title: Preparation of secolycorines against acetylcholinesterase.
abstract: 5,6-Secolycorines possessing a 5,6-dihydrophenanthridine skeleton were facilely prepared from lycorine through chemical transformations, mainly including N-alkylation, Hofmann degradation type reaction, reductive cleavage of trichloroethylcarbonyl moiety, and hydrogenation. Several secolycorine derivatives showed potent inhibitory activity against acetylcholinesterase with the IC(50) value at micromolar range and are more potent than galanthamine.
authors.affiliation: School of Pharmacy, College of Medicine, National Taiwan University, 1 Jen-Ai Rd., Sec. 1, Taipei 100, Taiwan, ROC. shoeilee@ha.mc.ntu.edu.tw
authors.forename: Shoei-Sheng
authors.initials: SS
authors.lastname: Lee
authors.forename: Uppala
authors.initials: U
authors.lastname: Venkatesham
authors.forename: Chitneni Prasad
authors.initials: CP
authors.lastname: Rao
authors.forename: Sio-Hong
authors.initials: SH
authors.lastname: Lam
authors.forename: Jung-Hsin
authors.initials: JH
authors.lastname: Lin
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D000478:Alkylation; D000818:Animals; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D002855:Chromatography, Thin Layer; D031407:Crinum / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004524:Eels; D005702:Galantamine / Q000494:pharmacology; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010617:Phenanthridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared; D013237:Stereoisomerism
chemical_list: D002800:Cholinesterase Inhibitors; D007202:Indicators and Reagents; D010617:Phenanthridines; D005702:Galantamine; D000110:Acetylcholinesterase