10 research outputs found
Cancer fighting cancer: synthesis of the new heterocyclic system diimidazo[1,2-a:1,2-c]pyrimidine
No full textn/
Synthesis and chemiluminescent high throughput screening for inhibition of acetylcholinesterase activity by imidazo[2,1-b]thiazole derivatives
No full text2-[(E)-3-(6-chloroimidazo[2,1-b]thiazol-5-ylprop-2-enyl]5,6-dimethoxy-3-methyl-1,4-benzo quinone: a new inhibitor of NADH dehydrogenase with antitumor activity
No full textSynthesis and Screening for Antiacetylcholinesterase Activity of (1-Benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles Related to Donepezil
No full textImidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors
No full textThe activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6
kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active
compounds indicates a high degree of selectivity for inhibition of RSK2 compared to a spectrum of other
related kinases. Selective inhibition of the MCF-7 breast tumor cell line compared to MCF-10A nontransformed
cells, as well as selective inhibition of the biomarker GSK3 provides evidence that the
compounds can affect the RSK2 target in cells
Antitumor Activity of Bis-indole Derivatives
No full textnone16noneA. Andreani; S. Burnelli; M. Granaiola; A. Leoni; A. Locatelli; R. Morigi; M. Rambaldi; L. Varoli; L. Landi; C. Prata; M. V. Berridge; C. Grasso; H-H. Fiebig; G. Kelter; A. M. Burger; M. W. KunkelA. Andreani; S. Burnelli; M. Granaiola; A. Leoni; A. Locatelli; R. Morigi; M. Rambaldi; L. Varoli; L. Landi; C. Prata; M. V. Berridge; C. Grasso; H-H. Fiebig; G. Kelter; A. M. Burger; M. W. Kunke
Substituted 3-(5-Imidazo[2,1-<i>b</i>]thiazolylmethylene)-2-indolinones and Analogues: Synthesis, Cytotoxic Activity, and Study of the Mechanism of Action
No full textThe synthesis of substituted 3-(5-imidazo[2,1-<i>b</i>]thiazolylmethylene)-2-indolinones and analogues is reported.
Their
cytotoxic activity was evaluated according to protocols available
at the National Cancer Institute (NCI), Bethesda, MD. The action of
selected compounds was examined for potential inhibition of tubulin
assembly in comparison with the potent colchicine site agent combretastatin
A-4. The most potent compounds also strongly and selectively inhibited
the phosphorylation of the oncoprotein kinase Akt in cancer cells.
The effect of the most interesting compounds was examined on the growth
of HT-29 colon cancer cells. These compounds caused the cells to arrest
in the G2/M phase of the cell cycle, as would be expected for inhibitors
of tubulin assembly
