These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Design, synthesis and in vitro cytotoxicity evaluation of 5-(2-carboxyethenyl)isatin derivatives as anticancer agents.
    Author: Han K, Zhou Y, Liu F, Guo Q, Wang P, Yang Y, Song B, Liu W, Yao Q, Teng Y, Yu P.
    Journal: Bioorg Med Chem Lett; 2014 Jan 15; 24(2):591-4. PubMed ID: 24360564.
    Abstract:
    Forty four di- or trisubstituted novel isatin derivatives were designed and synthesized in 5-6 steps in 25-45% overall yields. Their structures were confirmed by (1)H NMR and (13)C NMR as well as LC-MS. The anticancer activity of these new isatin derivatives against three human tumor cell lines, K562, HepG2 and HT-29, were evaluated by MTT assay in vitro. SAR studies suggested that the combination of 1-benzyl and 5-[trans-2-(methoxycarbonyl)ethen-1-yl] substitution greatly enhance their cytotoxic activity, whereas an intact carbonyl functionality on C-3 as present in the parent ring is required to such a potency. This study leads to the identification of two highly active molecules, compounds 2h (IC50=3 nM) and 2k (IC50=6 nM), against human leukemia K562 cells.
    [Abstract] [Full Text] [Related] [New Search]