Synthesis and biological evaluation of 3-substituted-indolin-2-one derivatives containing chloropyrrole moieties |
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Authors: | Jin Yun-Zhou Fu Da-Xu Ma Nan Li Zhan-Cheng Liu Quan-Hai Xiao Lin Zhang Rong-Hua |
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Affiliation: | Department of Chemistry, Tongji University, Shanghai, 200092, China. |
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Abstract: | Eighteen novel 3-substituted-indolin-2-ones containing chloropyrroles were synthesized and their biological activities were evaluated. The presence of a chlorine atom on the pyrrole ring was crucial to reduce cardiotoxicity. The presence of a 2-(ethyl-amino)ethylcarbamoyl group as a substituent at the C-4' position of the pyrrole enhanced the antitumor activities notably. IC50 values as low as 0.32, 0.67, 1.19 and 1.22 μM were achieved against non-small cell lung cancer (A549), oral epithelial (KB), melanoma (K111) and large cell lung cancer cell lines (NCI-H460), respectively. |
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