title: Efficient synthesis and antiproliferative activity of novel thioether-substituted flavonoids.
abstract: As widely occurring natural products, flavonoids are an important source for drug discovery, due to their structural diversity and broad-spectrum biological activity. In this work, a library of novel, thioether-substituted flavonoids with diverse heterocyclic groups was synthesized via a microwave-assisted procedure with the advantages of good yields, short times, mild conditions and ready isolation of the products. Their antiproliferative activities were evaluated against six cancer cell lines, HCCLM-7, Hela, MDA-MB-435S, SW-480, Hep-2, and MCF-7 by the MTT-based assay. Compared with the positive control 5-fluorouracil, three compounds, 6a, 6b and 6j were successfully identified as the most promising candidates, due to their higher potency and broad-spectrum bioactivity with IC50 values in the range of 0.43 μM-6.7 μM.
authors.affiliation: Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Huang
authors.forename: Qiong
authors.initials: Q
authors.lastname: Chen
authors.forename: Wen-Chao
authors.initials: WC
authors.lastname: Yang
authors.forename: Guang-Fu
authors.initials: GF
authors.lastname: Yang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D005419:Flavonoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D013440:Sulfides / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D005419:Flavonoids; D013440:Sulfides
keywords: Antiproliferative activity; Chromone; Flavonoids; Microwave-assisted synthesis; Thioether