2015
DOI: 10.1016/j.ejmech.2015.08.032
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Design, synthesis and evaluation of thiohydantoin derivatives as potent topoisomerase I (Top1) inhibitors with anticancer activity

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Cited by 70 publications
(61 citation statements)
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“…Camptothecin, the first small molecule targeting Top I for the treatment of advanced digestive carcinoma in clinical2331, which stabilizes the DNA cleavable complex to block the transient breaking and rejoining of DNA173233 and has been used as the Top I poison for the treatment of many digestive solid tumors widely34, was served as the positive control. As shown in Fig.…”
Section: Resultsmentioning
confidence: 99%
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“…Camptothecin, the first small molecule targeting Top I for the treatment of advanced digestive carcinoma in clinical2331, which stabilizes the DNA cleavable complex to block the transient breaking and rejoining of DNA173233 and has been used as the Top I poison for the treatment of many digestive solid tumors widely34, was served as the positive control. As shown in Fig.…”
Section: Resultsmentioning
confidence: 99%
“…The molecular docking simulations between Top I and hippeastrine was carried out using the Genetic Algorithm of AutoDock 4.2 software52. Briefly, the 3D structure of hippeastrine was established with MOE Molecule Builder tool, and then its energy minimization was executed by the MMFF94× force field.…”
Section: Methodsmentioning
confidence: 99%
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“…18 Thiohydantoin ( 7 ) derivatives have been identified as antimicrobials 19 and antitumor 20 agents with topoisomerase I inhibitory activities. 21 Rhodanine ( 8 ) derivatives are well known beta-lactamase inhibitors. 22,23 Analogues of thiazolidinedione ( 9 ) are peroxisome proliferator-activated receptor (PPAR) agonists and have been used as antidiabetic drugs.…”
mentioning
confidence: 99%
“…Topoisomerases (Topo) are universal nuclear enzymes that modulate DNA supercoiling during DNA replication, transcription, and chromatin assembly by forming a reversible covalent Topo‐DNA complex (Figure ) . Topo I and Topo II are two types of DNA topoisomerases, which cleave single or double DNA strands leading to transient DNA single‐strand breaks or double‐strand breaks, respectively . The mechanism of Topo inhibitors is to stabilize the DNA‐enzyme cleavable complex through intercalation between DNA base pairs.…”
Section: Introductionmentioning
confidence: 99%