Cytotoxic activity evaluation and QSAR study of chromene-based chalcones
Abstract Chalcone and chromene motifs are synthetic or naturally occurring scaffolds with significant cytotoxic profile. Two types of novel regioisomeric chromene-chalcone hybrids, namely 1-(6-chloro or 6-methoxy-2H-chromen-3-yl)-3-phenylprop-2-en-1-one (Type A) and 3-(6-chloro or 6-methoxy-2H-chromen-3-yl)-1-phenylprop-2-en-1-one (Type B), both with different substituents on the phenyl ring attached to propenone linkage, have been evaluated for their cytotoxic activity against breast cancer cell lines (MCF-7 and MDA-MB-231). The results indicate that type A of chromene-chalcones demonstrated better cytotoxic profile than type B especially in MDA-MB-231 cell line. In addition, the growth inhibitory activity of most of the target compounds is higher than Etoposide as a reference drug. QSAR analysis of these novel compounds demonstrated that topological and geometrical parameters are among the important descriptors that influence the cytotoxic activity profile of compounds..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2012 |
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| Erschienen: |
2012 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:35 |
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| Enthalten in: |
Archives of pharmacal research - 35(2012), 12 vom: Dez., Seite 2117-2125 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Firoozpour, Loghman [VerfasserIn] |
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| Links: |
Volltext [lizenzpflichtig] |
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| Anmerkungen: |
© The Pharmaceutical Society of Korea and Springer Science+Business Media Dordrecht 2012 |
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| doi: |
10.1007/s12272-012-1208-2 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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SPR024681962 |
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| 520 | |a Abstract Chalcone and chromene motifs are synthetic or naturally occurring scaffolds with significant cytotoxic profile. Two types of novel regioisomeric chromene-chalcone hybrids, namely 1-(6-chloro or 6-methoxy-2H-chromen-3-yl)-3-phenylprop-2-en-1-one (Type A) and 3-(6-chloro or 6-methoxy-2H-chromen-3-yl)-1-phenylprop-2-en-1-one (Type B), both with different substituents on the phenyl ring attached to propenone linkage, have been evaluated for their cytotoxic activity against breast cancer cell lines (MCF-7 and MDA-MB-231). The results indicate that type A of chromene-chalcones demonstrated better cytotoxic profile than type B especially in MDA-MB-231 cell line. In addition, the growth inhibitory activity of most of the target compounds is higher than Etoposide as a reference drug. QSAR analysis of these novel compounds demonstrated that topological and geometrical parameters are among the important descriptors that influence the cytotoxic activity profile of compounds. | ||
| 700 | 1 | |a Edraki, Najmeh |4 aut | |
| 700 | 1 | |a Nakhjiri, Maryam |4 aut | |
| 700 | 1 | |a Emami, Saeed |4 aut | |
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| 700 | 1 | |a Ardestani, Sussan Kabudanian |4 aut | |
| 700 | 1 | |a Khoshneviszadeh, Mehdi |4 aut | |
| 700 | 1 | |a Shafiee, Abbas |4 aut | |
| 700 | 1 | |a Foroumadi, Alireza |4 aut | |
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