Synthesis of some tropane-based compounds targeting colon cancer
Background: In continuation of a previous work concerned with the anticancer activity of some 8-alkyl-2,4-bisarylidene-8-nortropan-3-ones, this work focuses on further modification to the tropane/pyran fused skeleton aiming to obtain improved anticancer activity. Methodology: Reaction of 8-alkyl-2,4...
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| Main Authors: | , , , , , , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
23 November 2020
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| In: |
Future medicinal chemistry
Year: 2020, Volume: 12, Issue: 23, Pages: 2123-2140 |
| ISSN: | 1756-8927 |
| DOI: | 10.4155/fmc-2020-0097 |
| Online Access: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.4155/fmc-2020-0097 Verlag, lizenzpflichtig, Volltext: https://www.future-science.com/doi/10.4155/fmc-2020-0097 
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| Author Notes: | Nermin Samir, Riham F George, Eman Z Elrazaz, Iriny M Ayoub, ElSayed M Shalaby, Jasper R Plaisier, Nicola Demitri and Michael Wink |
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| 520 | |a Background: In continuation of a previous work concerned with the anticancer activity of some 8-alkyl-2,4-bisarylidene-8-nortropan-3-ones, this work focuses on further modification to the tropane/pyran fused skeleton aiming to obtain improved anticancer activity. Methodology: Reaction of 8-alkyl-2,4-bisarylidene-8-nortropan-3-ones 1-21 with malononitrile under basic conditions afforded tropane/pyran hybrids 22-40 and tropane/pyridine hybrids 41, 42. X-ray crystallography for compounds 22 and 41 as representative examples confirmed their structures. They were tested for their anticancer activity in the HCT116 cell line. Results: Compounds 26 and 33 were the most active compounds with IC50 values of 3.39 and 0.01 μM against HCT116. Moreover, they revealed cyclin-dependent kinase-2 (CDK2) inhibition with IC50 = 104.91 and 49.13 nM, respectively. Furthermore, molecular docking of compounds 26 and 33 in the active site of CDK2 confirmed the obtained results. Conclusion: Tropane/pyran scaffold can be considered as a promising core for anticancer agents acting as CDK2 inhibitors. | ||
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