DNA profiling and in vitro cytotoxicity studies of tetrazolo[1,5-a]pyrimidine-based copper(II) complexes

Haleel, Azees Khan; Rafi, Ummer Muhammed; Mahendiran, Dharmasivam; Mitu, Liviu; Veena, V.; Rahiman, A. Kalilur

doi:10.1007/s10534-019-00196-2

Cited by 9 publications

(9 citation statements)

References 42 publications

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“…Tetrazolo [1,5-a]pyrimidine-based Cu(II) complexes 11 have a square planar geometry, and despite their high capability to inhibit Top1, interact with CDK for 11 [86] and VEGF receptors for an analog of 11 [87]. Binuclear Cu(II) dipeptide piperazine-bridged complex 12 recognizes specific sequences in the DNA, oxidatively cleaves DNA, and displays superoxide dismutase (SOD) activity [88].…”

Section: Cuc Top1 Inhibitorsmentioning

confidence: 99%

“…Multiple stress factors ranging from various cell damages, ATP levels, and specific pathways (e.g., caspases) determine the type of cell death [157]. Most Top1 CuC inhibitors that interact with DNA [70,76,79,86,87,90], Top1 poison [89], Top2α CuC poison [109], or dual Top1/Top2 inhibitor [113] trigger apoptotic programmed cell death. Genetic damages and oxidative stress activate an intrinsic mitochondrial response [158].…”

Section: Programmed Cell Death Engaged By Copper Complexes and Top Inhibitorsmentioning

confidence: 99%

“…CuC dual Top inhibitors display a high antiproliferative activity. Particularly, some CuC and non-CuC are dual inhibitors of Top1 and superoxide dismutase agonist [88,207,208] or Cdk receptor, like VEGF inhibitors, involved in cancer cells proliferation [86,87,209,210] (Figure 5B). Another strategy to improve therapies is the association of a CuC with a TDP1/2 (tyrosyl-DNA-phosphodiesterase 1/2) inhibitor.…”

Section: Future Strategies For Copper Complexes As Top Inhibitors In Cancer Cell Treatmentsmentioning

confidence: 99%

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Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II

Molinaro

Martoriati

Pélinski

et al. 2020

Cancers

119

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Organometallics, such as copper compounds, are cancer chemotherapeutics used alone or in combination with other drugs. One small group of copper complexes exerts an effective inhibitory action on topoisomerases, which participate in the regulation of DNA topology. Copper complexes inhibitors of topoisomerases 1 and 2 work by different molecular mechanisms, analyzed herein. They allow genesis of DNA breaks after the formation of a ternary complex, or act in a catalytic mode, often display DNA intercalative properties and ROS production, and sometimes display dual effects. These amplified actions have repercussions on the cell cycle checkpoints and death effectors. Copper complexes of topoisomerase inhibitors are analyzed in a broader synthetic view and in the context of cancer cell mutations. Finally, new emerging treatment aspects are depicted to encourage the expansion of this family of highly active anticancer drugs and to expend their use in clinical trials and future cancer therapy.

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Section: Cuc Top1 Inhibitorsmentioning

confidence: 99%

Section: Programmed Cell Death Engaged By Copper Complexes and Top Inhibitorsmentioning

confidence: 99%

Section: Future Strategies For Copper Complexes As Top Inhibitors In Cancer Cell Treatmentsmentioning

confidence: 99%

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Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II

Molinaro

Martoriati

Pélinski

et al. 2020

Cancers

119

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“…This method is advantageous relative to mainstream synthetic frameworks in easy set-up, cost-effectiveness and high yield. Recently, several MCRs have been used effectively to build nitrogen-heterocyclic compounds especially the indole substructure that possesses distinct pharmacological and biological activities [28][29][30][31][32][33][34][35][36][37][38][39].…”

Section: Introductionmentioning

confidence: 99%

One-Pot Multicomponent Synthesis and Cytotoxic Evaluation of Novel 7-Substituted-5-(1H-Indol-3-yl)Tetrazolo[1,5-a] Pyrimidine-6-Carbonitrile

2020

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A series of novel 7-substituted-5-(1H-indol-3-yl)tetrazolo[1,5-a]pyrimidine-6-carbonitrile was synthesized via a one-pot, three-multicomponent reaction of appropriate aldehydes, 1H-tetrazole-5-amine and 3-cyanoacetyl indole in catalytic triethylamine. The cytotoxic activity of the new synthesized tetrazolopyrimidine-6-carbonitrile compounds was investigated against HCT-116, MCF-7, MDA-MB-231, A549 human cancer cell lines and one human healthy normal cell line (RPE-1) using the MTT cytotoxicity assay. Compounds 4h, 4b, 4c, 4i and 4a showed potent anticancer activities against human colon cancer. Additionally, all the compounds showed potent anticancer activities on human lung cancer.

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“…Substituted pyrimidines primarily display their anticancer activity through intercalating with DNA nucleotide bases. However, they may prevent ROS induced DNA mutations in a way similar to other anticancer and antiviral molecules [8][9][10][11]. In recent years, anticancer drugs already being used in medical practice or being tested in clinical studies have been often based on pyrimidine skeleton, and new pyrimidine derivatives continue to show promising activities [12][13][14][15].…”

Section: Introductionmentioning

confidence: 99%

Free Radical Scavenging and Cytotoxic Activities of Substituted Pyrimidines

Quratulain¹,

Hussain²,

Coudhary

et al. 2020

CTOIJ

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A library of substituted pyrimidines was synthesized and evaluated for free radical scavenging, and in vitro cytotoxic activity in 3T3 cells. All compounds showed good free radical scavenging activity with IC50 values in the range of 42.9 ± 0.31 to 438.3 ± 3.3 µM as compared to the standard butylated hydroxytoluene having IC50 value of 128.83 ± 2. 1 µM. The structure activity-relationship was also established. Selected analogues 1

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DNA profiling and in vitro cytotoxicity studies of tetrazolo[1,5-a]pyrimidine-based copper(II) complexes

Cited by 9 publications

References 42 publications

Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II

Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II

One-Pot Multicomponent Synthesis and Cytotoxic Evaluation of Novel 7-Substituted-5-(1H-Indol-3-yl)Tetrazolo[1,5-a] Pyrimidine-6-Carbonitrile

Free Radical Scavenging and Cytotoxic Activities of Substituted Pyrimidines

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