Azole Derivatives: Cutting‐Edge Agents in Cancer Therapy DOI

Anuradha Mehra,

Amit Mittal, Rekha Sangwan

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(43)

Published: Nov. 1, 2024

Abstract Monocyclic 5‐membered heterocycles including imidazoles, thiazoles, oxazoles, and their related compounds have gained significant attention in medicinal chemistry because of potent anticancerous activity. These small heterocyclic molecules possess versatile properties, biological activity, absorption, distribution, metabolism, excretion, chemical diversity that give them immense potential as anticancer agents. It is also a fact inherent characteristic azoles to combine with many through hydrogen bond, stacking, hydrophobic interaction makes effective against almost all cancer types. In the present paper author discusses way which connected structure monocyclic activity namely ability these intercalate DNA, inhibit some enzymes interfere cellular signaling pathways. Interestingly, several azole derivatives been seen be preclinical efficacy studies well clinical trials are considered overcoming problem resistance side effects common As synthetic progresses, structural system has diversified development pharmacology become more specific. This helped enhancing formation new class improved selectivity efficacy. Furthermore, comprehensive review explains how computational structure‐activity relationship (SAR) approaches applied design future‐generation compounds. light facts, this article designed broad overview current state azole‐based agents an attempt further assert its therapeutic promise spur attempts at infusing said into therapeutics fray. The discoveries made study may allow radical different approaches, could lead targeted treatment cancer.

Language: Английский

Fragment-based drug discovery: Small fragments, big impact − Success stories of approved oncology therapeutics DOI
Nilesh Raghunath Khedkar, Milind Sindkhedkar, Alex Joseph

et al.

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 156, P. 108197 - 108197

Published: Jan. 24, 2025

Language: Английский

Citations

1
Advances in Cancer Therapy: A Comprehensive Review of CDK and EGFR Inhibitors DOI Creative Commons
Mohammed Hawash

Cells, Journal Year: 2024, Volume and Issue: 13(19), P. 1656 - 1656

Published: Oct. 6, 2024

Protein kinases have essential responsibilities in controlling several cellular processes, and their abnormal regulation is strongly related to the development of cancer. The implementation protein kinase inhibitors has significantly transformed cancer therapy by modifying treatment strategies. These received substantial FDA clearance recent decades. emerged as primary objectives for therapeutic interventions, particularly context treatment. At present, 69 therapeutics been approved that target approximately 24 kinases, which are specifically prescribed neoplastic illnesses. novel agents inhibit certain such receptor protein-tyrosine protein-serine/threonine dual-specificity nonreceptor kinases. This review presents a comprehensive overview targets inhibitors, with specific focus on cyclin-dependent (CDKs) epidermal growth factor (EGFR). majority reviewed studies commenced an assessment cell lines concluded biological evaluation individual targets. articles provide detailed information structural features potent anticancer activity, refers ability selectively cancer-promoting including CDKs EGFR. Additionally, latest FDA-approved targeting these enzymes were highlighted accordingly.

Language: Английский

Citations

3
Computational design, synthesis, and assessment of 3-(4-(4-(1,3,4-oxadiazol-2-yl)-1H-imidazol-2-yl)phenyl)-1,2,4-oxadiazole derivatives as effective epidermal growth factor receptor inhibitors: a prospective strategy for anticancer therapy DOI
Nilesh Raghunath Khedkar, Milind Sindkhedkar, Alex Joseph

et al.

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 15(5), P. 1626 - 1639

Published: Jan. 1, 2024

Herein, we developed innovative EGFR inhibitor using the FBDD approach. Compound 30a emerged as highly potent, selective, capable of arresting cell cycle, and inducing apoptosis, underscoring its potential a novel anticancer therapeutic agent.

Language: Английский

Citations

1
Neuroprotective effects of trigonelline in eggplant on oxidative damage of PC12 cells and cognitive impairment in aging mice DOI Creative Commons

Jiahui Feng,

Weihua Liu,

Danqi Feng

et al.

Journal of Functional Foods, Journal Year: 2024, Volume and Issue: 121, P. 106441 - 106441

Published: Sept. 11, 2024

Language: Английский

Citations

1
Synthesis, Docking, and Dynamic Studies of New Pyrano‐[3,2‐e]‐Pyrazole Fused 1,2,4‐Triazolo‐[4,3‐c]‐pyrimidine Analogues as Anticancer Agents DOI Open Access

N.S. Kumar,

Ravi Kumar Ganta, Harihara Padhy

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(42)

Published: Nov. 1, 2024

Abstract A novel series of dihydropyrazolo‐[4′,3′:5,6]‐pyrano[3,2 ‐e ][1,2,4]triazolo[4,3 ‐c ]‐pyrimidine analogues were designed, synthesized, and their cytotoxic potential against four tumor cell lines assessed. HRMS, 1 H NMR, 13 C NMR spectra analysis used to describe the compounds. Compound 9c had noteworthy anticancer activity in vitro Hela, MCF‐7, A549, A2780 lines, with IC 50 values 0.98 ± 0.26, 3.11 0.18, 1.24 0.88, 2.62 0.56 µM, that order. The molecular docking dynamics simulation studies revealed lead molecule's action mechanism EGFR target protein.

Language: Английский

Citations

0
Azole Derivatives: Cutting‐Edge Agents in Cancer Therapy DOI

Anuradha Mehra,

Amit Mittal, Rekha Sangwan

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(43)

Published: Nov. 1, 2024

Abstract Monocyclic 5‐membered heterocycles including imidazoles, thiazoles, oxazoles, and their related compounds have gained significant attention in medicinal chemistry because of potent anticancerous activity. These small heterocyclic molecules possess versatile properties, biological activity, absorption, distribution, metabolism, excretion, chemical diversity that give them immense potential as anticancer agents. It is also a fact inherent characteristic azoles to combine with many through hydrogen bond, stacking, hydrophobic interaction makes effective against almost all cancer types. In the present paper author discusses way which connected structure monocyclic activity namely ability these intercalate DNA, inhibit some enzymes interfere cellular signaling pathways. Interestingly, several azole derivatives been seen be preclinical efficacy studies well clinical trials are considered overcoming problem resistance side effects common As synthetic progresses, structural system has diversified development pharmacology become more specific. This helped enhancing formation new class improved selectivity efficacy. Furthermore, comprehensive review explains how computational structure‐activity relationship (SAR) approaches applied design future‐generation compounds. light facts, this article designed broad overview current state azole‐based agents an attempt further assert its therapeutic promise spur attempts at infusing said into therapeutics fray. The discoveries made study may allow radical different approaches, could lead targeted treatment cancer.

Language: Английский

Citations

0