NDLI: Synthesis of 2-(2,4-dihydroxyphenyl)thieno-1,3-thiazin-4-ones, their lipophilicity and anticancer activity in vitro

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Synthesis of 2-(2,4-dihydroxyphenyl)thieno-1,3-thiazin-4-ones, their lipophilicity and anticancer activity in vitro

Content Provider	Springer Nature Link
Author	Matysiak, Joanna Juszczak, Małgorzata Karpińska, Monika M. Langner, Ewa Walczak, Katarzyna Lemieszek, Marta K. Skrzypek, Alicja Niewiadomy, Andrzej Rzeski, Wojciech
Copyright Year	2015
Abstract	A new one-step synthesis of novel biologically active 2-substituted 2,4-dihydroxyphenyl-4 $$H$$ -thieno[3,2- $$d$$ ][1,3]thiazin-4-ones and 4 $$H$$ -thieno[2,3- $$d$$ ][1,3]thiazin-4-ones has been elaborated and described. The compounds were prepared by the reaction of aryl-modified sulfinylbis [(2,4-dihydroxyphenyl)methanethione]s and the corresponding aminothiophenecarboxamides. The derivatives showed anticancer activity in vitro. These compounds inhibited the proliferation and viability of lung cancer A549, colon cancer HT-29 and glioma C6 cells in a concentration-dependent manner. Some of the derivatives had no influence on normal skin fibroblasts culture viability. Moreover, one compound (1b) showed the ability to inhibit DNA synthesis in cancer cells, especially in C6 cells, and was not toxic for normal oligodendrocytes and hepatocytes. Using reversed phase RP 18 HPLC and immobilised artificial membrane (IAM) chromatography the phase affinity of the compounds was determined. The influence of lipophilicity on the activity of compounds has been discussed.
Starting Page	725
Ending Page	736
Page Count	12
File Format	PDF
ISSN	13811991
Journal	Molecular Diversity
Volume Number	19
Issue Number	4
e-ISSN	1573501X
Language	English
Publisher	Springer International Publishing
Publisher Date	2015-04-29
Publisher Place	Cham
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Anticancer agents Antiproliferative activity Cytotoxicity Lipophilicity Thieno-1,3-thiazin-4-ones Resorcinols Biochemistry Organic Chemistry Polymer Sciences Pharmacy
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Medicine Drug Discovery Molecular Biology Physical and Theoretical Chemistry Information Systems Catalysis Inorganic Chemistry

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