Design, synthesis and cytotoxic evaluation of novel furo[2,3-b]quinoline derivatives

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 8a, 8e, 10a, 10b and 10c exhibited more potent cytotoxicities compared to 2-bromine-6-hydroxyfuro-[2,3-b]quinoline (7). Compound 10c exhibited higher anti-proliferative activity (IC₅₀ values ranging from 4.32 to 24.96 μM) against four human cancer cell lines (HCT-116, MCF-7, U2OS and A549) and weak cytotoxicity on normal cell HL-7702, which suggested that 10c might be an ideal anticancer candidate. Compounds 8a, 10a, 10b 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.

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A number of novel furo[2,3-b]quinoline derivatives were designed and synthesized and screened for cytotoxic activities against four human cancer cell lines.

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