Synthesis and biological research of novel azaacridine derivatives as potent DNA-binding ligands and topoisomerase II inhibitors

Li, Dan; Yuan, Zigao; Chen, Shaopeng; Zhang, Cunlong; Song, Lu; Gao, Chunmei; Chen, Yu Zong; Tan, Chunyan; Jiang, Yuyang

doi:10.1016/j.bmc.2017.04.030

Cited by 17 publications

(2 citation statements)

References 34 publications

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“…According to the above experiments, compounds 7d and 8d could inhibit the activity of Topo II and interact with DNA, which may induce apoptosis in cancer cell lines. Annexin V and PI dual staining assay was used to detect early and late apoptotic cells (annexin-V + /PI − and annexin-V + /PI + ), necrotic (annexin-V − /PI + ) as well as viable cells (annexin-V − /PI − ) [41] . As showed in Fig.…”

Section: Annexin V-fitc/pi (Av/pi) Dual Staining Assaymentioning

confidence: 99%

Synthesis and biological evaluation of xanthone derivatives as anti-cancer agents targeting topoisomerase II and DNA

et al. 2022

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Topoisomerase is one of the most important targets of anticancer drugs. In order to develop effective and low-toxic topoisomerase inhibitors, a series of xanthone derivatives have been designed and synthesized using the principles of skeleton transition. In vitro growth inhibition experiments of human breast cancer(MCF-7), gastric cancer (MGC-803), and cervical cancer(Hela) cell lines were used to evaluate the compound's anti-tumor cell proliferation activity. Most of the compounds showed anti-tumor growth activity, and also showed low toxicity to human normal cells L929. In the enzyme activity inhibition experiment, compounds 7d and 8d showed the best inhibitory activity. The DNA binding studies disclosed that the most potent compounds 7d and 8d can intercalate into DNA, induce apoptosis in MGC-803 cells and arrested at G2/M phase. Molecular docking showed that compounds 7d and 8d could bind with topoisomerase II and DNA through hydrogen bonds and π-stacking interactions.

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Section: Annexin V-fitc/pi (Av/pi) Dual Staining Assaymentioning

confidence: 99%

Synthesis and biological evaluation of xanthone derivatives as anti-cancer agents targeting topoisomerase II and DNA

et al. 2022

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“…Interestingly, 9-amino-azaacridine derivatives bearing the same chloro and methoxy substituents as PYR on the benzo-naphthyridine tricyclic core were found to function as potent DNA-binding Topo2 poisons and inducing apoptosis of cancer cells. [107] 6 | DISCUSSION Pyronaridine is a potent anti-malarial drug, used in combination with artesunate to treat uncomplicated P. falciparum infections in many counties. This drug is useful to limit the appearance of artemisininresistance.…”

Section: Anticancer Activity Of Pyronaridinementioning

confidence: 99%

Pyronaridine: An update of its pharmacological activities and mechanisms of action

Bailly

2020

Biopolymers

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Pyronaridine (PYR) is an erythrocytic schizonticide with a potent antimalarial activity against multidrug-resistant Plasmodium. The drug is used in combination with artesunate for the treatment of uncomplicated P. falciparum malaria, in adults and children. The present review briefly retraces the discovery of PYR and recent antimalarial studies which has led to the approval of PYR/artesunate combination (Pyramax) by the European Medicines Agency to treat uncomplicated malaria worldwide. PYR Pyronaridine (PYR, Figure 1), initially known as "antimalaria drug 7351", is a benzo-naphthyridine derivative originally synthesized in 1979 [1] and developed in China from the early 1980s. [2][3][4] Rapidly, experimental studies demonstrated that this compound was more active than chloroquine against different isolates of Plasmodium falciparum, the malaria pathogen.

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Acridine derivatives as inhibitors/poisons of topoisomerase II

Kožurková

2021

J of Applied Toxicology

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The potential of acridines (amsacrine) as a topoisomerase II inhibitor or poison was first discovered in 1984, and since then, a considerable number of acridine derivatives have been tested as topoisomerase inhibitors/poisons, containing different substituents on the acridine chromophore. This review will discuss a series of studies published over the course of the last decade, which have investigated various novel acridine derivatives against topoisomerase II activity.

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Synthesis and biological research of novel azaacridine derivatives as potent DNA-binding ligands and topoisomerase II inhibitors

Cited by 17 publications

References 34 publications

Synthesis and biological evaluation of xanthone derivatives as anti-cancer agents targeting topoisomerase II and DNA

Synthesis and biological evaluation of xanthone derivatives as anti-cancer agents targeting topoisomerase II and DNA

Pyronaridine: An update of its pharmacological activities and mechanisms of action

Acridine derivatives as inhibitors/poisons of topoisomerase II

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