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Sci. Pharm. 2012, 80(3), 509-530; doi:10.3797/scipharm.1204-02

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

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.
Received: 2 April 2012 / Accepted: 3 May 2012 / Published: 3 May 2012
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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.
Keywords: Thiopyrano[2,3-d][1,3]thiazoles; Alkylation; Cyanoethylation; Anticancer activity; COMPARE analysis Thiopyrano[2,3-d][1,3]thiazoles; Alkylation; Cyanoethylation; Anticancer activity; COMPARE analysis
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

KRYSHCHYSHYN, A.; ATAMANYUK, D.; LESYK, R. Fused Thiopyrano[2,3-d]thiazole Derivatives as Potential Anticancer Agents. Sci. Pharm. 2012, 80, 509-530.

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