title: Isatin derivatives with activity against apoptosis-resistant cancer cells.
abstract: In a search of small molecules active against apoptosis-resistant cancer cells, a series of isatin-based heterocyclic compounds were synthesized and found to inhibit proliferation of cancer cell lines resistant to apoptosis. The synthesis of these compounds involved a condensation of commercially available, active methylene heterocycles with isatin proceeding in moderate to excellent yields. The heterocyclic scaffolds prepared in the current investigation appear to be a useful starting point for the development of agents to fight cancers with apoptosis resistance, and thus, associated with dismal prognoses.
authors.affiliation: Department of Molecular and Medical Pharmacology, University of California, Los Angeles, CA 90095, United States; Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, United States. Electronic address: nevdokim@chem.ucla.edu.
authors.forename: Nikolai M
authors.initials: NM
authors.lastname: Evdokimov
authors.affiliation: Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, United States.
authors.forename: Igor V
authors.initials: IV
authors.lastname: Magedov
authors.affiliation: Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, United States.
authors.forename: Dominic
authors.initials: D
authors.lastname: McBrayer
authors.affiliation: Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, United States; Department of Chemistry and Biochemistry, Texas State University, San Marcos, TX 78666, United States. Electronic address: a_k76@txstate.edu.
authors.forename: Alexander
authors.initials: A
authors.lastname: Kornienko
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007510:Isatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009369:Neoplasms / Q000473:pathology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007510:Isatin
keywords: Anticancer activity; Apoptosis resistance; Cytotoxic compounds; Indirubin; Isatin