Structure and anti-proliferation function of 5,5-diphenyl-2-thiohydantoin (DPTH) derivatives in vascular endothelial cells

Cheng Kuo Cheng, Jender Wu, Yuan Liu, Tong Sheng Lee, Shuo Jhen Kang, Ming Thau Sheu, Wen Sen Lee

研究成果: 雜誌貢獻文章

8 引文 (Scopus)

摘要

Previously, we identified DPTH, an analogue of antiepileptic drug phenytoin (5,5-diphenylhydantoin, DPT), capable of retarding the cell cycle in the human vascular endothelial cells. Our data suggest that DPTH inhibits human umbilical venous endothelial cells (HUVEC) proliferation by increasing the level of p21 protein, which in turn inhibits the activities of cyclin-dependent kinase (CDK)2 and CDK4, and finally interrupts the cell cycle. To search chemicals with more potency in anti-angiogenic activity, we designed and synthesized several chemical compounds based on the structure-activity relationship consideration. We evaluated the anti-angiogenic activity of these compounds by examining their effects on DNA synthesis, cell number, p21 induction and capillary-like tube formation. Our results showed that introduction of side chain containing an aromatic ring structure with right spatial arrangement at sulfur atom of DPTH enhanced the anti-angiogenic activity in HUVEC.

原文英語
頁(從 - 到)138-142
頁數5
期刊Vascular Pharmacology
48
發行號2-3
DOIs
出版狀態已發佈 - 二月 2008

指紋

Umbilicus
Endothelial Cells
Phenytoin
Cell Cycle
Cyclin-Dependent Kinase 2
Structure-Activity Relationship
Sulfur
Human Activities
Anticonvulsants
Cell Count
Cell Proliferation
DNA
diphenylthiohydantoin
Proteins

ASJC Scopus subject areas

  • Pharmacology

引用此文

Structure and anti-proliferation function of 5,5-diphenyl-2-thiohydantoin (DPTH) derivatives in vascular endothelial cells. / Cheng, Cheng Kuo; Wu, Jender; Liu, Yuan; Lee, Tong Sheng; Kang, Shuo Jhen; Sheu, Ming Thau; Lee, Wen Sen.

於: Vascular Pharmacology, 卷 48, 編號 2-3, 02.2008, p. 138-142.

研究成果: 雜誌貢獻文章

Cheng, Cheng Kuo ; Wu, Jender ; Liu, Yuan ; Lee, Tong Sheng ; Kang, Shuo Jhen ; Sheu, Ming Thau ; Lee, Wen Sen. / Structure and anti-proliferation function of 5,5-diphenyl-2-thiohydantoin (DPTH) derivatives in vascular endothelial cells. 於: Vascular Pharmacology. 2008 ; 卷 48, 編號 2-3. 頁 138-142.
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AU - Cheng, Cheng Kuo

AU - Wu, Jender

AU - Liu, Yuan

AU - Lee, Tong Sheng

AU - Kang, Shuo Jhen

AU - Sheu, Ming Thau

AU - Lee, Wen Sen

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KW - Capillary-like tube formation

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KW - Endothelial cells

KW - p21

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