title: [Inhibitory activity of dioxy-pyrrolino [3', 4'-d]isoxazoline derivatives containing (1', 2'-O-cyclohexylidendioxyethyl) against Cdc25A and CD45].
abstract: Fifteen 3-(1', 2'-di-O-cyclohexylidendioxyethyl)-5-aryl-3a, 6a-dihydro-4, 6-dioxo-pyrrolino[3', 4'-d] isoxazoline derivatives (3a-3o) were synthesized by 1, 3-dipolar cycloaddition reaction of N-arylmaleimides and the nitrile oxide in situ generated from 2, 3-O-cyclohexylidene-D-glycerohydroximoyl chloride, in the presence of triethylamine. The structures of the target compounds 3a-3o were characterized by 1H NMR, IR and elemental analysis. The preliminary bioassay on the compounds showed that some compounds possess in vitro anticancer activity and the leukocyte common antigen activity to a different extent. The compounds 3e, 3h, 3j and 31 showed Cdc25A phosphatase inhibitory activity of 60.6%, 58.6%, 51.4% and 98.4% respectively at the test concentration of 20 microg x mL(-1), and among them 31 had inhibition rate of 86.97% even at the concentration as low as 5 microg x mL(-1), indicating worthy to be future studied. The compounds 3e, 31 and 3n showed an inhibitory activity of 57.7%, 74.4% and 77.3% on CD45 protein tyrosine phosphatase A, respectively, at the test concentration of 20 micromol x mL(-1). The structure-activity relationship of 3-(1', 2'-di-O-cyclohexylidendioxyethyl)-5-aryl-3a, 6a- dihydro-4, 6-dioxo-pyrrolino[3', 4'-d]isoxazoline derivatives was also discussed.
authors.affiliation: College of Chemistry and Chemical Engineering, Xinjiang University, Urumqi 830046, China.
authors.forename: Aynur
authors.initials: A
authors.lastname: Hudabergen
authors.forename: Abdukaiyum
authors.initials: A
authors.lastname: Abdurashid
authors.forename: Mukhtar
authors.initials: M
authors.lastname: Imerhasan
authors.forename: Turmuhammad
authors.initials: T
authors.lastname: Ali
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017493:Leukocyte Common Antigens / Q000037:antagonists & inhibitors*; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D007555:Isoxazoles; D011758:Pyrroles; D017493:Leukocyte Common Antigens; D020687:cdc25 Phosphatases