Synthesis and antitumor activity of 2-cyanocinnamic acid amides and their indole analogues

By the reaction of substituted benzaldehydes and indol-3-carbaldehydes (2E)-2-cyano-N-[5-(R-benzyl)-1,3-thiazol-2-yl]-3-(R1-phenyl)prop-2-enamides 3-(1-R1-1H-indol-3-yl)-2-cyano-N-(5-(R-benzyl)-1,3-thiazol-2-yl)prop-2-enamides were synthesised. The antitumor activity of prepared compounds were investigated. 3-(1-Benzyl-1H-indol-3-yl)-2-cyano-N-(5-(2-chlorobenzyl)-1,3-thiazol-2-yl)prop-2-enamide (7b) has been identified as hit compound with values of MG-MID GI50 = 3.903 µM, TGI = 29.10 µM, LC50 = 57.54 µM.

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Publication Details

Journal
Current Chemistry Letters
Published
2024-11-13
DOI
https://doi.org/10.5267/j.ccl.2024.9.001
Citations
1
Primary Topic
Synthesis and Reactions of Organic Compounds
Type
article
Field-Weighted Citation Impact
0.25

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article

Synthesis and antitumor activity of 2-cyanocinnamic acid amides and their indole analogues

Nataliya Shtoyko, Іryna Drapak, V. S. Matiychuk, Liubov Kostyshyn et al.
1 citations
Current Chemistry Letters
Synthesis and Reactions of Organic Compounds
0.25
article

Synthesis and antitumor activity of 2-cyanocinnamic acid amides and their indole analogues

Nataliya Shtoyko, Іryna Drapak, V. S. Matiychuk, Liubov Kostyshyn, Yuliia Matiichuk, S. S. Kramarenko, Yana Drapak
article en
1 citations

Abstract

By the reaction of substituted benzaldehydes and indol-3-carbaldehydes (2E)-2-cyano-N-[5-(R-benzyl)-1,3-thiazol-2-yl]-3-(R1-phenyl)prop-2-enamides 3-(1-R1-1H-indol-3-yl)-2-cyano-N-(5-(R-benzyl)-1,3-thiazol-2-yl)prop-2-enamides were synthesised. The antitumor activity of prepared compounds were investigated. 3-(1-Benzyl-1H-indol-3-yl)-2-cyano-N-(5-(2-chlorobenzyl)-1,3-thiazol-2-yl)prop-2-enamide (7b) has been identified as hit compound with values of MG-MID GI50 = 3.903 µM, TGI = 29.10 µM, LC50 = 57.54 µM.

Current Chemistry LettersVol. 14(1)
Ministry of Education and Science of Ukraine
Clean water and sanitation
Openalex Percentile: Top 46%
Synthesis and Reactions of Organic Compounds
0.25
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