Synthesis of a platinum(II) complex with 2-(4-methoxy-phenyl) imidazo [4,5-f]-[1,10] phenanthrolin and study of its antitumor activity

Qin, Qi‐Pin; Chen, Zhen-Feng; Shen, Wangyang; Jiang, Yinlai; Cao, Dong; Li, Yulan; Xu, Qinghua; Liu, Yancheng; Huang, Ke-Bin; Liang, Hong

doi:10.1016/j.ejmech.2014.10.019

Cited by 26 publications

(4 citation statements)

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“…The X-Ray crystallography structures of L a , complexes 3 , 7 and 10 were solved by Sheldrick method78. The antitumor mechanism of complexes 1 – 14 were similar to that reported by Chen437980. The TRAP-silver staining assay of complexes 1 – 6 , 8 and 11 were performed as reported by Neidle and Reed31.…”

Section: Methodssupporting

confidence: 65%

Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity

Qin

Meng

et al. 2016

Sci Rep

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A series of group-10 metal complexes 1–14 of oxoisoaporphine derivatives were designed and synthesized. 1–14 were more selectively cytotoxic to Hep-G2 cells comparing with normal liver cells. In vitro cytotoxicity results showed that complexes 1–6, 7, 8, 10 and 11, especially 3, were telomerase inhibitors targeting c-myc, telomeric, and bcl-2 G4s and triggered cell senescence and apoptosis; they also caused telomere/DNA damage and S phase arrest. In addition, 1–6 also caused mitochondrial dysfunction. Notably, 3 with 6-amino substituted ligand La exhibited less side effects than 6 with 8-amino substituted ligand Lb and cisplatin, but similar tumor growth inhibition efficacy in BEL-7402 xenograft model. Complex 3 has the potential to be developed as an effective anticancer agent.

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Section: Methodssupporting

confidence: 65%

Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity

Qin

Meng

et al. 2016

Sci Rep

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“…Meanwhile, the extracellular acidification rate (ECAR) assay showed that Zn1 and Zn2 could inhibit glycolysis in T-24 cells (Figure S23). Tumor glycolysis inhibition strengthens the antitumor effect by inducing ICD-associated features. , The caspase-3/9 plays a crucial role in the mitochondrial apoptotic pathway . Next, the stimulation of caspase-9/3 activities was observed, showing that the proportion of activated caspase-3 and caspase-9 was 30.8 and 58.5% when exposed to Zn1 (10 μM) and Zn2 (9 μM), accounting for 13.8 and 30.6% of total cells, respectively (Figure S24).…”

Section: Resultsmentioning

confidence: 93%

“…67,68 The caspase-3/ 9 plays a crucial role in the mitochondrial apoptotic pathway. 69 Next, the stimulation of caspase-9/3 activities was observed, showing that the proportion of activated caspase-3 and caspase-9 was 30.8 and 58.5% when exposed to Zn1 (10 μM) and Zn2 (9 μM), accounting for 13.8 and 30.6% of total cells, respectively (Figure S24). Double staining of Annexin V-FITC/PI indicated that Zn1 and Zn2 dose-dependently induced apoptosis (Figure S25).…”

Section: ■ Introductionmentioning

confidence: 95%

Potent Zinc(II)-Based Immunogenic Cell Death Inducer Triggered by ROS-Mediated ERS and Mitochondrial Ca²⁺ Overload

et al. 2023

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Zn1 and Zn2 are Zn-based complexes that activate the immunogenic cell death (ICD) effect by Ca2+-mediated endoplasmic reticulum stress (ERS) and mitochondrial dysfunction. Compared with Zn1, Zn2 effectively caused reactive oxidative species (ROS) overproduction in the early phase, leading to ERS response. Severe ERS caused the release of Ca2+ from ER to cytoplasm and further to mitochondria. Excessive Ca2+ in mitochondria triggered mitochondrial dysfunction. The damage-associated molecular patterns (DAMPs) of CRT, HMGB1, and ATP occurred in T-24 cells exposed to Zn1 and Zn2. The vaccination assay demonstrated that Zn1 and Zn2 efficiently suppressed the growth of distant tumors. The elevated CD8+ cytotoxic T cells and decreased Foxp3+ cells in vaccinated mice supported our conclusion. Moreover, Zn1 and Zn2 improved the survival rate of mice compared with oxaliplatin. Collectively, our findings provided a new design strategy for a zinc-based ICD inducer via ROS-induced ERS and mitochondrial Ca2+ overload.

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“…Therefore, telomerase is regarded as an effective drug target 5 . Regulating the stability of telomerase G-quadruplex as anticancer agents have been widely reported [6][7][8][9][10][11][12][13] .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety

Han

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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Based on previous studies, 66 2-phenyl-4H-chromone derivatives containing amide and 1,3,4-oxadiazole moieties were prepared as potential telomerase inhibitors. The results showed most of the title compounds exhibited significantly inhibitory activity on telomerase. Among them, some compounds demonstrated the most potent telomerase inhibitory activity (IC 50 < 1 mM), which was significantly superior to the staurosporine (IC 50 ¼ 6.41 mM). In addition, clear structure-activity relationships were summarised, indicating that the substitution of the methoxy group and the position, type and number of the substituents on the phenyl ring had significant effects on telomerase activity. Among them, compound A33 showed considerable inhibition against telomerase. Flow cytometric analysis showed that compound A33 could arrest MGC-803 cell cycle at G2/M phase and induce apoptosis in a concentration-dependent way. Meanwhile, Western blotting revealed that this compound could reduce the expression of dyskerin, which is a fragment of telomerase.

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Synthesis of a platinum(II) complex with 2-(4-methoxy-phenyl) imidazo [4,5-f]-[1,10] phenanthrolin and study of its antitumor activity

Cited by 26 publications

References 51 publications

Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity

Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity

Potent Zinc(II)-Based Immunogenic Cell Death Inducer Triggered by ROS-Mediated ERS and Mitochondrial Ca²⁺ Overload

Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety

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Synthesis of a platinum(II) complex with 2-(4-methoxy-phenyl) imidazo [4,5-f]-[1,10] phenanthrolin and study of its antitumor activity

Cited by 26 publications

References 51 publications

Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity

Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity

Potent Zinc(II)-Based Immunogenic Cell Death Inducer Triggered by ROS-Mediated ERS and Mitochondrial Ca2+ Overload

Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety

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Potent Zinc(II)-Based Immunogenic Cell Death Inducer Triggered by ROS-Mediated ERS and Mitochondrial Ca²⁺ Overload