Synthesis and biological evaluation of SHetA2 (NSC-721689) analogs against the ovarian cancer cell line A2780

Nammalwar, Baskar; Bunce, Richard A.; Berlin, K. Darrell; Benbrook, Doris M.; Toal, Coralee

doi:10.1016/j.ejmech.2019.03.010

Cited by 7 publications

(3 citation statements)

References 29 publications

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“…5,6 A2780, an ovarian cancer cell line, was established from an ovarian endometrioid adenocarcinoma tumour in an untreated patient, which is commonly used as a model to observe the effects and test the potency of various chemicals, methods of delivery and treatments for ovarian cancer. [7][8][9] Therefore, developing an effective technique for A2780 sensitive detection and achieving an early diagnosis of OC is crucial for improving the survival rate of OC patients.…”

Section: Introductionmentioning

confidence: 99%

A signal-on electrochemiluminescence immunosensor for A2780 cell detection based on the excellent catalytic performance of Co²⁺ doped TiO₂ nanodisks

et al. 2023

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Section: Introductionmentioning

confidence: 99%

A signal-on electrochemiluminescence immunosensor for A2780 cell detection based on the excellent catalytic performance of Co²⁺ doped TiO₂ nanodisks

et al. 2023

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“…The most effective agents were found in a group of derivatives with electron-withdrawing substituents introduced to the terminal phenyl rings. In recent years, some trifluoromethyl-and trifluoromethoxyphenyl(thio)ureas bearing the thiochroman ring have been synthesized, which exerted an ovarian cancer cell inhibitory effect [19]. Several biphenyl thiourea derivatives, which incorporated CF 3 , nitro, and halogen groups on the pendent aryl rings, were described as inhibitors of lung cancer cell A549 growth, with blocking of K-Ras protein as the identified mechanism [20].…”

Section: Introductionmentioning

confidence: 99%

Investigation of the Mechanisms of Cytotoxic Activity of 1,3-Disubstituted Thiourea Derivatives

et al. 2021

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Substituted thiourea derivatives possess confirmed cytotoxic activity towards cancer but also normal cells. To develop new selective antitumor agents, a series of 3-(trifluoromethyl)phenylthiourea analogs were synthesized, and their cytotoxicity was evaluated in vitro against the cell line panel. Compounds 1–5, 8, and 9 were highly cytotoxic against human colon (SW480, SW620) and prostate (PC3) cancer cells, and leukemia K-562 cell lines (IC50 ≤ 10 µM), with favorable selectivity over normal HaCaT cells. The derivatives exerted better growth inhibitory profiles towards selected tumor cells than the reference cisplatin. Compounds incorporating 3,4-dichloro- (2) and 4-CF3-phenyl (8) substituents displayed the highest activity (IC50 from 1.5 to 8.9 µM). The mechanisms of cytotoxic action of the most effective thioureas 1–3, 8, and 9 were studied, including the trypan blue exclusion test of cell viability, interleukin-6, and apoptosis assessments. Compounds reduced all cancerous cell numbers (especially SW480 and SW620) by 20–93%. Derivatives 2 and 8 diminished the viability of SW620 cells by 45–58%. Thioureas 1, 2, and 8 exerted strong pro-apoptotic activity. Compound 2 induced late apoptosis in both colon cancer cell lines (95–99%) and in K-562 cells (73%). All derivatives acted as inhibitors of IL-6 levels in both SW480 and SW620 cells, decreasing its secretion by 23–63%.

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“…The mortality of ovarian epithelial cancer ranks first of the various gynecological tumors, posing a serious threat to females (2). Due to the deep location, small volume and atypical symptoms, OC is hard to diagnose at early stage (3). Non-metastatic ovarian epithelial cancer only accounts for 30% of all OC cases (4).…”

Section: Introductionmentioning

confidence: 99%

LINC00460 accelerates progression of ovarian cancer by activating transcriptional factor ZNF703

Wang¹,

Gan²,

Liu³

et al. 2020

Oncol Lett

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Potential function of LINC00460 in the progression of ovarian cancer (OC) and its underlying mechanism were studied. LINC00460 level in OC tissues and normal ovarian tissues was detected by quantitative real-time polymerase chain reaction (qRT-PCR). Correlation between LINC00460 level with tumor stage, tumor size and pathological subtypes of OC was analyzed. Potential influence of LINC00460 on proliferative ability and cell cycle progression was evaluated. In vivo tumorigenesis model was conducted by administration of A2780 cells transfected with sh-NC or sh-LINC00460 in nude mice. Predicted through JASPAR database, ZNF703 was screened out as the transcriptional factor binding to LINC00460 promoter region. Chromatin immunoprecipitation (ChIP) assay was performed to verify the binding relationship between ZNF703 and LINC00460. The potential role of ZNF703 in LINC00460-mediated OC progression was examined. LINC00460 was upregulated in OC tissues and cell lines. Its level increased with the deterioration of tumor stage and enlargement of tumor size. LINC00460 was highly expressed in serous ovarian cancer relative to other subtypes of OC. Knockdown of LINC00460 attenuated proliferative ability and arrested cell cycle of A2780 and HO8910 cells. ZNF703 was upregulated in OC tissues. ChIP assay showed pronounced enrichment of LINC00460 in ZNF703. Rescue experiments revealed that ZNF703 overexpression reversed the regulatory effects of LINC00460 on cellular behavior of OC cells. LINC00460 is upregulated in OC tissues and cell lines, which is closely related to tumor progression. It accelerates proliferative ability and cell cycle progression of OC cells via interacting with ZNF703.

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Synthesis and biological evaluation of SHetA2 (NSC-721689) analogs against the ovarian cancer cell line A2780

Cited by 7 publications

References 29 publications

A signal-on electrochemiluminescence immunosensor for A2780 cell detection based on the excellent catalytic performance of Co²⁺ doped TiO₂ nanodisks

A signal-on electrochemiluminescence immunosensor for A2780 cell detection based on the excellent catalytic performance of Co²⁺ doped TiO₂ nanodisks

Investigation of the Mechanisms of Cytotoxic Activity of 1,3-Disubstituted Thiourea Derivatives

LINC00460 accelerates progression of ovarian cancer by activating transcriptional factor ZNF703

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Synthesis and biological evaluation of SHetA2 (NSC-721689) analogs against the ovarian cancer cell line A2780

Cited by 7 publications

References 29 publications

A signal-on electrochemiluminescence immunosensor for A2780 cell detection based on the excellent catalytic performance of Co2+ doped TiO2 nanodisks

A signal-on electrochemiluminescence immunosensor for A2780 cell detection based on the excellent catalytic performance of Co2+ doped TiO2 nanodisks

Investigation of the Mechanisms of Cytotoxic Activity of 1,3-Disubstituted Thiourea Derivatives

LINC00460 accelerates progression of ovarian cancer by activating transcriptional factor ZNF703

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A signal-on electrochemiluminescence immunosensor for A2780 cell detection based on the excellent catalytic performance of Co²⁺ doped TiO₂ nanodisks

A signal-on electrochemiluminescence immunosensor for A2780 cell detection based on the excellent catalytic performance of Co²⁺ doped TiO₂ nanodisks