title: Design, synthesis and antiproliferative activity of novel 2-substituted-4-amino-6-halogenquinolines.
abstract: Two series of novel 2-substituted-4-amino-6-halogenquinolines 8a-l and 13a-h were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl substituents exhibited good to excellent antiproliferative activity. Among them, compound 8e was a considered promising lead for further structural modifications with IC₅₀ values of 0.03 μM, 0.55 μM, 0.33 μM and 1.24 μM, which was 2.5- to 186-fold more active than gefitinib and compound 1.
authors.affiliation: Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, China.
authors.forename: Nan
authors.initials: N
authors.lastname: Jiang
authors.forename: Xin
authors.initials: X
authors.lastname: Zhai
authors.forename: Ting
authors.initials: T
authors.lastname: Li
authors.forename: Difa
authors.initials: D
authors.lastname: Liu
authors.forename: Tingting
authors.initials: T
authors.lastname: Zhang
authors.forename: Bin
authors.initials: B
authors.lastname: Wang
authors.forename: Ping
authors.initials: P
authors.lastname: Gong
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D000077156:Gefitinib; D006801:Humans; D020128:Inhibitory Concentration 50; D011799:Quinazolines / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011799:Quinazolines; D011804:Quinolines; D000077156:Gefitinib