A New Series of Cycloalkane-fused Coumarin Sulfonates: Synthesis and In Vitro Antiproliferative Screening
- A New Series of Cycloalkane-fused Coumarin Sulfonates: Synthesis and In Vitro Antiproliferative Screening
- 오창현; 모하메드엘가말; 백대진
- Anticancer; Antiproliferative; Cycloalkane-fused coumarin; In silico studies
- Issue Date
- Bulletin of the Korean Chemical Society
- VOL 37, NO 2-191
- In this paper, we report the synthesis of 14 new cycloalkane-fused tricyclic coumarin sulfonate derivatives. They were examined for in vitro anticancer activity against NCI-57 cancer cell line panel of nine different cancer types. Among all the target analogs, compounds 1c, 1e, and 1n showed the highest activities. Compound 1e exerted the highest percentage growth inhibition (91.91%) against SNB-75 CNS cancer cell line at 10 mu M concentration and was more active than carmustine against this cell line. Compound 1c also showed strong activity against HT29 colon, ACHN renal, and PC-3 prostate cancer cell lines. Furthermore, compound 1n was selective toward the HT29 colon cancer cell line. Compounds 1c, 1e, and 1n showed superior selectivity against cancer cell lines compared to the noncancerous RAW 264.7 macrophages. The in silico predictions estimate the oral bioavailability, which is in compliance with Lipinski's rule of five.
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