Development of 1,3,4-oxadiazole thione based novel anticancer agents: Design, synthesis and in-vitro studies

Yadav, Nalini; Kumar, Parveen; Chhikara, Aruna; Chopra, Madhu

doi:10.1016/j.biopha.2017.08.110

Cited by 23 publications

(10 citation statements)

References 39 publications

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“…The results revealed a synergistic effect in the treatment combination of ADR and Olaparib; combined treatment induced G2/M cell cycle arrest. In addition, the protein expression of Cyclin B1 was downregulated; the inhibition of cyclin B1 could lead to cell cycle arrest in the G2/M phase (29). In conclusion, these results suggested that the combined treatment of ADR and Olaparib may be more effective than monotherapy in treating ADR resistant leukemia.…”

Section: Discussionmentioning

confidence: 99%

PARP inhibitor re‑sensitizes Adriamycin resistant leukemia cells through DNA damage and apoptosis

Xiao

Yuan

et al. 2018

Mol Med Report

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Resistance to Adriamycin (ADR) is an increasing problem in the treatment of leukemia and the development of novel therapeutic strategies is becoming increasingly important. Olaparib is a poly (adenosine diphosphate-ribose) polymerase (PARP) 1 inhibitor, which has promising antitumor activity in patients with metastatic breast cancer and germline BRCA mutations. Previously published studies have indicated that Olaparib is able to overcome drug resistance in cancer; however, its underlying mechanism of action is yet to be elucidated. The aim of the present study was to explore the mechanism underlying re-sensitization. Annexin V-propidium iodide staining indicated that the percentage of apoptotic ADR resistant cells was markedly increased and the cell cycle was blocked at the G2/M-phase following treatment with ADR combined with Olaparib, when compared with the control group. The alkaline comet assay demonstrated that ADR combined with Olaparib significantly upregulated the induction of the DNA damage response in ADR-resistant cells. Western blot analysis revealed that the protein expression of γ-H2A histone family member X, cleaved PARP, caspase 3 and cleaved caspase 3 was markedly enhanced, while the cell cycle-associated protein cyclin B1 was downregulated in K562/ADR cells following treatment with a combination of ADR and Olaparib. Similar synergistic cytotoxicity was observed in blood mononuclear cells, which were isolated from patients with chemotherapy-resistant leukemia. As Olaparib is available for clinical use, the results of the present study provide a rationale for the development of Olaparib combinational therapies for cases of ADR resistant leukemia.

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Section: Discussionmentioning

confidence: 99%

PARP inhibitor re‑sensitizes Adriamycin resistant leukemia cells through DNA damage and apoptosis

Xiao

Yuan

et al. 2018

Mol Med Report

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“…They influence the apoptosis and inhibition of the cell cycle by activating caspase-3, arresting the cell in the G2-M phase of the cycle, as well as through condensation of chromatin and cutting of PARP. In addition, there is an increased expression of proapoptotic factor Bax with decreased expression of antiapoptotic factor Bcl-2 [45].…”

Section: Anti-proliferative Effects Of 134-oxadiazole Derivativesmentioning

confidence: 99%

Anti-Cancer Activity of Derivatives of 1,3,4-Oxadiazole

2018

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Compounds containing 1,3,4-oxadiazole ring in their structure are characterised by multidirectional biological activity. Their anti-proliferative effects associated with various mechanisms, such as inhibition of growth factors, enzymes, kinases and others, deserve attention. The activity of these compounds was tested on cell lines of various cancers. In most publications, the most active derivatives of 1,3,4-oxadiazole exceeded the effect of reference drugs, so they may become the main new anti-cancer drugs in the future.

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“…1,3,4-Oxadiazole derivatives showed numerous biological activities [1][2][3][4][5][6][7][8][9][10][11][12][13][14]. In addition, the 1,3,4-oxadiazole derivatives showed anti-proliferative properties against MCF-7 breast cancer cell Line [15][16][17], ovarian cancer cell lines (ovcar-3 and Hela) [18,19], human lung cancer cell line (L2987) [20] and colorectal cancer [21]. These compounds have different mechanisms of action, which is very important in view of the observed resistance of tumors to standard drug treatment.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Some 2,3-Dihydro-1,3,4-Oxadiazoles and 4,5-Dihydro-1,2,4-Triazoles as Anticancer Agents

Yahya

Abdullah

2020

Int J Pharm Pharm Sci

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Objective: The main objective of this work was to synthesize and evaluate the novel 2,3-dihydro-1,3,4-oxadiazole and 4,5-dihydro-1,2,4-triazole derivatives for cytotoxic activities. Methods: The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were synthesized by cyclization of N'-(substituted-benzylidene) isonicotinohydrazide 3a-e in refluxing acetic anhydride. The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were converted into the corresponding 4,5-dihydro-1,2,4-triazoles 5a-h using ammonia. All the synthesized compounds were identified, depending on the physical and spectral data. Title compounds were assessed for their cytotoxic activity against human cancer cell line (MCF-7) by using Sulforhodamine B (SRB) colorimetric assay. Results: All the synthesized compounds showed characteristic peaks in FTIR, 1HNMR and Mass spectral analysis. The results of the in vitro cytotoxic activity revealed that the compound 4c exhibited equipotent cytotoxic activity with an IC50 value of 8.04 µM when compared with that of standard drug doxorubicin (IC50= 8.02 µM). The reminder compounds have shown good to moderate cytotoxic activities when compared with that of a reference standard. Conclusion: We synthesized a series of title compounds in quantitative yields. Most derivatives showed moderate to good cytotoxic activity.

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Development of 1,3,4-oxadiazole thione based novel anticancer agents: Design, synthesis and in-vitro studies

Cited by 23 publications

References 39 publications

PARP inhibitor re‑sensitizes Adriamycin resistant leukemia cells through DNA damage and apoptosis

PARP inhibitor re‑sensitizes Adriamycin resistant leukemia cells through DNA damage and apoptosis

Anti-Cancer Activity of Derivatives of 1,3,4-Oxadiazole

Synthesis of Some 2,3-Dihydro-1,3,4-Oxadiazoles and 4,5-Dihydro-1,2,4-Triazoles as Anticancer Agents

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