title: Asymmetric synthesis and evaluation of α-quaternary chiral lactam derivatives as novel anticancer agents.
abstract: Asymmetric synthesis of α-quaternary chiral lactam derivatives as novel anticancer agents and evaluation of their cytotoxic potentials and spectrums are reported. Among the developed lactam derivatives, the most active new compounds (S)-4m and (S)-4n synthesized via asymmetric phase-transfer catalytic alkylation in very high optical yields (98 % ee) show promising in vitro anticancer activities with low micromolar IC50 values against colon, uterus, lung, and breast human cancer cells.
authors.affiliation: College of Pharmacy, Inje University, 607 Obang-dong, Gimhae, 621-749, Gyeongnam, Korea.
authors.forename: Hwanhyuk
authors.initials: H
authors.lastname: Lee
authors.forename: Su Jung
authors.initials: SJ
authors.lastname: Hwang
authors.forename: Jisung
authors.initials: J
authors.lastname: Jung
authors.forename: Suckchang
authors.initials: S
authors.lastname: Hong
authors.forename: Myungmo
authors.initials: M
authors.lastname: Lee
authors.forename: Hyeung-geun
authors.initials: HG
authors.lastname: Park
authors.forename: Hyo-Jong
authors.initials: HJ
authors.lastname: Lee
authors.forename: Yohan
authors.initials: Y
authors.lastname: Park
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007769:Lactams / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007769:Lactams