title: Heterocycles 27. Microwave assisted synthesis and antitumour activity of novel phenothiazinyl-thiazolyl-hydrazine derivatives.
abstract: A series of new phenothiazinyl-thiazolyl-hydrazine derivatives were synthesized by Hantzsch cyclization of 1-(10-ethyl-10H-phenothiazin-3-yl)-methylidene-thiosemicarbazide with α-halocarbonyl derivatives. Comparison between classical and microwave assisted synthesis emphasizes the great advantages induced by microwaves irradiation which afforded high reaction yields in much shorter reaction time. Structural assignments were based on spectroscopic methods (high resolution NMR, FTIR, MS). The new compounds were tested in vitro for their antiproliferative activity against tumor cell lines using spectrometric methods. Most of the compounds exhibit cytotoxicity against hepatic and colon tumor cells in a dose-dependent mode and a relationship between the structure and their biological activity was observed.
authors.affiliation: Faculty of Pharmacy, Iuliu Haţieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania.
authors.forename: Adriana
authors.initials: A
authors.lastname: Ignat
authors.forename: Tamas
authors.initials: T
authors.lastname: Lovasz
authors.forename: Mihai
authors.initials: M
authors.lastname: Vasilescu
authors.forename: Eva
authors.initials: E
authors.lastname: Fischer-Fodor
authors.forename: Corina Bianca
authors.initials: CB
authors.lastname: Tatomir
authors.forename: Castelia
authors.initials: C
authors.lastname: Cristea
authors.forename: Luminiţa
authors.initials: L
authors.lastname: Silaghi-Dumitrescu
authors.forename: Valentin
authors.initials: V
authors.lastname: Zaharia
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D018929:Cell Culture Techniques; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003500:Cyclization; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D008872:Microwaves; D015394:Molecular Structure; D010640:Phenothiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; D006834:Hydrazines; D010640:Phenothiazines; D013844:Thiazoles