Substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones with antiproliferative activity. Study of the effects on HL-60 leukemia cells.

  title={Substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones with antiproliferative activity. Study of the effects on HL-60 leukemia cells.},
  author={Alberto Leoni and Alessandra Locatelli and Rita Morigi and Mirella Rambaldi and Concettina Cappadone and Giovanna Farruggia and Stefano Iotti and Lucia Merolle and Maddalena Zini and Claudio Stefanelli},
  journal={European journal of medicinal chemistry},

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 antiproliferative and apoptosis-inducing activity of novel 3-substituted-3-hydroxy-2-oxindole compounds

The results obtained showed that this compound increased the percentage of tail DNA, increased the occurrence of the sub-G1 phase, and induced G2M arrest and apoptosis in DU145 cells after exposure for 48 h to a 55-μM concentration.


The overall tumor analysis showed that 6 treatment significantly inhibited the breast tumor incidence, tumor multiplicity, and tumor size in the DMBA-initiated rat model, showing that the 6 treatment was significantly effective in reduction of tumors versus the cancer controls.

Chapter One – Oxindoles



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.

The ability of these derivatives to inhibit cellular proliferation was accompanied by increased level of p53 and its transcriptional targets p21 and Bax, interference in the cell cycle progression with cell accumulation in the G2/M phase, and activation of apoptosis.

Substituted E-3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones with antitumor activity. Effect on the cell cycle and apoptosis.

The synthesis and antitumor activity of new E-3-(2-chloro-3-indolylmethylene)1,3-dihydroindol-2-ones is described and the effects on the cell cycle and apoptosis are dedicated.

Substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues: synthesis, cytotoxic activity, and study of the mechanism of action.

The most potent compounds strongly and selectively inhibited the phosphorylation of the oncoprotein kinase Akt in cancer cells and caused the cells to arrest in the G2/M phase of the cell cycle, as would be expected for inhibitors of tubulin assembly.

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.

New antitumor imidazo[2,1-b]thiazole guanylhydrazones and analogues.

The synthesis of new antitumor 6-substituted imidazothiazole guanylhydrazones is described. Moreover, a series of compounds with a different basic chain at the 5 position were prepared. Finally, the