Synthesis of novel 1,2,3-triazole based artemisinin derivatives and their antiproliferative activity

Kapkoti, Deepak Singh; Singh, Shilpi; Luqman, Suaib; Bhakuni, R. S.

doi:10.1039/c7nj04271j

Cited by 41 publications

(25 citation statements)

References 47 publications

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“…Similarly, a novel series of artemisinlcone hybrids ( 24 , 25 ) prepared by Gaur et al showed potent activity against HL-60 (leukemia), Mia PaCa-2 (pancreatic cancer), PC-3 (prostate cancer), LS180 (colon cancer) and HEPG2 (hepatocellular carcinoma) cancer cell lines with a high selectivity index [ 69 ]. Kapkoti et al designed 1,2,3-triazole-containing artemisinin–chalcone hybrids ( 26 , IC 50 : 7.16–57.18 µM; 27 , IC 50 : 17.14–69.67 µM) displaying remarkable activity against K562 (human chronic myeloid leukemia cell), PC-3 (human prostate cancer cell), A431 (human skin squamous cell carcinoma), MDA-MB-231 (human metastatic breast cancer cell line), COLO-205 (human colon cancer cell), A549 (human lung cancer cell), and HEK-293 (human embryonic kidney cell) cancer cell lines with significant induction of ROS formation [ 70 ]. Moreover, a toxicity study on human erythrocytes revealed that these molecules are nontoxic (IC 50 : >100 μg/mL).…”

Section: Strategies Employed To Produce Anticancer Chalconesmentioning

confidence: 99%

Chalcone Derivatives: Role in Anticancer Therapy

et al. 2021

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Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.

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Section: Strategies Employed To Produce Anticancer Chalconesmentioning

confidence: 99%

Chalcone Derivatives: Role in Anticancer Therapy

et al. 2021

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“…1,2,3-Triazole-tethered dihydroartemisinin-chalcone hybrid 63 (Figure 11, IC 50 : 7.16 μm, MTT assay) display comparable activity to doxorubicin (IC 50 : 6.36 μm), but it is more potent than dihydroartemisinin (IC 50 : 43.43 μm) against A549 cells, and this hybrid (IC 50 : > 100 μm) is nontoxic toward human erythrocyte and normal kidney cells (HEK-293) (Kapkoti et al, 2018). An SAR study implies that incorporation of the second dihydroartemisinin moiety could boost the activity to some extent.…”

Section: Miscellaneous 123-triazole-containing Compoundsmentioning

confidence: 99%

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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“…Notably, triazole rings exhibit various medicinal applications, such as usages as anticancer [18] anti-HIV [19], antimalarial [20], antiplasmodial [21], and antibacterial agents [1,22]. Some significant triazole derivatives in this context are shown in Figure 1 [8,[23][24][25][26][27]. As such, there is still a demand for the expansion of ways to access new 1,2,3-triazole heterocyclic rings in rapid, efficient, and versatile ways.…”

Section: Introductionmentioning

confidence: 99%

A recent overview on the synthesis of 1,4,5-trisubstituted 1,2,3-triazoles

Shiri¹,

Amani²,

Mayer‐Gall³

2021

Beilstein J. Org. Chem.

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Diverse strategies for the efficient and attractive synthesis of a wide variety of relevant 1,4,5-trisubstituted 1,2,3-triazole molecules are reported. The synthesis of this category of diverse fully functionalized 1,2,3-triazoles has become a necessary and unique research subject in modern synthetic organic key transformations in academia, pharmacy, and industry. The current review aims to cover a wide literature survey of numerous synthetic strategies. Recent reports (2017–2021) in the field of 1,4,5-trisubstituted 1,2,3-triazoles are emphasized in this current review.

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Synthesis of novel 1,2,3-triazole based artemisinin derivatives and their antiproliferative activity

Abstract: Novel artemisinin-1,2,3-triazole derivatives show significant antiproliferative activity, and induce apoptosis and ROS generation and arrest the cell cycle at the G2/M phase.

Cited by 41 publications

References 47 publications

Chalcone Derivatives: Role in Anticancer Therapy

Chalcone Derivatives: Role in Anticancer Therapy

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

A recent overview on the synthesis of 1,4,5-trisubstituted 1,2,3-triazoles

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