Pyrido[2',1':2,3]imidazo[4,5-<i>c</i>]isoquinolin-5-amines as Potential Cytotoxic Agents against Human Neuroblastoma
We report herein the evaluation of various pyrido[2',1':2,3]imidazo[4,5-<i>c</i>]isoquinolin-5-amines as potential cytotoxic agents. These molecules were obtained by developing the multicomponent Groebke-Blackburn-Bienaymé reaction to yield various pyrido[2',1':2,3]im...
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| Main Authors: | , , , , , , , |
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| Format: | Book |
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MDPI AG,
2021-07-01T00:00:00Z.
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| Summary: | We report herein the evaluation of various pyrido[2',1':2,3]imidazo[4,5-<i>c</i>]isoquinolin-5-amines as potential cytotoxic agents. These molecules were obtained by developing the multicomponent Groebke-Blackburn-Bienaymé reaction to yield various pyrido[2',1':2,3]imidazo[4,5-c]quinolines which are isosteres of ellipticine whose biological activities are well established. To evaluate the anticancer potential of these pyrido[2',1':2,3]imidazo[4,5-<i>c</i>]isoquinolin-5-amine derivatives in the human neuroblastoma cell line, the cytotoxicity was examined using the WST-1 assay after 72 h drug exposure. A clonogenic assay was used to assess the ability of treated cells to proliferate and form colonies. Protein expressions (Bax, bcl-2, cleaved caspase-3, cleaved PARP-1) were analyzed using Western blotting. The colony number decrease in cells was 50.54%, 37.88% and 27.12% following exposure to compounds <b>2d</b>, <b>2g</b> and <b>4b</b> respectively at 10 μM. We also show that treating the neuroblastoma cell line with these compounds resulted in a significant alteration in caspase-3 and PARP-1 cleavage. |
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| Item Description: | 10.3390/ph14080750 1424-8247 |