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Synthesis and Anticancer Activity of New 2‐Aryl‐4 H ‐3,1‐benzothiazines
Author(s) -
Niewiadomy Andrzej,
Matysiak Joanna,
Karpińska Monika M.
Publication year - 2011
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.201000228
Subject(s) - chemistry , benzothiazine , aryl , stereochemistry , cytotoxicity , cisplatin , cancer cell lines , in vitro , proton nmr , combinatorial chemistry , medicinal chemistry , cancer cell , organic chemistry , biochemistry , cancer , medicine , alkyl , surgery , chemotherapy
New compounds of 2‐aryl‐4 H ‐3,1‐benzothiazine set were synthesized and tested for their antiproliferative activity as part of our research in the antitumor field. The title compounds were obtained by the reaction of aryl‐modified sulfinylbis((2,4‐dihydroxyphenyl)methanethione) with 2‐aminobenzyl alcohols. The reaction proceeded through thiobenzanilide intermediates, which were converted to the 4 H ‐3,1‐benzothiazine fused ring by an endocyclization process. The structures of compounds were identified from elemental, IR, 1 H‐NMR, 13 C‐NMR, and MS spectra analyses. The cytotoxicity in vitro against four human cancer cell lines was determined. The antiproliferative properties of some compounds were more beneficial than cisplatin studied comparatively.