Cytotoxic activities of substituted 3-(3,4,5-trimethoxybenzylidene)-1,3-dihydroindol-2-ones and studies on their mechanisms of action.

Authors :: Andreani A
Granaiola M
Locatelli A
Morigi R
Rambaldi M
Varoli L
Vieceli Dalla Sega F
Prata C
Nguyen TL
Bai R
Hamel E
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2013 Jun; Vol. 64, pp. 603-12. Date of Electronic Publication: 2013 Apr 03.
Publication Year :: 2013
Abstract: The synthesis of new trimethoxybenzylidene-indolinones is reported. Their cytotoxic activity was evaluated according to Developmental Therapeutics Program, National Cancer Institute, Bethesda, MD, drug screen protocols. The study of the mechanism of action suggests that inhibition of Nox4 in B1647 cells (acute myeloid leukemia) could contribute to the antiproliferative effect of some compounds. Moreover, inhibition of tubulin assembly was observed for the most cytotoxic compound, and the structural basis for this activity was delineated by binding models.<br /> (Copyright © 2013 Elsevier Masson SAS. All rights reserved.)

Subjects :: Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Benzylidene Compounds chemical synthesis
Benzylidene Compounds chemistry
Cell Proliferation drug effects
Cell Survival drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Indoles chemical synthesis
Indoles chemistry
Models, Molecular
Molecular Structure
Structure-Activity Relationship
Tumor Cells, Cultured
Antineoplastic Agents pharmacology
Benzylidene Compounds pharmacology
Indoles pharmacology

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