1,2,3‐Triazole hybrids as anticancer agents: A review

Archiv der Pharmazie, Journal Year: 2021, Volume and Issue: 355(1)

Published: Sept. 24, 2021

Despite the advancements in development of anticancer agents, more effective and safer drugs still need to be developed as current agents cause unwanted side effects many patients have become drug resistant. 1,2,3-Triazoles, due their remarkable biological potential, received considerable attention discovery for agents. The present review article presents an overview recent advances 1,2,3-triazole hybrids with potential over last 2 years, chemical structures, structure-activity relationships, mechanisms action, well insights into docking studies.

Language: Английский

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Schiff bases and their metal complexes to target and overcome (multidrug) resistance in cancer

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 270, P. 116363 - 116363

Published: March 29, 2024

Language: Английский

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Advances of antitumor drug discovery in traditional Chinese medicine and natural active products by using multi‐active components combination

Medicinal Research Reviews, Journal Year: 2023, Volume and Issue: 43(5), P. 1778 - 1808

Published: May 14, 2023

Abstract The antitumor efficacy of Chinese herbal medicines has been widely recognized. Leading compounds such as sterols, glycosides, flavonoids, alkaloids, terpenoids, phenylpropanoids, and polyketides constitute their complex active components. monomers derived from medicine possess an attractive anticancer activity. However, use was limited by low bioavailability, significant toxicity, side effects, hindering clinical applications. Recently, new chemical entities have designed synthesized combining natural drugs with other small drug molecules or moieties to improve the activity selectivity, reduce effects. Such a novel conjugated that can interact several vital biological targets in cells may more synergistic than single‐molecule drug. In addition, conjugates could be obtained pharmacophores containing two known leading compounds. Based on these studies, research development greatly shortened. This study reviews progress based medicine. It is expected serve valuable reference application traditional

Language: Английский

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Poly (ADP-ribose) polymerase (PARP) inhibitors as anticancer agents: An outlook on clinical progress, synthetic strategies, biological activity, and structure-activity relationship

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 274, P. 116535 - 116535

Published: May 31, 2024

Language: Английский

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Designing an anticancer Pd(II) complex as poly(ADP-ribose) polymerase 1 inhibitor

International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: 297, P. 139885 - 139885

Published: Jan. 14, 2025

Language: Английский

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Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer

European Journal of Medicinal Chemistry, Journal Year: 2020, Volume and Issue: 210, P. 112954 - 112954

Published: Oct. 30, 2020

Language: Английский

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Design, synthesis, biological activity, molecular docking and computational studies on novel 1,4-disubstituted-1,2,3-Triazole-Thiosemicarbazone hybrid molecules

Journal of Molecular Structure, Journal Year: 2020, Volume and Issue: 1209, P. 127951 - 127951

Published: Feb. 22, 2020

Language: Английский

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Evaluation of inhibitory effects of some novel phenolic derivatives on the mushroom tyrosinase activity: Insights from spectroscopic analyses, molecular docking and in vitro assays

Food Chemistry, Journal Year: 2022, Volume and Issue: 387, P. 132938 - 132938

Published: April 9, 2022

Language: Английский

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Designing Tailored Thiosemicarbazones with Bespoke Properties: The Styrene Moiety Imparts Potent Activity, Inhibits Heme Center Oxidation, and Results in a Novel “Stealth Zinc(II) Complex”

Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 66(2), P. 1426 - 1453

Published: Jan. 17, 2023

A novel, potent, and selective antitumor agent, namely (E)-3-phenyl-1-(2-pyridinyl)-2-propen-1-one 4,4-dimethyl-3-thiosemicarbazone (PPP44mT), its analogues were synthesized characterized displayed strikingly distinctive properties. This activity was mediated by the inclusion of a styrene moiety, which through steric electrochemical mechanisms prevented deleterious oxy-myoglobin or oxy-hemoglobin oxidation relative to other potent thiosemicarbazones, i.e., di-2-pyridylketone-4-cyclohexyl-4-methyl-3-thiosemicarbazone (DpC) di-2-pyridylketone-4,4-dimethyl-3-thiosemicarbazone (Dp44mT). Structure–activity relationship analysis demonstrated specific tuning PPP44mT electrochemistry further inhibited oxidation. Both Cu(II) complexes showed conspicuous almost immediate cytotoxicity against SK-N-MC tumor cells (within 3 h). In contrast, [Zn(PPP44mT)2] pronounced delay in activity, taking 48 h before marked antiproliferative efficacy apparent. As such, designated as "stealth Zn(II) complex" that overcomes near copper complexes. Upon examination suppression oncogenic signaling, superior at inhibiting cyclin D1 expression compared DpC Dp44mT.

Language: Английский

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Synthesis and anticancer mechanisms of zinc(ii)-8-hydroxyquinoline complexes with 1,10-phenanthroline ancillary ligands

Dalton Transactions, Journal Year: 2023, Volume and Issue: 52(15), P. 4737 - 4751

Published: Jan. 1, 2023

Twenty new zinc(II) complexes with 8-hydroxyquinoline (H-Q1-H-Q6) in the presence of 1,10-phenanthroline derivatives (D1-D10) were synthesized and formulated as [Zn(Q1)2(D1)] (DQ1), [Zn(Q2)2(D2)]·CH3OH (DQ2), [Zn(Q1)2(D3)] (DQ3), [Zn(Q1)2(D4)] (DQ4), [Zn(Q3)2(D5)] (DQ5), [Zn(Q3)2(D4)] (DQ6), [Zn(Q4)2(D5)]·CH3OH (DQ7), [Zn(Q4)2(D6)] (DQ8), [Zn(Q4)2(D3)]·CH3OH (DQ9), [Zn(Q4)2(D1)]·H2O (DQ10), [Zn(Q5)2(D4)] (DQ11), [Zn(Q6)2(D6)]·CH3OH (DQ12), [Zn(Q5)2(D2)]·5CH3OH·H2O (DQ13), [Zn(Q5)2(D7)]·CH3OH (DQ14), [Zn(Q5)2(D8)]·CH2Cl2 (DQ15), [Zn(Q5)2(D9)] (DQ16), [Zn(Q5)2(D1)] (DQ17), [Zn(Q5)2(D5)] (DQ18), [Zn(Q5)2(D10)]·CH2Cl2 (DQ19) [Zn(Q5)2(D3)] (DQ20). They characterized using multiple techniques. The cytotoxicity DQ1-DQ20 was screened human cisplatin-resistant SK-OV-3/DDP ovarian cancer (SK-OV-3CR) cells normal hepatocyte (HL-7702) cells. Complex DQ6 showed low IC50 values (2.25 ± 0.13 μM) on SK-OV-3CR cells, more than 3.0-8.0 times cytotoxic DQ1-DQ5 DQ7-DQ20 (≥6.78 μM), even 22.2 standard cisplatin, corresponding free H-Q1-H-Q6 D1-D10 alone (>50 μM). As a comparison, displayed nontoxic rates against healthy HL-7702 Furthermore, DQ11 induced significant apoptosis via mitophagy pathways. also significantly inhibited tumor growth an vivo SK-OV-3-xenograft model (ca. 49.7%). Thus, may serve lead complex for discovery antitumor agents.

Language: Английский

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