title: Indole-based hydrazide-hydrazones and 4-thiazolidinones: synthesis and evaluation as antitubercular and anticancer agents.
abstract: A new series of indolylhydrazones (6) and indole-based 4-thiazolidinones (7, 8) have been designed, synthesized and screened for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. 4-Thiazolidinone derivatives 7g-7j, 8g, 8h and 8j displayed notable antituberculosis (anti-TB) activity showing 99% inhibition at MIC values ranging from 6.25 to 25.0 µg/ml. Compounds 7g, 7h, 7i, 8h and 8j demonstrated anti-TB activity at concentrations 10-fold lower than those cytotoxic for the mammalian cell lines. The indolylhydrazone derivative 6b has also been evaluated for antiproliferative activity against human cancer cell lines at the National Cancer Institute (USA). Compound 6b showed an interesting anticancer profile against different human tumor-derived cell lines at sub-micromolar concentrations with obvious selectivity toward colon cancer cell line COLO 205.
authors.affiliation: a Department of Pharmaceutical Chemistry , Faculty of Pharmacy .
authors.forename: Gökçe
authors.initials: G
authors.lastname: Cihan-Üstündağ
authors.affiliation: b Department of Microbiology and Clinical Microbiology , Istanbul Faculty of Medicine , and.
authors.forename: Dilek
authors.initials: D
authors.lastname: Şatana
authors.affiliation: c Department of Pharmaceutical Toxicology , Faculty of Pharmacy, Istanbul University , Istanbul , Turkey.
authors.forename: Gül
authors.initials: G
authors.lastname: Özhan
authors.affiliation: a Department of Pharmaceutical Chemistry , Faculty of Pharmacy .
authors.forename: Gültaze
authors.initials: G
authors.lastname: Çapan
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006834:Hydrazines / Q000737:chemistry / Q000494:pharmacology*; D006835:Hydrazones / Q000737:chemistry / Q000494:pharmacology*; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D000995:Antitubercular Agents; D006834:Hydrazines; D006835:Hydrazones; D007211:Indoles; D053778:Thiazolidines
keywords: 4-thiazolidinone; Anticancer activity; antitubercular activity; hydrazide-hydrazone; indole