Синтез и цитостатическая активность ( E )-этил-2-амино-5-(3,3-диметил-4-оксобутилиден)-4-оксо-1-(2-фениламинобензамидо)-4,5-дигидро-1 H -пиррол-3-карбоксилата

Reaction of ( Z )-N-(5- tert -butyl)-2-oxofuran-3(2H)-ylidene-2-phenylaminobenzohydrazide (I) with cyanoacetic ester in the presence of triethylamine yielded ( E )-ethyl-2-amino-5-(3,3-dimethyl-4-oxo-butyliden)-4-oxo-1-(2-phenylaminobenzamido)-4,5-dihydro-1 H -pyrrole-3-carboxylate (II). Acute toxicity of compound II was studied and its cytotoxic activity with respect to T-1 cell line of gastrointestunal stromal tumor (GIST) was evaluated. Compound II showed time- and concentration-dependent effect comparable with that of well-known antitumor drugs imatinib, paclitaxel, doxorubicin, etoposide, and hydroxyurea.