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- Title
Design, synthesis, and cytotoxic evaluation of novel furo[2,3‐b]quinoline derivatives.
- Authors
Wang, Bing; Li, Qiangqiang; Shi, Wei; Chen, Li; Sun, Jianbo
- Abstract
A number of novel furo[2,3‐b]quinoline derivatives were designed and synthesized by introducing benzyl ether, benzoate, and benzenesulfonate to 6‐position of furo[2,3‐b]quinoline and their chemical structures were confirmed by ESI‐MS, 1H NMR, and 13C NMR spectra. All target compounds were evaluated in vitro against four human cancer cell lines (HCT‐116, MCF‐7, U2OS, and A549) by MTT method. Cytotoxic assay showed that compounds <bold>8a</bold>,<bold> 8e</bold>,<bold> 10a</bold>,<bold> 10b,</bold> and <bold>10c</bold> exhibited more potent cytotoxicities compared to 2‐bromine‐6‐hydroxy‐furo‐[2,3‐b]quinoline (<bold>7</bold>). Compound <bold>10c</bold> exhibited higher antiproliferative activity (IC50 values ranging from 4.32 to 24.96 μ m) against four human cancer cell lines (HCT‐116, MCF‐7, U2OS, and A549) and weak cytotoxicity on normal cell HL‐7702, which suggested that <bold>10c</bold> might be an ideal anticancer candidate. Compounds <bold>8a</bold>,<bold> 10a</bold>,<bold> 10b</bold> showed good selectivities to MCF‐7 and HCT‐116, which could be considered as ideal selective candidates for further study. The SARs showed that the introduction of the benzyl ether and benzenesulfonate could significantly improve cytotoxicities, while the benzoate failed to enhance potency obviously.
- Subjects
ANTINEOPLASTIC agents; QUINOLINE; AROMATIC compounds; CELL-mediated cytotoxicity; BENZENESULFONATES; THERAPEUTICS
- Publication
Chemical Biology & Drug Design, 2018, Vol 91, Issue 4, p957
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13154