Substituted E-3-(3-indolylmethylene)-1,3-dihydroindol-2-ones with antitumor activity. In depth study of the effect on growth of breast cancer cells.

@article{Andreani2010SubstitutedEW,
  title={Substituted E-3-(3-indolylmethylene)-1,3-dihydroindol-2-ones with antitumor activity. In depth study of the effect on growth of breast cancer cells.},
  author={Aldo Andreani and Stefania Bellini and Silvia Burnelli and Massimiliano Granaiola and Alberto Leoni and Alessandra Locatelli and Rita Morigi and Mirella Rambaldi and Lucilla Varoli and Natalia Calonghi and Concettina Cappadone and Maddalena Zini and Claudio Stefanelli and Lanfranco Masotti and Robert H. Shoemaker},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 15},
  pages={
          5567-75
        }
}
The synthesis of new substituted E-3-(3-indolylmethylene)-1,3-dihydroindol-2-ones is reported. The antitumor activity was evaluated according to protocols available at the National Cancer Institute (NCI), Bethesda, MD. Structure-activity relationships are discussed. The action of selected compounds was investigated in MCF-7 breast cancer cells. The ability of these derivatives to inhibit cellular proliferation was accompanied by increased level of p53 and its transcriptional targets p21 and Bax… 

Figures and Tables from this paper

Synthesis and anticancer activity of oxindole derived imidazo[1,5-a]pyrazines.

Synthesis and Biological Evaluation of New Bis-Indolinone Derivatives Endowed with Cytotoxic Activity

A series of new Knoevenagel adducts, bearing two indolinone systems, has been synthesized and evaluated on human cancer cell lines according to protocols available at the National Cancer Institute, and compound 5b emerged as the most active.

Synthesis and Anticancer Activity of Indolin‐2‐one Derivatives Bearing the 4‐Thiazolidinone Moiety

A novel series of indolin‐2‐one derivatives containing the 4‐thiazolidinone moiety (5a—5p) was synthesized and the cytotoxicity of these derivatives was evaluated in vitro against three human cancer

Facile Synthesis of Isoindigo Derivatives from 3-Indolyl-2-Oxindoles with DDQ

Isoindigo (3,30-biindolylidene-2,20-dione) and its derivatives have received much attention due to their biological activity such as anti-leukemia, antiproliferative, and antiinflammatory activity

Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors.

Synthesis of a new class of antimicrobial agents incorporating the indolin-2-one moiety

New furanone derivatives incorporating the indolin-2-one moiety 3 were prepared via the Perkin reaction of isatins 1 with aroylpropionic acids 2 under conventional conditions or microwave irradiation and screened for antibacterial activity against Gram-positive bacteria, Gram-negative bacteria and antifungal activity against Aspergillus flavus and Candida albicans.

Chemistry of 3-acyl-2-haloindoles (Review)

Methods for the synthesis and transformation of 3-acyl-2-haloindoles, which are polyfunctional reagents used for preparing various indole derivatives, are summarized. The reduction and oxidation of

References

SHOWING 1-10 OF 36 REFERENCES

Synthesis and Antitumor Activity of 1,5,6-Substituted E-3-(2-Chloro-3-indolylmethylene)-1,3-dihydroindol-2-ones1

Synthesis and antitumor activity of new E-3-(2-chloro-3-indolylmethylene)-1,3-dihydroindol-2-ones are described. All compounds prepared were active in the primary test (three human cell lines) and

Potential antitumor agents. 25 [1]. Synthesis and cytotoxic activity of 3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones.

The Knoevenagel reaction between 2-indolinones and 2-chloroindolaldehydes gave 3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones which were tested as potential antitumor agents on cultures of

Synthesis and antitumor activity of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones.

From the analysis of the antitumor data, 3-1(2,6-dimethylimidazo[2,1-bJ-thiazol-5-yl)methylenel- 5-methoxy-2-indolinone was the most active of the whole series.

Study on compounds with potential antitumor activity. III. Hydrazone derivatives of 5-substituted 2-chloro-3-formyl-6-methylindole.

The synthesis of 5-methoxy- (IX) and 5-hydroxy- (X) 2-chloro-3-formyl-6-methylindole is reported: three hydrazonic derivatives were prepared from each compound. Preliminary results on the activity of

Chemical and biological properties of some oxindolidyl-3-methines

Several 1-methyloxindohdyl-3-methines have been synthesized, either by condensation of 1-methyloxindole with an aldehyde, or by a Wittig reaction of a chloromethylene compound with a 1-methylisatin

Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases.

Structural-activity analysis supports the use of subsets of 3-substituted indolin-2-ones as specific chemical leads for the development of RTK-specific drugs with broad application for the treatment of human diseases.

Antitumor activity and COMPARE analysis of bis-indole derivatives.