ChemInform Abstract: Synthesis and SAR of Aziridinylquinoline‐5,8‐diones as Agents Against Malignant Tumor Cells.

Yoo, Kyung Ho; Yoon, Eun Young; Park, Yoon Young; Park, Sang Woo; Lee, Chong‐Ock; Lee, Won Koo; Yoon, Dae; Kim, Dong Jin

doi:10.1002/chin.200217132

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2019

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“…Connection of 5,8-quinolinedione with a 2-methylaziridinyl fragment led to compounds 55 – 57 and 58 – 60 (Figure 9), which exhibited a moderate activity depending on the R group. The research showed that the substituent type affects cytotoxic activity as follows: amine ( 57 and 60 ) > methoxy ( 56 and 59 ) > chloride ( 55 and 58 ) [72].…”

Section: Biological Activitymentioning

confidence: 99%

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5,8-Quinolinedione Scaffold as a Promising Moiety of Bioactive Agents

et al. 2019

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Natural 5,8-quinolinedione antibiotics exhibit a broad spectrum of activities including anticancer, antibacterial, antifungal, and antimalarial activities. The structure–activity research showed that the 5,8-quinolinedione scaffold is responsible for its biological effect. The subject of this review report is a presentation of the pharmacological activity of synthetic 5,8-quinolinedione compounds containing different groups at C-6 and/or C-7 positions. The relationship between the activity and the mechanism of action is included if these data have been included in the original literature. The review mostly covers the period between 2000 and 2019. Previously published literature data were used to present historical points.

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Section: Biological Activitymentioning

confidence: 99%

“…A comparison of activities in both series of compounds showed that the derivatives containing the aziridinyl moiety at the C-6 position ( 58 – 60 ) were characterized by a higher cytotoxicity against the SK-OV-3, SK-MEL-2, and XF498 cell lines than the C-7 analogues 55 – 57 [72].…”

Section: Biological Activitymentioning

confidence: 99%