Synthesis and evaluation of novel phosphasugar anticancer agents

Autor:	Mayumi Yamaoka, Nobuhisa Ozaki, Keita Kiyofuji, Satoki Nakamura, Junko Yamashita, Akiho Sawada, Mitsuji Yamashita, Kazuhide Asai, Mitsuo Toda, Masaki Sugiyama, Taishi Niimi, Manabu Yamada, Reiko Makita, Michio Fujie, Takuya Suyama, Kazunori Ohnishi
Rok vydání:	2011
Předmět:	Antitumor activity medicine.diagnostic_test Stereochemistry General Chemical Engineering General Chemistry In vitro Leukemia cell line Flow cytometry Comparative evaluation chemistry.chemical_compound chemistry Biochemistry Apoptosis medicine Dichlorophenylphosphine K562 cells
Zdroj:	Pure and Applied Chemistry. 84:37-48
ISSN:	1365-3075 0033-4545
DOI:	10.1351/pac-con-11-10-09
Popis:	Starting materials of phosphasugars, 1-phenyl-2-phospholene 1-oxides, were prepared from dienes and phenylphosphonous dichloride (dichlorophenylphosphine). Several substituted novel phosphasugars (3- or 4-halo-substituted)-1-phenyl-2-phospholene 1-oxides as well as 1-phenyl-2-phospholane 1-oxides were prepared from 2-phospholenes. The synthesized compounds were evaluated for their antitumor activities against the leukemia cell lines (U937 and K562) by in vitro 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. 2,3,4-Tribromo-3-methyl-1-phenylphospholane 1-oxide showed superior antitumor activity against U937 and K562 cell lines in a comparative evaluation with Glivec. The analysis by flow cytometry implied that 2,3-dibromo-3-methyl-1-phenylphospholane 1-oxide induced apoptosis to leukemia cell lines.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::58d5701661e00fe84110ab816dfe82fd https://doi.org/10.1351/pac-con-11-10-09 Zobrazit plný text záznamu