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Updated: May 9, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis and Biological Activity of New Thiopyrano[2,3-d]thiazoles Containing a Naphthoquinone Moiety
Dmytro Atamanyuk1, Borys Zimenkovsky, Vasyl Atamanyuk
1Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010 Lviv, Ukraine. ; Present address: Mutabilis, 102 Avenue Gaston Roussel, 93230 Romainville, France.
Abstract:
Novel 11-substituted 3,11-dihydro-2H-benzo[6,7]thiochromeno[2,3-d][1,3]-thiazole-2,5,10-triones 4a-i were synthesized in 75-90% yields via the hetero-Diels-Alder reaction of 5-arylidene-4-thioxo-2-thiazolidinones with 1,4-naphthoquinone. The synthesized compounds were evaluated for their antineoplastic and antimycobacterial activities. A moderate selectivity against melanoma cancer cells (GI50 (UACC-257-melanoma) = 0.22 μM) was demonstrated for 4i, whereas derivatives 4a, 4c, 4g, and 4h showed promising antimycobacterial activity at a low toxicity level.
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