title: Synthesis and evaluation of the anti-proliferative activity of diaryl-3-pyrrolin-2-ones and fused analogs.
abstract: Analogs containing a central 3-pyrrolin-2-one core with different methoxyphenyl and/or indole substituents were prepared and tested for anti-proliferative activity in U-937 cells. The most efficacious analogs were non-rigid, (non-fused) contained methoxyaryl groups located at the 4-position, and contained either methoxyaryl or indole groups located at the 3-position. Both the number of methoxy groups contained in the substituents and the particular location of the indole rings with respect to the lactam carbonyl had significant affects on anti-proliferative activity. This work provides a framework to better understand structure-activity relationships for inducing anti-proliferative activity in diaryl heterocyclic scaffolds.
authors.affiliation: Department of Biology, Hobart and William Smith Colleges, Geneva, NY 14456, USA. Electronic address: mowery@hws.edu.
authors.forename: Patricia
authors.initials: P
authors.lastname: Mowery
authors.affiliation: Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA.
authors.forename: Fernando
authors.initials: F
authors.lastname: Banales Mejia
authors.affiliation: Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA.
authors.forename: Courtney L
authors.initials: CL
authors.lastname: Franceschi
authors.affiliation: Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA.
authors.forename: Maeve H
authors.initials: MH
authors.lastname: Kean
authors.affiliation: Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA.
authors.forename: Deborah O
authors.initials: DO
authors.lastname: Kwansare
authors.affiliation: Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA.
authors.forename: Megan M
authors.initials: MM
authors.lastname: Lafferty
authors.affiliation: Department of Biology, Hobart and William Smith Colleges, Geneva, NY 14456, USA.
authors.forename: Namita D
authors.initials: ND
authors.lastname: Neerukonda
authors.affiliation: Department of Biology, Hobart and William Smith Colleges, Geneva, NY 14456, USA; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA.
authors.forename: Carly E
authors.initials: CE
authors.lastname: Rolph
authors.affiliation: Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA.
authors.forename: Nathanyal J
authors.initials: NJ
authors.lastname: Truax
authors.affiliation: Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA. Electronic address: pelkey@hws.edu.
authors.forename: Erin T
authors.initials: ET
authors.lastname: Pelkey
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003500:Cyclization; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D011760:Pyrrolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D006576:Heterocyclic Compounds, 4 or More Rings; D011760:Pyrrolidinones
keywords: Anti-cancer; Indoles; Lactams; MTT