Identification of N-arylsulfonylpyrimidones as anticancer agents
| Autor: | Sang-Hun Jung, Pulla Reddy Boggu, Jieun Yun, Santhosh Subramanian |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Imidazolidinone Antineoplastic Agents Pyrimidinones Pharmacology 010402 general chemistry 01 natural sciences Structure-Activity Relationship 03 medical and health sciences Prostate Cell Line Tumor Drug Discovery medicine Humans Moiety Structure–activity relationship Arylsulfonates Chemistry Stomach Organic Chemistry 0104 chemical sciences 030104 developmental biology medicine.anatomical_structure Cell culture Molecular Medicine Xtt assay Drug Screening Assays Antitumor Human cancer |
| Zdroj: | Archives of Pharmacal Research. 41:251-258 |
| ISSN: | 1976-3786 0253-6269 |
| DOI: | 10.1007/s12272-018-1003-9 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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