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Title of Journal: Pharm Chem J

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Abbravation: Pharmaceutical Chemistry Journal

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Springer US

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DOI

10.1016/j.baae.2010.11.006

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ISSN

1573-9031

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Synthesis and Cytotoxic Activity of Ethyl 2Amino

Authors: S S Zykova A R Galembikova B R Ramazanov T F Odegova N M Igidov M A Kiselev S V Boichuk
Publish Date: 2016/04/02
Volume: 49, Issue: 12, Pages: 817-820
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Abstract

Recyclization of 5aryl23dihydro2furandione 3benzoylhydrazones I induced by cyanoacetic ester produced ethyl 2amino1benzamido4oxo52oxo2arylethylidene45dihydro1Hpyrrole3carboxylates IIag The biological activity of the synthesized compounds which possessed low toxicities was investigated Ethyl 2amino1benzamido524chlorophenyl2oxoethylidene4oxo45dihydro1Hpyrrole3carboxylate IIf and the 5234dimethoxyphenyl2oxoethylidene analog IIc exhibited the greatest cytotoxicities against several connectivetissue tumor cell lines namely gastrointestinal stromal tumors GISTs osteosarcoma U2OS and leiomyosarcoma SKLMS1 Ethyl 2amino1benzamido4oxo52oxo2ptolylethylidene45dihydro1Hpyrrole3carboxylate IIa suppressed significantly tumor growth of GIST LMS and OS cell lines Its activity against GIST cells at 10 μM was comparable with that of imatinib 1 μM and at lower concentrations 25 and 5 μM with those of doxorubicin 025 μg/mL and etoposide 40 μM and exceeded significantly those of taxol 1 μM and hydroxyurea 1 mM The cytotoxicities of most of the studied compounds at 10 μM against SKLMS1 and U2OS cells in vitro were significantly greater than all reference drugs doxorubicin taxol etoposide etc

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