Isatin derivatives with activity against apoptosis-resistant cancer cells

• Published in: Bioorganic & medicinal chemistry letters Vol. 26; no. 6; pp. 1558 - 1560
• Main Authors: Evdokimov, Nikolai M., Magedov, Igor V., McBrayer, Dominic, Kornienko, Alexander
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 15.03.2016; Elsevier
• Subjects: Anticancer activity; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Apoptosis - drug effects; Apoptosis resistance; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry; Chemistry, Medicinal; Chemistry, Organic; Cytotoxic compounds; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Indirubin; Isatin; Isatin - analogs & derivatives; Isatin - chemical synthesis; Isatin - chemistry; Isatin - pharmacology; Life Sciences & Biomedicine; Molecular Structure; Neoplasms - pathology; Pharmacology & Pharmacy; Physical Sciences; Science & Technology; Structure-Activity Relationship; Indirubin; Apoptosis resistance; Cytotoxic compounds; Isatin; Anticancer activity; SURVIVAL; GLIOBLASTOMA; POTENT; MODELS; GLYCOGEN-SYNTHASE KINASE-3; INHIBITORS; CHEMOTHERAPY
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2016.02.015

[Display omitted] 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.