, this technique saves lot time money order new agents.

Language: Английский

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Incorporation of human β-defensin-1 into immunoliposomes to facilitate targeted autophagy therapy of colon carcinoma

World Journal of Clinical Oncology, Journal Year: 2025, Volume and Issue: 16(3)

Published: Jan. 20, 2025

Based on the discovery that human β-defensin-1 (hBD-1) triggers autophagy in colon cancer cells and inhibits proliferation, we proposed consideration of its druggability. As a protein, stability, targetability bioavailability must be improved. Compared with traditional medicinal chemistry technology, nanotechnology is more economical for increasing druggability hBD-1 can readily scaled up. Here, propose an immunoliposome system containing to improve stability bioavailability. To enhance targetability, anti-epidermal growth factor receptor (EGFR) antibodies were conjugated liposomal bilayer produce immunoliposomes target EGFR, which highly expressed cells. Although studies are needed support clinical trials large-scale manufacturing, these have great potential as therapeutics. Thus, suitable nanovesicles hBD-1; however, additional basic translational research systems warranted.

Language: Английский

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Nitrogen, Oxygen, and Sulphur Heterocycles as Potent Anti‐Inflammatory Agents: Insight Into the Synthetic Routes

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(9)

Published: March 1, 2025

Abstract Nitrogen, oxygen, and sulfur‐containing heterocyclic compounds are broadly established as key scaffolds with potential chemical biological properties. Benzimidazole, indole, benzoxazole, benzothiazole, pyrazole, thiophene analogs significant motifs that bear almost all pharmacological activities. Anti‐inflammatory activity is one of the most commonly associated activities these heterocycles thus has attracted interest researchers to synthesize study them in‐depth. The present review highlights mainly various synthetic methodologies utilized prepare diverse their properties limited anti‐inflammatory Further, this will provide a comprehensive idea used biologically active nitrogen, sulfur‐bearing possibly invoke new thoughts in search for rational designs developing more promising agents.

Language: Английский

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New amidrazone analogs as multi-kinase inhibitors: in-silico and biological investigation as an anticancer agent

Medicinal Chemistry Research, Journal Year: 2025, Volume and Issue: unknown

Published: March 26, 2025

Language: Английский

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Synthesis and evaluation of carmofur analogs as antiproliferative agents, inhibitors to the main protease (Mpro) of SARS-CoV-2, and membrane rupture-inducing agents

Discover Chemistry., Journal Year: 2025, Volume and Issue: 2(1)

Published: April 7, 2025

Language: Английский

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Design, synthesis and biological evaluation of thienopyridine derivatives as c-Met kinase inhibitors

Molecular Diversity, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 2, 2024

Language: Английский

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