SYNTHESIS AND ANTITUMOR ACTIVITY OF
NOVEL 2-THIOXO-4-THIAZOLIDINONES WITH
BENZOTHIAZOLE MOIETIES.
LUDMYLA MOSULA¹, BORYS ZIMENKOVSKY¹, DMYTRO
HAVRYLYUK¹, ALEXANDRU-VASILE MISSIR², ILEANA
CORNELIA CHIRIŢĂ², ROMAN LESYK¹*
1 Department of Pharmaceutical, Organic and Bioorganic Chemistry,
Danylo Halytsky Lviv National Medical University, 79010 Lviv, Ukraine,
2 Department of Pharmaceutical Chemistry,"Carol Davila" University of
Medicine and Pharmacy, 020955 Bucharest, Romania
*corresponding author: dr_r_lesyk@org.lviv.net
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Abstract:

Following the reaction of benzothiazol-2-yl-hydrazine or (2-oxo-benzothiazol-3- yl)-acetic acid hydrazide with thiocarbonyl-bis-thioglycolic acid, 3-(benzothiazol-2- ylamino)-2-thioxothiazolidin-4-one (1) and 2-(2-oxobenzothiazol-3-yl)-N-(4-oxo-2-thioxothiazolidin-3-yl)-acetamide(2) were synthesized, as starting compounds for obtaining new5-arylidenederivatives (3-6) in Knoevenagel condensation with aromatic aldehydes and isatines. The synthesized compounds showed antitumor activity on renal cancer, non-small cell lung cancer and ovarian cancer cell lines. The most efficient anticancer agent, 2-{2-[3-(benzothiazol-2-ylamino)-4-oxo-2-thioxo-thiazolidin-5- ylidenemethyl]-4-chloro-phenoxy}-N-(4-methoxyphenyl)-acetamide 3d was found to be active with average values of -5.38 and -4.45 for logGI₅₀ and logTGI, respectively.

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