Synthesis and Cytotoxicity of Chalcone Based 1,2,3-Triazole Derivatives

Raghavender, M.; Kumar, A. Kishore; Sunitha, V.; Vishnu, T.; Pochampally, Jalapathi

doi:10.1134/s1070363220040210

Cited by 15 publications

(4 citation statements)

References 18 publications

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“…An SAR study demonstrated that introducing a methoxy group into the phenyl ring could not increase the activity apparently, and the activity of compounds 9 (GI 50 : 4.7-11.9 μm, SRB assay) is considerably inferior to that of combretastatin-A4 (GI 50 : 0.08 μm) against A549 cells (Hussaini et al, 2016). Further study proved that the benzyl group at the N-1 position of the 1,2,3-triazole moiety is not crucial for the activity, and replacement by the phenyl ring is also permitted, as evidenced by that compounds 10a,b (IC 50 : 62.51 and 75.41 μm, MTT assay) show comparable activity to doxorubicin (IC 50 : 39.86 μm) against A549 cells (Raghavender et al, 2020 (Chinthala et al, 2015).…”

Section: Introductionmentioning

confidence: 92%

1,2,3-Triazole-Containing Compounds as Anti–Lung Cancer Agents: Current Developments, Mechanisms of Action, and Structure–Activity Relationship

Liang

Sun

et al. 2021

Front. Pharmacol.

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Lung cancer is the most common malignancy and leads to around one-quarter of all cancer deaths. Great advances have been achieved in the treatment of lung cancer with novel anticancer agents and improved technology. However, morbidity and mortality rates remain extremely high, calling for an urgent need to develop novel anti–lung cancer agents. 1,2,3-Triazole could be readily interact with diverse enzymes and receptors in organisms through weak interaction. 1,2,3-Triazole can not only be acted as a linker to tether different pharmacophores but also serve as a pharmacophore. This review aims to summarize the recent advances in 1,2,3-triazole–containing compounds with anti–lung cancer potential, and their structure–activity relationship (SAR) together with mechanisms of action is also discussed to pave the way for the further rational development of novel anti–lung cancer candidates.

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Section: Introductionmentioning

confidence: 92%

1,2,3-Triazole-Containing Compounds as Anti–Lung Cancer Agents: Current Developments, Mechanisms of Action, and Structure–Activity Relationship

Liang

Sun

et al. 2021

Front. Pharmacol.

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“…[61] The 1,2,3-triazole-tethered chalcone derivatives 50 and 51 exerted antiproliferative activity with IC 50 values of 62.51 and 75.41 μM, respectively, against A549 cancer cells. [62]…”

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confidence: 99%

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

Alam

2021

Archiv der Pharmazie

157

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

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“…Ten 1,2,3-triazole-linked chalcone hybrids ( 20a – 20j , Figure 8 ) were synthesized by CuAAC reaction from O -propargylated chalcones and aryl or alkyl azides [ 64 ]. All compounds were shown to have moderate-to-low activity against the A549 cancer cell line (IC 50 = 62.51–174.27 µM), compared to the positive control DOX (IC 50 = 39.86 µM).…”

Section: 123-triazole-linked Flavonoid Hybrids With Antitumor Activitymentioning

confidence: 99%

Recent Advances in Bioactive Flavonoid Hybrids Linked by 1,2,3-Triazole Ring Obtained by Click Chemistry

et al. 2021

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As a result of the biological activities of natural flavonoids, several synthetic strategies aiming to obtain analogues with improved potency and/or pharmacokinetic profile have been developed. Since the triazole ring has been associated with several biological activities and metabolic stability, hybridization with a 1,2,3-triazole ring has been increasingly reported over the last years. The feasible synthesis through copper (I) catalyzed azide-alkyne cycloaddition (CuAAC) has allowed the accomplishment of several hybrids. Since 2017, almost 700 flavonoid hybrids conjugated with 1,2,3-triazole, including chalcones, flavones, flavanones and flavonols, among others, with antitumor, antimicrobial, antidiabetic, neuroprotective, anti-inflammatory, antioxidant, and antifouling activity have been reported. This review compiles the biological activities recently described for these hybrids, highlighting the mechanism of action and structure–activity relationship (SAR) studies.

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Synthesis and Cytotoxicity of Chalcone Based 1,2,3-Triazole Derivatives

Cited by 15 publications

References 18 publications

1,2,3-Triazole-Containing Compounds as Anti–Lung Cancer Agents: Current Developments, Mechanisms of Action, and Structure–Activity Relationship

1,2,3-Triazole-Containing Compounds as Anti–Lung Cancer Agents: Current Developments, Mechanisms of Action, and Structure–Activity Relationship

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

Recent Advances in Bioactive Flavonoid Hybrids Linked by 1,2,3-Triazole Ring Obtained by Click Chemistry

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