title: Synthesis and Investigation of Novel Spiro-isoxazolines as Anti-Cancer Agents.
abstract: A series of structurally diverse 4-bromo spiro-isoxazolines possessing a variety of aromatic and aliphatic substituents at the 3 position, were synthesized through a 1,3-dipolar cycloaddition followed by intramolecular cyclization of a pendant hydroxyl or carboxylic acid group. The biochemical antiproliferative activity was evaluatedin vitroby using two breast cancer cell lines (MCF-7 and MDA-MB-231) and two prostate cancer cell lines (PC-3 and DU-145) using the MTT viability assay, and the IC50values were obtained. Spiro-isoxazoline derivatives bearing ap-chloro or ano-dichloro aromatic substituent at the 3-position of the isoxazoline showed considerable antitumor activities in all four cell lines with IC50value ranging from 43μM to 56μM.
authors.affiliation: Department of Chemistry & Biochemistry, Jackson State University 1400 J. R. Lynch St, PO Box 17910, Jackson, Ms 39217, USA.
authors.forename: Prasanta
authors.initials: P
authors.lastname: Das
authors.affiliation: Department of Chemistry & Biochemistry, Jackson State University 1400 J. R. Lynch St, PO Box 17910, Jackson, Ms 39217, USA.
authors.forename: Ann O
authors.initials: AO
authors.lastname: Omollo
authors.affiliation: Department of Chemistry & Biochemistry, Jackson State University 1400 J. R. Lynch St, PO Box 17910, Jackson, Ms 39217, USA.
authors.forename: Lungile J
authors.initials: LJ
authors.lastname: Sitole
authors.affiliation: Department of Chemistry & Biochemistry, Jackson State University 1400 J. R. Lynch St, PO Box 17910, Jackson, Ms 39217, USA.
authors.forename: Eric
authors.initials: E
authors.lastname: McClendon
authors.affiliation: Department of Chemistry, University of Portland, Portland, OR 97203, USA.
authors.forename: Edward J
authors.initials: EJ
authors.lastname: Valente
authors.affiliation: Department of Biochemistry, University of Mississippi Medical Center, Jackson, MS, 39216, USA.
authors.forename: Drazen
authors.initials: D
authors.lastname: Raucher
authors.affiliation: Department of Biochemistry, University of Mississippi Medical Center, Jackson, MS, 39216, USA.
authors.forename: Leslie R
authors.initials: LR
authors.lastname: Walker
authors.affiliation: Department of Chemistry & Biochemistry, Jackson State University 1400 J. R. Lynch St, PO Box 17910, Jackson, Ms 39217, USA.
authors.forename: Ashton T
authors.initials: AT
authors.lastname: Hamme
keywords: 1,3-dipolar Cycloaddition; Bioevaluation; Regioselectivity; Spiro-isoxazolines; Stereoselective Intramolecular Cyclization
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