Synthesis and cytotoxic studies of novel 5-phenylisatin derivatives and their anti-migration and anti-angiogenic evaluation.

ABSTRACT: A number of 5-arylisatin derivatives were synthesized in 5-6 steps from readily available starting materials. Their structures were confirmed by ¹H NMR and ¹³C NMR as well as LC/MS. The cytotoxicity of these novel isatins against human leukemia K562 cells were evaluated by MTT assay in vitro. SAR studies indicated that the N-substituted benzyl and C-5 substituted phenyl groups greatly enhance their cytotoxic activity, whereas an intact carbonyl functionality on C-3 present in the parent ring is required to maintain such a potency. Particularly, N-(p-methoxybenzyl)-5-(p-methoxyphenyl)isatin (compound 2m) showed the highest antitumor activity against K562 cell lines (IC₅₀ = 0.03 μM). Moreover, treatment with compound 2m significantly inhibited liver cancer He

SUBMITTER: Zhang Q 

PROVIDER: S-EPMC7115506 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature