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Volume 80
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Article

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

by
Anna KRYSHCHYSHYN
1,
Dmytro ATAMANYUK
1,2 and
Roman LESYK
1,*
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
Submission received: 2 April 2012 / Accepted: 3 May 2012 / Published: 3 May 2012
Versions Notes

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

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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. https://doi.org/10.3797/scipharm.1204-02

AMA Style

KRYSHCHYSHYN A, ATAMANYUK D, LESYK R. Fused Thiopyrano[2,3-d]thiazole Derivatives as Potential Anticancer Agents. Scientia Pharmaceutica. 2012; 80(3):509-530. https://doi.org/10.3797/scipharm.1204-02

Chicago/Turabian Style

KRYSHCHYSHYN, Anna, Dmytro ATAMANYUK, and Roman LESYK. 2012. "Fused Thiopyrano[2,3-d]thiazole Derivatives as Potential Anticancer Agents" Scientia Pharmaceutica 80, no. 3: 509-530. https://doi.org/10.3797/scipharm.1204-02

APA Style

KRYSHCHYSHYN, A., ATAMANYUK, D., & LESYK, R. (2012). Fused Thiopyrano[2,3-d]thiazole Derivatives as Potential Anticancer Agents. Scientia Pharmaceutica, 80(3), 509-530. https://doi.org/10.3797/scipharm.1204-02

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