title: Synthesis of 5- and 6-N-heterocyclic methylenebisphosphonate derivatives and evaluation of their cytogenetic activity in normal human lymphocyte cultures.
abstract: Methods for the preparation of various aminomethylene bisphosphonates were developed. The required bisphosphonates were obtained by applying tetraethyl methylenebisphosphonate reagent to different types of oxazinones and the relevant Schiff base derivatives. Based on the prediction results (Pass program), we further estimated the sister chromatid exchange frequency and proliferation rate index values of human lymphocyte cultures after the administration of four newly synthesized bisphosphonates in order to evaluate their cytotoxic/cytostatic and possible antineoplastic potency. The results showed that all four bisphosphonates cause a dose-dependent increase in sister chromatid exchange frequency, followed by a decrease in proliferation rate index in both experiments compared to the control.
authors.affiliation: Chemical Industries Division, National Research Centre, Elbohouth St., Dokki, Cairo, Egypt.
authors.forename: Wafaa M
authors.initials: WM
authors.lastname: Abdou
authors.forename: Azza A
authors.initials: AA
authors.lastname: Kamel
authors.forename: Rizk E
authors.initials: RE
authors.lastname: Khidre
authors.forename: Athina
authors.initials: A
authors.lastname: Geronikaki
authors.forename: Maria T
authors.initials: MT
authors.lastname: Ekonomopoulou
mesh_terms: D000328:Adult; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D004164:Diphosphonates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008214:Lymphocytes / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D008745:Methylation; D012854:Sister Chromatid Exchange / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D004164:Diphosphonates; D006571:Heterocyclic Compounds