Department of Chemistry, Tongji University, Shanghai, 200092, China.
Molecules. 2011 Nov 8;16(11):9368-85. doi: 10.3390/molecules16119368.
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.
合成了 18 种新型 3-取代-吲哚啉-2-酮，其中含有氯代吡咯，评估了它们的生物活性。吡咯环上的氯原子的存在对于降低心脏毒性至关重要。在吡咯的 C-4'位置上带有 2-(乙基-氨基)乙基氨甲酰基作为取代基，显著增强了抗肿瘤活性。对非小细胞肺癌（A549）、口腔上皮（KB）、黑色素瘤（K111）和大细胞肺癌细胞系（NCI-H460）的 IC50 值分别低至 0.32、0.67、1.19 和 1.22 μM。
