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The most promising anticancer derivatives (5l, 5k, 5i and 5p) were further docked to study their binding efficacy to the active site of the cyclin-dependent kinase-8.
The information obtained in this study will be helpful for the design of new derivatives of 1 with most promising anticancer activity.
Compound 3a was the most promising anticancer agent in the series, based upon its potent growth inhibition via RhoB-mediated signaling.
Results from the bioassay based on a double fluorochrome staining were worthy to be described because they provide a clue to the mode of action of one (18) of the most promising anticancer lead structures of the series.
Amongst the tested compounds, the compound 5e was the most promising anticancer agent with IC50 value of 15.54 μM in MCF-7 cells, compared to Doxorubicin as standard drug.
Among these strongly antiproliferative active molecules, the disclosed three thiophene bioisosteres (11, 17 and 18) are proposed as the most promising anticancer lead structures for the rational design of more selective antitumour agents because they proved to be markedly lower cytotoxic towards normal than tumour cells.
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Accordingly, synthetic analogue 16Z was identified as the most promising potential anticancer agent in present study, and was selected as lead compound for further detailed investigations.
Histone deacetylase inhibitors are considered among the most promising new anticancer drugs, and several agents have recently entered clinical trials.
Inhibition of angiogenesis is one of the most promising approaches in anticancer therapy.
One of the most promising strategies in anticancer therapies is the targeted delivery through malignancy-associated cellular markers.
The thiourea derivatives represent one of the most promising classes of anticancer agents with a wide range of activities against various leukemia and solid tumors [9 17].
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