DMXAA-pyranoxanthone hybrids enhance inhibition activities against human cancer cells with multi-target functions

Liu, Jie; Zhang, Fan; Zhang, Lei; Wang, Huailing; Zhang, Jianrun; Cao, Zhang; Jiang, Zhenlei; Li, Yanbing; Liu, Zhijun; Chen, Heru

doi:10.1016/j.ejmech.2017.10.074

Cited by 17 publications

(13 citation statements)

References 33 publications

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“…Initially, the cellular plasma membrane remains intact but undergoes structural changes, such as the distribution of phosphatidylserine in the outer layer of the membrane, which is a signal for recognition by phagocytes. Thus, the dead cell is rapidly phagocytosed by macrophages and removed without extravasation of the cytoplasmic content [60]. After treatment with 3c (13 and 26 μM), it was observed that 16.7 and 27.2% of the cells were in initial apoptosis and 7.4 and 18.1% in late apoptosis phase, respectively.…”

Section: Study Of the Induction Of Cell Death By The Annexin V Testmentioning

confidence: 99%

Biological Evaluation of Arylsemicarbazone Derivatives as Potential Anticancer Agents

et al. 2019

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Fourteen arylsemicarbazone derivatives were synthesized and evaluated in order to find agents with potential anticancer activity. Cytotoxic screening was performed against K562, HL-60, MOLT-4, HEp-2, NCI-H292, HT-29 and MCF-7 tumor cell lines. Compounds 3c and 4a were active against the tested cancer cell lines, being more cytotoxic for the HL-60 cell line with IC50 values of 13.08 μM and 11.38 μM, respectively. Regarding the protein kinase inhibition assay, 3c inhibited seven different kinases and 4a strongly inhibited the CK1δ/ε kinase. The studied kinases are involved in several cellular functions such as proliferation, migration, cell death and cell cycle progression. Additional analysis by flow cytometry revealed that 3c and 4a caused depolarization of the mitochondrial membrane, suggesting apoptosis mediated by the intrinsic pathway. Compound 3c induced arrest in G1 phase of the cell cycle on HL-60 cells, and in the annexin V assay approximately 50% of cells were in apoptosis at the highest concentration tested (26 μM). Compound 4a inhibited cell cycle by accumulation of abnormal postmitotic cells at G1 phase and induced DNA fragmentation at the highest concentration (22 μM).

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Section: Study Of the Induction Of Cell Death By The Annexin V Testmentioning

confidence: 99%

Biological Evaluation of Arylsemicarbazone Derivatives as Potential Anticancer Agents

et al. 2019

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“…The cell viability was assessed with the MTT assay, as previously described. 10 Briey, A549 cells (5 Â 10 4 ) were seeded in a 96-well plate for the initial attachment and incubated with different concentrations of LZOs at various time intervals. Aer incubation, the medium was removed and the cells were incubated with freshly prepared MTT (1 mg mL À1 ) for 3 h. The formazan salt was dissolved with 100 mL of DMSO, and the absorbance was taken at 570 nm.…”

Section: Cell Culture and Mtt Assaymentioning

confidence: 99%

“…Inhibiting the p53/MDM2 interactions to restore the p53 activity represents an appealing therapeutic strategy for numerous wildtype p53 tumors with overexpressed MDM2. 10 Multiple evidence support that excessive ROS accumulation promotes cell apoptosis. 24 Since, the cell cycle arrest has veried the involvement of p53 during LZO-3 treatment, so we detected the expressions of p53 and MDM2 aer the treatments of LZO-3.…”

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confidence: 99%

LingZhi oligopeptides amino acid sequence analysis and anticancer potency evaluation

et al. 2020

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“…Moreover, additional efforts aiming to identify derivatives with improved activity than DMXAA ( 2 ) are under investigation. Recently, DMXAA-pyranoxanthone hybrids were reported to enhance inhibition activity against human cancer cells with multi-target functions [150].…”

Section: Synthetic Carboxyxanthone Derivativesmentioning

confidence: 99%

Carboxyxanthones: Bioactive Agents and Molecular Scaffold for Synthesis of Analogues and Derivatives

et al. 2019

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Xanthones represent a structurally diverse group of compounds with a broad range of biological and pharmacological activities, depending on the nature and position of various substituents in the dibenzo-γ-pyrone scaffold. Among the large number of natural and synthetic xanthone derivatives, carboxyxanthones are very interesting bioactive compounds as well as important chemical substrates for molecular modifications to obtain new derivatives. A remarkable example is 5,6-dimethylxanthone-4-acetic acid (DMXAA), a simple carboxyxanthone derivative, originally developed as an anti-tumor agent and the first of its class to enter phase III clinical trials. From DMXAA new bioactive analogues and derivatives were also described. In this review, a literature survey covering the report on carboxyxanthone derivatives is presented, emphasizing their biological activities as well as their application as suitable building blocks to obtain new bioactive derivatives. The data assembled in this review intends to highlight the therapeutic potential of carboxyxanthone derivatives and guide the design for new bioactive xanthone derivatives.

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DMXAA-pyranoxanthone hybrids enhance inhibition activities against human cancer cells with multi-target functions

Cited by 17 publications

References 33 publications

Biological Evaluation of Arylsemicarbazone Derivatives as Potential Anticancer Agents

Biological Evaluation of Arylsemicarbazone Derivatives as Potential Anticancer Agents

LingZhi oligopeptides amino acid sequence analysis and anticancer potency evaluation

Carboxyxanthones: Bioactive Agents and Molecular Scaffold for Synthesis of Analogues and Derivatives

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