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Sci. Pharm.Scientia Pharmaceutica
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  • Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
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3 May 2012

21 Pages

Fused Thiopyrano[2,3-d]thiazole Derivatives as Potential Anticancer Agents

,
and
1
Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010, Lviv, Ukraine
2
Mutabilis, 102 Avenue Gaston Roussel, 93230 Romainville, France
*
Author to whom correspondence should be addressed.
Sci. Pharm.2012, 80(3), 509-530;https://doi.org/10.3797/scipharm.1204-02
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Abstract

rel-(5aR,11bR)-3,5a,6,11b-tetrahydro-2Н,5Н-chromeno[4',3':4,5]thiopyrano[2,3-d][1,3]thiazol-2-ones formed by the stereoselective Knoevenagel-hetero-Diels-Alder reaction were functionalized at the nitrogen in position 3 via reactions of alkylation, cyanoethylation, and acylation. The synthesized compounds were evaluated for their anticancer activity in NCI60 cell lines. Among the tested compounds, 3f was found to be the most active candidate with the greatest influence on leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, prostate cancer, and breast cancer subpanel cell lines with GI50 values over a range of 0.37–0.67 μM.

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