Discovery of novel tris-1,2,3-triazole-based hybrids as VEGFR2 inhibitors with potent anti-proliferative and cytotoxicity through apoptosis induction

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 155, P. 108131 - 108131

Published: Jan. 8, 2025

Language: Английский

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Therapeutic potential of chalcone-1,2,3-triazole hybrids as anti-tumour agents: a systematic review and SAR studies

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 17(4), P. 449 - 465

Published: Jan. 31, 2025

The study of chalcone-1,2,3-triazole hybrids for anticancer activity is quite a recent area focus, primarily because the increasing demand developing new drugs to treat cancer. chalcones and 1,2,3-triazole rings in hybrid compounds has recently emerged as promising strategy novel agents. ring, known its stability hydrogen bonding capabilities, enhances target binding affinity these hybrids. Chalcones possess an α,β-unsaturated carbonyl system crucial their synergistic effect two moieties results with potent properties. This review explores structure-activity relationship studies which revealed that electronic lipophilic properties substituents on phenyl significantly influence activity. Electron-donating electron-withdrawing groups can affect cellular uptake engagement. Incorporating various into ring improve selectivity potency against specific cancer cell lines. These often exert effects through apoptosis cycle disruption. Recent research indicates chalcone hold therapeutic promise Further optimization SAR in-depth mechanistic investigations could lead development highly selective agents minimal toxicity.

Language: Английский

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Insights into Novel Isoniazide Encompassing triazolo[4,3-b][1,2,4]triazoles as Anti-TB, Antioxidant and Antidiabetic agents: A Spectral analysis, DFT calculations, ADME, In vitro, and in silico Molecular Modeling Studies

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: unknown, P. 141876 - 141876

Published: Feb. 1, 2025

Language: Английский

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Carvacrol-Derived 1,2,3-Triazole Hybrids: Synthesis, Computational Insights, and Targeted Inhibition of EGFR, BRAF V600E, and Tubulin Enzymes

Journal of Fluorescence, Journal Year: 2025, Volume and Issue: unknown

Published: March 18, 2025

Language: Английский

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Facile green diversity-oriented synthesis, molecular docking, and cytotoxicity evaluation of quinoline -triazole appended peptidomimetics as inhibitors of human breast cancer cell line MCF-7

Results in Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 102172 - 102172

Published: March 1, 2025

Language: Английский

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Recent advances in regulating the cell cycle through inhibiting CDKs for cancer treatment

Chinese Journal of Natural Medicines, Journal Year: 2025, Volume and Issue: 23(3), P. 286 - 298

Published: March 1, 2025

Language: Английский

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The importance of glycotriazoles in medicinal chemistry – A narrative review

Journal of Carbohydrate Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 27

Published: April 11, 2025

Language: Английский

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Recent progress in synthetic strategies for novel β-lactams linked with five-membered heterocycles (N/O/S): advances in medicinal chemistry (2020–2025)

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

Published: April 12, 2025

Language: Английский

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Synthesis and antitumoral activity of novel biaryl hydroxy-triazole and fluorene-triazole hybrids

Published: April 21, 2025

Aim: The development of selective and potent antitumor agents remains a significant challenge. This study aimed to synthesize evaluate biaryl hydroxy-1,2,3-triazoles 9H-fluorene-1,2,3-triazole hybrids, inspired by previously identified bioactive 1,2,3-triazoles, for their cytotoxic potential against human cancer cell lines. Methods: A library 13 11 fluorene-1,2,3-triazoles was synthesized using optimized Suzuki telescopic one-pot reactions, with yields ranging from 16% 97%. cytotoxicity these compounds tested HCT-116 (colorectal cancer), SNB-19 (astrocytoma), MDA-MB-231 (triple-negative breast MOLM-13 (acute myeloid leukemia, FLT3-ITD mutant) Results: Two fluorene-triazoles, 1-(2-bromophenyl)-4-(9H-fluoren-9-yl)-1H-1,2,3-triazole (LSO258) 1-(4-bromophenyl)-4-(2-fluoro-9H-fluoren-9-yl)-1H-1,2,3-triazole (LSO272), both containing bromine substituents, exhibited MOLM-13, half-maximal inhibitory concentration (IC50) values 25.5 μM 12.5 μM, respectively. Furthermore, LSO258 LS0272 showed selectivity index ≥ 2 towards the line. Biaryl displayed broader activity, [1,1’-biphenyl]-2-yl(1-(2,5-dibromophenyl)-1H-1,2,3-triazol-4-yl)methanol (LSO278), featuring two groups, demonstrating potency across HCT-116, MDA-MB-231, (IC50: 23.4 34.3 18.7 respectively). However, structural rigidity did not consistently predict as 1-(2,5-dibromophenyl)-4-(9H-fluoren-9-yl)-1H-1,2,3-triazole (LSO275), rigid fluorene-triazole, inactive. most sensitive line, such 4-(9H-fluoren-9-yl)-1-(4-(trifluoromethyl)phenyl)-1H-1,2,3-triazole (LSO259) (1-(4-bromophenyl)-1H-1,2,3-triazol-4-yl)(4’-fluoro-[1,1’-biphenyl]-2-yl)methanol (LSO280), achieving maximum growth inhibition (MGI > 55%) despite reaching IC50 values. Conclusions: results highlight critical role substitution on aryl azide-derived ring in modulating activity. reinforces fluorene-based scaffolds promising leads targeted therapies FLT3-mutant aligning previous reports 1,2,3-triazole hybrids antiproliferative activity leukemia models.

Language: Английский

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Microwave-Assisted Synthesis and Investigation of Urease Inhibitory Activities of Some 1,2,4-Triazol-3-ones Containing Salicyl and Isatin Moieties

Russian Journal of General Chemistry, Journal Year: 2024, Volume and Issue: 94(8), P. 2018 - 2022

Published: Aug. 1, 2024

Language: Английский

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