|
KMID : 0043320180410030251
|
|
Archives of Pharmacal Research
2018 Volume.41 No. 3 p.251 ~ p.258
|
|
|
Identification of N-arylsulfonylpyrimidones as anticancer agents
|
|
Subramanian Santhosh
Boggu Pulla Reddy
Yun Ji-Eun
Jung Sang-Hun
|
|
|
Abstract
|
|
|
|
For confirming the role of five membered ring of imidazolidinone moiety of N-arylsulfonylimidazolidinones (7) previously reported with highly potent anticancer agent, a series of N-arylsulfonylpyrimidones (10a?g) and N-arylsulfonyltetrahydropyrimidones (11a?e) were prepared and their anti-proliferating activity was measured against human cancer cell lines (renal ACHN, colon HCT-15, breast MDA-MB-231, lung NCI-H23, stomach NUGC-3, and prostate PC-3) using XTT assay. Among them, 1-(1-acetylindolin-5-ylsulfonyl)-4-phenyltetrahydropyrimidin-2(1H)-one (11d, mean GI50 = 3.50 μM) and ethyl 5-(2-oxo-4-phenyltetrahydropyrimidin-1(2H)-ylsulfonyl)-indoline-1-carboxylate (11e, mean GI50 = 0.26 μM) showed best growth inhibitory activity against human cancer cell lines. Considering the activity results, N-arylsulfonyltetrahydropyrimidones (11) exhibited more potent activity compared to N-arylsulfonylpyrimidones (10) and comparable activity to N-arylsulfonylimidazolidinones (7). Especially, tetrahydropyrimidin-2(1H)-one analogs containing acylindolin-5-ylsulfonyl moiety at position 1 demonstrated their strong growth inhibitory activity against human cancer cell lines.
|
|
|
KEYWORD
|
|
|
N-arylsulfonylpyrimidones, N-arylsulfonyltetrahydropyrimidones, Anticancer activity, Antimitotic agent
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|
|