title: Synthesis and cytotoxic evaluation of novel N-substituted amidino-1-hydroxybenzimidazole derivatives.
abstract: A new class of N-substituted amidino-1-hydroxybenzimidazole derivatives (15-24) were synthesized and evaluated for their in vitro cytotoxic activities against human leukemia cell lines, HL-60 and K562. The preliminary results showed that compounds 16, 20, 21 and 23 had moderate antitumor activity against HL-60 cell line. Further investigation on the mechanism of the observed cytotoxic effects demonstrated that compound 21 increased the expression of autophagic and apoptotic genes and induced apoptosis of HL-60 cells.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100, Tandogan, Ankara, Turkey, malp@pharmacy.ankara.edu.tr.
authors.forename: Mehmet
authors.initials: M
authors.lastname: Alp
authors.forename: Hakan
authors.initials: H
authors.lastname: Göker
authors.forename: Tulin
authors.initials: T
authors.lastname: Ozkan
authors.forename: Asuman
authors.initials: A
authors.lastname: Sunguroglu
mesh_terms: D000578:Amidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects / Q000235:genetics; D051017:Apoptosis Regulatory Proteins / Q000235:genetics / Q000378:metabolism; D001343:Autophagy / Q000187:drug effects / Q000235:genetics; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015972:Gene Expression Regulation, Neoplastic; D018922:HL-60 Cells; D006801:Humans; D020014:K562 Cells; D015394:Molecular Structure; D012333:RNA, Messenger / Q000378:metabolism
chemical_list: D000578:Amidines; D000970:Antineoplastic Agents; D051017:Apoptosis Regulatory Proteins; D001562:Benzimidazoles; D012333:RNA, Messenger