title: Synthesis and antileukemic activity of novel 2-(4-(2,4-dimethoxybenzoyl)phenoxy)-1-(4-(3-(piperidin-4-yl)propyl)piperidin-1-yl)ethanone derivatives.
abstract: A series of novel 2-(4-(2,4-dimethoxybenzoyl)phenoxy)-1-(4-(3-(piperidin-4-yl)propyl) piperidin-1-yl)ethanone derivatives 9(a-e) and 10(a-g) were synthesized and characterized by (1) H NMR, IR, mass spectral, and elemental analysis. These novel compounds were evaluated for their antileukemic activity against two human leukemic cell lines (K562 and CEM) by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide assay. Some of the tested compounds showed good antiproliferative activity with IC(50) values ranging from 1.6 to 8.0 μm. Compound 9c, 9e, and 10f with an electron-withdrawing halogen substituent at the para position on the phenyl ring showed excellent in vitro potency against tested human leukemia cells (K562 and CEM).
authors.forename: Kambappa
authors.initials: K
authors.lastname: Vinaya
authors.forename: Chandagirikoppal V
authors.initials: CV
authors.lastname: Kavitha
authors.forename: Doddakunche S
authors.initials: DS
authors.lastname: Prasanna
authors.forename: Siddappa
authors.initials: S
authors.lastname: Chandrappa
authors.forename: Somasagara R
authors.initials: SR
authors.lastname: Ranganatha
authors.forename: Sathees C
authors.initials: SC
authors.lastname: Raghavan
authors.forename: Kanchugarakoppal S
authors.initials: KS
authors.lastname: Rangappa
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001577:Benzophenones / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007938:Leukemia; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology
chemical_list: C572060:4-(3-(1-(2-(4-(2,4-dimethoxybenzoyl)phenoxy)acetyl)piperidin-4-yl)propyl)-N-(4-fluorophenyl)piperidine-1-carboxamide; D000970:Antineoplastic Agents; D001577:Benzophenones; C572062:N-(4-chlorophenyl)-4-(3-(1-(2-(4-(2,4--dimethoxybenzoyl)phenoxy)acetyl)piperidin-4-yl)propyl)piperidine-1-carbothioamide; C572061:N-(4-chlorophenyl)-4-(3-(1-(2-(4-(2,4-dimethoxybenzoyl)phenoxy)acetyl)piperidin-4-yl)propyl)piperidine-1-carboxamide; D010880:Piperidines; C032727:piperidine