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Heterocycles 27. Microwave Assisted Synthesis and Antitumour Activity of Novel Phenothiazinyl‐Thiazolyl‐Hydrazine Derivatives
Author(s) -
Ignat Adriana,
Lovasz Tamas,
Vasilescu Mihai,
FischerFodor Eva,
Tatomir Corina Bianca,
Cristea Castelia,
SilaghiDumitrescu Luminiţa,
Zaharia Valentin
Publication year - 2012
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201100355
Subject(s) - hydrazine (antidepressant) , chemistry , microwave irradiation , in vitro , cytotoxicity , combinatorial chemistry , microwave , stereochemistry , organic chemistry , catalysis , biochemistry , physics , quantum mechanics
A series of new phenothiazinyl‐thiazolyl‐hydrazine derivatives were synthesized by Hantzsch cyclization of 1‐(10‐ethyl‐10 H ‐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.