title: Design, synthesis and anticancer activity of novel dihydrobenzofuro[4,5-b][1,8]naphthyridin-6-one derivatives.
abstract: On the basis of the chemical structures of psorospermin with a xanthone template and acronycine derivatives with an acridone template, rac-1 and rac-2 constructed on an 1,2-dihydrobenzofuro[4,5-b][1,8]naphthyridin-6(11H)-one scaffold were designed and synthesized as potential anticancer agents. Their anticancer activities were evaluated against five human cancer cell lines. Rac-2 showed similar anticancer activity to doxorubicin and rac-1 exhibited even higher anticancer activity against LNCaP (IC(50)=0.14 μM), DU145 (IC(50)=0.15 μM), PC3 (IC(50)=0.30 μM) and MCF-7 (IC(50)=0.26 μM) cancer lines than doxorubicin and rac-2. Also, rac-1 revealed very potent anticancer activity (IC(50)=0.15 μM) against MCF-7/ADR cell (doxorubicin-resistant breast cancer cell) lines and induced G2/M phase arrest of the cell cycle in MCF-7/ADR cells.
authors: College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan 609-735, Republic of Korea.
authors: Jin-Ah
authors: JA
authors: Kang
authors: Zunhua
authors: Z
authors: Yang
authors: Ji Yeon
authors: JY
authors: Lee
authors: Umasankal
authors: U
authors: De
authors: Tae Hyung
authors: TH
authors: Kim
authors: Ji Young
authors: JY
authors: Park
authors: Hye Jin
authors: HJ
authors: Lee
authors: Yun Jung
authors: YJ
authors: Park
authors: Pusoon
authors: P
authors: Chun
authors: Hyung Sik
authors: HS
authors: Kim
authors: Lak Shin
authors: LS
authors: Jeong
authors: Hyung Ryong
authors: HR
authors: Moon
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015195:Drug Design; D055808:Drug Discovery; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008297:Male; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D044004:Xanthones / Q000737:chemistry / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D009287:Naphthyridines; D044004:Xanthones; C025543:psorospermin