Synthesis, antiproliferative activity and 2D-QSAR study of some 8-alkyl-2,4-bisbenzylidene-3-nortropinones
Aim: Colon cancer is the third leading cause of death worldwide; therefore, there is a need for an effective therapy with lower side effects. Methods: A series of 8-alkyl-2,4-bisbenzylidene-3-nortropinones 3 & 14-39 was prepared via Claisen-Schmidt condensation of 8-alkyl-3-nortropinones 11-13 w...
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| Hauptverfasser: | , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
10 December 2018
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| In: |
Future medicinal chemistry
Year: 2018, Jahrgang: 10, Heft: 24, Pages: 2815-2833 |
| ISSN: | 1756-8927 |
| DOI: | 10.4155/fmc-2018-0205 |
| Online-Zugang: | Verlag, Volltext: https://doi.org/10.4155/fmc-2018-0205 Verlag: https://www.future-science.com/doi/10.4155/fmc-2018-0205 
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| Verfasserangaben: | Riham F George, Nermin Samir, Iriny M Ayoub, ElSayed M Shalaby, Nicola Demitri & Michael Wink |
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| 245 | 1 | 0 | |a Synthesis, antiproliferative activity and 2D-QSAR study of some 8-alkyl-2,4-bisbenzylidene-3-nortropinones |c Riham F George, Nermin Samir, Iriny M Ayoub, ElSayed M Shalaby, Nicola Demitri & Michael Wink |
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| 520 | |a Aim: Colon cancer is the third leading cause of death worldwide; therefore, there is a need for an effective therapy with lower side effects. Methods: A series of 8-alkyl-2,4-bisbenzylidene-3-nortropinones 3 & 14-39 was prepared via Claisen-Schmidt condensation of 8-alkyl-3-nortropinones 11-13 with different aromatic aldehydes. The target compounds were screened for their antiproliferative activity. Results: Most of the prepared compounds showed promising antiproliferative activity against many of 60 National Cancer Institute cell lines at 10 μM. Furthermore, 8-ethyl-2,4-bis(3,4-dimethoxybenzylidene)-8-nortropin-3-one 29 and its 3,4,5-trimethoxy analog 30 were the most active compounds against HCT116 cell line with IC50 values 0.01 and 0.46 μM, respectively. Using CODESSA-Pro software, a significant 2D-quantitative structure-activity relationship (QSAR) model was obtained. Conclusion: The 8-Alkyl-2,4-bisbenzylidene-8-azabicyclo[3.2.1]octan-3-one represents an interesting core for further structural optimization to obtain more promising hits. | ||
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