title: Synthesis and anticancer activity of a novel class of flavonoids: 2,4-diarylchromane[4,3-d]-delta(1,9b)-1,2,3-thiadiazolines.
abstract: A series of 2,4-diarylchromane[4,3-d]-Delta(1,9b)-1,2,3-thiadiazolines have been synthesized by cyclization of corresponding 2-arylchroman-4-one-arylhydrazones with SOCl(2) then treated with alcohol. All the compounds have been tested for their antiproliferative activity in vitro against six human tumor cell lines, and the highly potent derivative 11a exhibited in vivo inhibitory effect on tumor growth. Mechanism research indicated that it is due to 11a that induces DNA fragmentation.
authors.affiliation: ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang 310058, China.
authors.forename: Huazhou
authors.initials: H
authors.lastname: Ying
authors.forename: Yongzhou
authors.initials: Y
authors.lastname: Hu
authors.forename: Qiaojun
authors.initials: Q
authors.lastname: He
authors.forename: Runping
authors.initials: R
authors.lastname: Li
authors.forename: Bo
authors.initials: B
authors.lastname: Yang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002839:Chromans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D053938:DNA Fragmentation; D004354:Drug Screening Assays, Antitumor; D005419:Flavonoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D021241:Spectrometry, Mass, Electrospray Ionization; D013055:Spectrophotometry, Infrared; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D002839:Chromans; D005419:Flavonoids; D013830:Thiadiazoles