title: Synthesis and biological evaluation of novel cytotoxic azanaphthoquinone annelated pyrrolo oximes.
abstract: Two series of azanaphthoquinone annelated pyrrolo oximes have been synthesized. The antiproliferative activities of 10 compounds were evaluated on at least four different cell lines. One series of pyrrolo derivatives showed high cytotoxic activity. The effects on cell cycle and caspase activity were investigated. Compounds 9a and 9b showed an accumulation of cells in G2/M phase. Substantial and dose-dependent caspase activity was found after treatment of cells with 9a and 9b. This indicates an apoptosis inducing property of these compounds.
authors: Department of Drug and Natural Product Synthesis, University of Vienna, Althanstrasse 14, Vienna, Austria.
authors: Karem
authors: K
authors: Shanab
authors: Nipawan
authors: N
authors: Pongprom
authors: Eva
authors: E
authors: Wulz
authors: Wolfgang
authors: W
authors: Holzer
authors: Helmut
authors: H
authors: Spreitzer
authors: Peter
authors: P
authors: Schmidt
authors: Babette
authors: B
authors: Aicher
authors: Gilbert
authors: G
authors: Müller
authors: Eckhard
authors: E
authors: Günther
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D020169:Caspases / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D008942:Mitoxantrone / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D015394:Molecular Structure; D009285:Naphthoquinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010091:Oximes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D009285:Naphthoquinones; D010091:Oximes; D011758:Pyrroles; D008942:Mitoxantrone; D020169:Caspases