Insight into divergent chemical modifications of chitosan biopolymer: Review

International Journal of Biological Macromolecules, Год журнала: 2024, Номер 277, С. 134347 - 134347

Опубликована: Июль 31, 2024

Язык: Английский

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Unveiling anti-diabetic potential of new thiazole-sulfonamide derivatives: Design, synthesis, in vitro bio-evaluation targeting DPP-4, α-glucosidase, and α-amylase with in-silico ADMET and docking simulation

Bioorganic Chemistry, Год журнала: 2024, Номер 151, С. 107671 - 107671

Опубликована: Июль 23, 2024

Язык: Английский

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Synthesis and modification of novel thiazole-fused quinoxalines as new insecticidal agents against the cotton leafworm Spodoptera litura: design, characterization, in vivo bio-evaluation, toxicological effectiveness, and study their mode of action

RSC Advances, Год журнала: 2025, Номер 15(2), С. 1391 - 1406

Опубликована: Янв. 1, 2025

New insecticidal agents based on quinoxaline derivatives targeting the cotton leafworm, Spodoptera litura .

Язык: Английский

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Unveiling a novel pyrazolopyrimidine scaffold as a dual COX-2/5-LOX inhibitor with immunomodulatory potential: Design, synthesis, target prediction, anti-inflammatory activity, and ADME-T with docking simulation

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 290, С. 117499 - 117499

Опубликована: Март 13, 2025

Язык: Английский

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Novel 3‐Substituted‐2H‐Chromene Scaffold Based Fluorinated Hydrophobic Fragment as In‐Vitro Antiproliferative Agents and Apoptosis Inducers Targeting Both VEGFR‐2/BRAF^V600E and h‐DHFR With Molecular Docking Simulation

Drug Development Research, Год журнала: 2025, Номер 86(2)

Опубликована: Март 28, 2025

ABSTRACT Recently, there has been an increasing interest in the use of protein kinase inhibitors as a therapeutic strategy for treatment cancer. In this study, new series 2 H ‐chromene derivatives ( ‐ 5 and 6 8 ) 3 ‐benzo[ f ]chromene carbohydrazide derivative 9 were synthesized. The structure designed was characterized by IR, 1 H/ 13 C NMR, elemental analysis. Moreover, cytotoxic activity newly synthesized chromenes evaluated against breast cancer cell lines (MDA‐MB‐231 MCF‐7) cervical line (HeLa). results these evaluations demonstrated promising activity, ranging from good to moderate. Additionally, lung fibroblast (WI‐38), normal line, also utilized assess active derivatives' selectivity. Among compounds tested, chromene highest potency, exhibiting IC 50 values 5.36 ± 0.50, 7.82 0.60, 9.28 0.70 µM MDA‐MB 231, MCF‐7, HeLa lines, respectively. potential chromone multi‐targeted anticancer agent assessed evaluating its BRAF VEGFR‐2. Notably, most significant VEGFR2 with value 0.224 compared sorafenib's 0.045 µM, while inhibitory 1.695 relative Vemurafenib's 0.468 µM. addition, compound inhibits DHFR enzyme 2.217 0.014 methotrexate (IC = 0.4315 0.019 µM). These revealed that multifaceted mechanisms action may augment effectiveness. causes overexpression caspase‐3 Bax 6.13 8.85‐fold, It downregulates antiapoptotic Bcl‐2 level 0.4775‐fold untreated 231 cells. Flow cytometry analysis MDA‐MB‐231 cells indicates induces cycle arrest G0‐G1 phase, observed percentage 73.15%. in‐silico toxicity prediction profile. Finally, molecular docking studies supported findings confirming strong binding affinities VEGFR‐2, BRAF, DHFR.

Язык: Английский

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Design and Synthesis of some novel Quinazoline-thioacetamide derivatives as anticancer agents, apoptotic inducers, radio-sensitizers, and VEGFR inhibitors

Journal of Molecular Structure, Год журнала: 2024, Номер 1317, С. 139060 - 139060

Опубликована: Июнь 17, 2024

Язык: Английский

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Exploring a novel thiazole derivatives hybrid with fluorinated-indenoquinoxaline as dual inhibitors targeting VEGFR2/AKT and apoptosis inducers against hepatocellular carcinoma with docking simulation

Bioorganic Chemistry, Год журнала: 2024, Номер 154, С. 108023 - 108023

Опубликована: Дек. 2, 2024

Язык: Английский

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Green synthesis, molecular docking and in vitro biological evaluation of novel hydrazones, pyrazoles, 1,2,4-triazoles and 1,3,4-oxadiazoles

Synthetic Communications, Год журнала: 2024, Номер 54(22), С. 1984 - 2002

Опубликована: Окт. 24, 2024

Ultrasonic waves were used for synthesis of novel hydrazones, bishydrazones, pyrazoles, 1,2,4-triazole and 1,3,4-oxadiazole. The structural formulae the synthesized compounds elucidated in terms elemental spectroscopic analyses. All estimated by testing total antioxidant capacity, iron‐reducing power, scavenging activity against ABTS DPPH radicals addition to anti‐diabetic, anti‐Alzheimer anti‐arthritic activities. displayed good potent bioactivity. Compounds 6, 10 exhibit highest free Furthermore, demonstrate strongest inhibition α‐amylase α-glucosidase. Compound 12 acetylcholinesterase among prepared compounds. However, 18a,b, 19 show a significantly higher percentage protein denaturation proteinase. most bioactive investigated toward docking methodology appropriate protein.

Язык: Английский

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Efficient synthesis and molecular docking of new organoselenium and organosulphur compounds as dual inhibitors for the therapy of Alzheimer's disease as well as Diabetes Mellitus

Journal of Molecular Structure, Год журнала: 2024, Номер unknown, С. 140606 - 140606

Опубликована: Ноя. 1, 2024

Язык: Английский

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A novel chitosan-Schiff bases bearing a new quinoxaline moiety as an approach for potent antimicrobial agent: Synthesis, characterization and in vitro assessments

Carbohydrate Polymers, Год журнала: 2024, Номер 352, С. 123205 - 123205

Опубликована: Дек. 31, 2024

Язык: Английский

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