Archives of Pharmacal Research

, Volume 41, Issue 3, pp 251–258 | Cite as

Identification of N-arylsulfonylpyrimidones as anticancer agents

  • Santhosh Subramanian
  • Pulla Reddy Boggu
  • Jieun Yun
  • Sang-Hun JungEmail author
Research Article


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.


N-arylsulfonylpyrimidones N-arylsulfonyltetrahydropyrimidones Anticancer activity Antimitotic agent 



This work was supported by Research Fund of the Chungnam National University.

Supplementary material

12272_2018_1003_MOESM1_ESM.docx (685 kb)
Supplementary material 1 (DOCX 684 kb)


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Copyright information

© The Pharmaceutical Society of Korea 2018

Authors and Affiliations

  • Santhosh Subramanian
    • 1
  • Pulla Reddy Boggu
    • 1
  • Jieun Yun
    • 2
  • Sang-Hun Jung
    • 1
    Email author
  1. 1.College of Pharmacy and Institute of Drug Research and DevelopmentChungnam National UniversityDaejeonRepublic of Korea
  2. 2.Department of Pharmaceutical EngineeringCheongju UniversityCheongjuRepublic of Korea

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