Kaminskyy Danylo, Khyluk Dmytro, Vasylenko Olexandr, Zaprutko Lucjusz, Lesyk Roman
Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010, Lviv, Ukraine.
Sci Pharm. 2011 Oct-Dec;79(4):763-77. doi: 10.3797/scipharm.1109-14. Epub 2011 Oct 3.
The synthesis and evaluation of the anticancer activity of 3'-aryl-5'-arylidene-spiro[3H-indole-3,2'-thiazolidine]-2,4'(1H)-diones and spiro[3H-indole-3,2'-thi-azolidine]-2,4'(1H)-dione-3'-alkanoic acid esters were described. The structure of the compounds was determined by (1)H and (13)C NMR and their in vitro anticancer activity was tested in the National Cancer Institute. Among the tested compounds, (5'Z)-5'-(benzylidene)-3'-(4-chlorophenyl)spiro[3H-indole-3,2'-thia-zolidine]-2,4'(1H)-dione (IIa) and (5'Z)-3'-(4-chlorophenyl)-5'-[4-(1-methylethyl)-benzylidene]spiro[3H-indole-3,2'-thiazolidine]-2,4'(1H)-dione (IIb) were superior to other related compounds.
描述了3'-芳基-5'-亚芳基-螺[3H-吲哚-3,2'-噻唑烷]-2,4'(1H)-二酮和螺[3H-吲哚-3,2'-噻唑烷]-2,4'(1H)-二酮-3'-链烷酸酯的合成及其抗癌活性评价。通过(1)H和(13)C NMR确定了化合物的结构，并在美国国立癌症研究所测试了它们的体外抗癌活性。在所测试的化合物中，(5'Z)-5'-(亚苄基)-3'-(4-氯苯基)螺[3H-吲哚-3,2'-噻唑烷]-2,4'(1H)-二酮(IIa)和(5'Z)-3'-(4-氯苯基)-5'-[4-(1-甲基乙基)-亚苄基]螺[3H-吲哚-3,2'-噻唑烷]-2,4'(1H)-二酮(IIb)优于其他相关化合物。
