Bradykinin antagonists and thiazolidinone derivatives as new potential anti-cancer compounds

Avdieiev, Stanislav; Gera, Lajos; Havrylyuk, Dmytro; Hodges, Robert S.; Lesyk, Roman; Ribrag, Vincent; Vassetzky, Yegor S.; Kavsan, V. M.

doi:10.1016/j.bmc.2014.06.046

Cited by 30 publications

(16 citation statements)

References 28 publications

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“…Their strong affinity for various biological targets including JNK‐stimulating phosphatase‐1 (JSP‐1; Cutshall, O'Day, & Prezhdo, ), non‐membrane protein tyrosine phosphatase (SHP‐2; Geronikaki et al., ), tumour necrosis factor‐α (Carter et al., ) and antiapoptotic biocomplex Bcl‐xL/BH3 (Degterev et al., ) might be potential reasons for the anticancer activity. Anticancer activities for various thiazolidinone compounds against breast cancer (Wu et al., ), glioblastoma (Avdieiev et al., ) and drug‐resistant lung cancer (Zhou et al., ) have been reported in the literature.…”

Section: Introductionmentioning

confidence: 99%

Design and synthesis of phenylpiperazine derivatives as potent anticancer agents for prostate cancer

et al. 2019

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Novel thiourea (5a, 5b) and thiazolidinone derivatives (6a, 6b) were synthesized by hybridizing molecules starting from the compound 6‐(4‐phenylpiperazin‐1‐yl)pyridin‐3‐amine (4) which is known to show anticancer activity. The synthesis of the leading compound was carried out by using 1‐(5‐nitropyridin‐2‐yl)‐4‐phenylpiperazine (3) which was obtained by a novel method of the reaction of 2‐chloro‐5‐nitropyridine (1) and N‐phenylpiperazine (2). The structures of the compounds were confirmed using FTIR, 1H NMR, 13C NMR, HRMS spectroscopic methods and elemental analysis. The organic molecules were tested for their anticancer activities against prostate cancer (PC) cell lines: DU 145, PC‐3 and LNCaP. As the compound 5a exerted the highest cytotoxic activity, IC50 concentrations of compound 5a were further investigated in terms of morphology, colony‐forming ability, RNA expression, fragmented DNA and cell cycle distributions of PC cell lines. Overall data revealed that compound 5a treatment induces apoptosis and DNA fragmentation in PC cell lines and inhibits cell cycle progression resulting in the accumulation of cells in either the G1 or the S phases.

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Section: Introductionmentioning

confidence: 99%

Design and synthesis of phenylpiperazine derivatives as potent anticancer agents for prostate cancer

et al. 2019

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“…Fusion of the furanone 1 with methyl‐4‐aminobenzoate in an oil bath gave the pyrrolone derivative 7 . Refluxing 7 with hydrazine hydrate in methanol gave the acid hydrazide derivative .…”

Section: Resultsmentioning

confidence: 99%

“…Thiazolidinone derivatives have been used as antitubercular, antimicrobial, anti‐inflammatory, and antiviral agents, especially as anti‐HIV agents. It has been extensively reported that the presence of different moieties at different positions in the thiazolidinone ring enhanced its anti‐microbial activity, may be because of its inhibitory activity of enzyme Mur B which is a precursor acting during the biosynthesis of peptidoglycan . Numerous reports had appeared in the literature dealing with their chemistry and pharmacological uses .…”

Section: Introductionmentioning

confidence: 99%

Utilization of 2(3H)‐Furanone Bearing a Pyrazolyl Side Chain for the Construction of a Variety of Thiazolidinone Derivatives

Abou‐Elmagd

Hashem

2015

Journal of Heterocyclic Chem

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2(3H)‐Furanone 1 was utilized for the construction of thiazolidinone derivatives. Thus, upon treatment the cyano derivatives 5 with thioglycolic acid afforded the thiazolidinone derivatives 6. Reaction of the Schiff base derivative 9 with thioglycolic acid gave the thiazolidinone derivative 10. Decomposition of the azides 11 in dry benzene in the presence of thioglycolic acid gave the thiazolidindione derivative 12. Antimicrobial activities of synthesized compounds were tested. Some of the tested compounds showed promising activities.

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“…Bradykinin promotes the invasion of gliomas [7] by stimulating the B2 receptor [8,9] and epidermal growth factor receptor (EGFR) signaling pathways [10,11], which promote angiogenesis through the upregulation of VEGF expression. Bradykinin antagonists suppress the growth of glioma tumor cells [12][13][14], and peptide analogs of domain 5 of KNG1 inhibit angiogenesis [15] and metastasis [16].…”

Section: Introductionmentioning

confidence: 99%

Aberrant ceRNA-mediated regulation of KNG1 contributes to glioblastoma-induced angiogenesis

Ren¹,

Nan²,

Kang³

et al. 2016

Oncotarget

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Glioblastoma is a highly vascularized brain tumor that causes high mortality. Kininogen-1 (KNG1) has demonstrated both tumor suppressor and antiangiogenesis properties in gliobastoma cells. We analyzed the microarray and proteomic profiles of tumor tissues from glioblastoma patients (N = 180), and identified potential RNA regulators of the KNG1. Validation experiments in U87 glioblastoma cells showed that the regulation of KNG1 by CTU1, KIAA1274, and RAX was mediated by miR-138. The siRNA-mediated knockdown of CTU1, KIAA1274, or RAX in U87 cells and immortalized human endothelial cells (iHECs) significantly reduced KNG1 expression (P < 0.05 for all), which resulted in the upregulation of oncogenic EGFR signaling in both cell lines, and stimulated angiogenic processes in cultured iHECs and zebrafish and mouse xenograft models of glioblastoma-induced angiogenesis. Angiogenic transduction of iHECs occurred via the uptake of U87-derived exosomes enriched in miR-138, with the siRNA-mediated knockdown of KNG1, CTU1, KIAA1274, or RAX increasing the level of miR-138 enrichment to varying extents and enhancing the angiogenic effects of the U87-derived exosomes on iHECs. The competing endogenous RNA network of KNG1 represents potential targets for the development of novel therapeutic strategies for glioblastoma.

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Bradykinin antagonists and thiazolidinone derivatives as new potential anti-cancer compounds

Cited by 30 publications

References 28 publications

Design and synthesis of phenylpiperazine derivatives as potent anticancer agents for prostate cancer

Design and synthesis of phenylpiperazine derivatives as potent anticancer agents for prostate cancer

Utilization of 2(3H)‐Furanone Bearing a Pyrazolyl Side Chain for the Construction of a Variety of Thiazolidinone Derivatives

Aberrant ceRNA-mediated regulation of KNG1 contributes to glioblastoma-induced angiogenesis

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