title: Synthesis and biological evaluation of 3-substituted-indolin-2-one derivatives containing chloropyrrole moieties.
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.
authors: Department of Chemistry, Tongji University, Shanghai, 200092, China.
authors: Yun-Zhou
authors: YZ
authors: Jin
authors: Da-Xu
authors: DX
authors: Fu
authors: Nan
authors: N
authors: Ma
authors: Zhan-Cheng
authors: ZC
authors: Li
authors: Quan-Hai
authors: QH
authors: Liu
authors: Lin
authors: L
authors: Xiao
authors: Rong-Hua
authors: RH
authors: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor / Q000187:drug effects; D002713:Chlorine / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry*; D036341:Intercellular Signaling Peptides and Proteins / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D036341:Intercellular Signaling Peptides and Proteins; D011758:Pyrroles; C456900:indolin-2-one; D002713:Chlorine; D040301:Vascular Endothelial Growth Factor Receptor-2