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Arch Pharm Res. 2018 Mar;41(3):251-258. doi: 10.1007/s12272-018-1003-9. Epub 2018 Jan 13.

Identification of N-arylsulfonylpyrimidones as anticancer agents.

Author information

1
College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon, 34134, Republic of Korea.
2
Department of Pharmaceutical Engineering, Cheongju University, Cheongwon-gu, Cheongju, 28503, Republic of Korea.
3
College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon, 34134, Republic of Korea. jungshh@cnu.ac.kr.

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.

KEYWORDS:

Anticancer activity; Antimitotic agent; N-arylsulfonylpyrimidones; N-arylsulfonyltetrahydropyrimidones

PMID:
29332183
DOI:
10.1007/s12272-018-1003-9
[Indexed for MEDLINE]

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