Facile synthesis and antiproliferative activity of 7H-benzo[7,8]chromeno[2,3-d]pyrimidin-8-amines
Copyright © 2016 Elsevier Masson SAS. All rights reserved..
A series of 7H-benzo[7,8]chromeno[2,3-d]pyrimidin-8-amines 6a-t were synthesized as new potential antiproliferative agents. The in vitro antiproliferative activity evaluation of title compounds using MTT assay revealed that most compounds showed significant activity against tested cancer cell lines (A549, MOLT-4, and HeLa). The 2-fluoro-aniline derivatives 6e and 6l were the most active compounds against A549 and MOLT-4 cells, respectively. The benzylamine analog 6h showed superior activity against HeLa cells. However, compound 6l with IC50 values of 5.2-6.9 μM had the best profile of activity against all tested cell lines. The morphological and flow cytometric analyses showed that compound 6l can induce apoptosis in the MOLT-4 cells.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2017 |
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| Erschienen: |
2017 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:127 |
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| Enthalten in: |
European journal of medicinal chemistry - 127(2017) vom: 15. Feb., Seite 128-136 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Akrami, Hamidreza [VerfasserIn] |
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| Links: |
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| Themen: |
Anticancer |
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| Anmerkungen: |
Date Completed 21.02.2017 Date Revised 12.01.2018 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejmech.2016.12.037 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM26759545X |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2016 Elsevier Masson SAS. All rights reserved. | ||
| 520 | |a A series of 7H-benzo[7,8]chromeno[2,3-d]pyrimidin-8-amines 6a-t were synthesized as new potential antiproliferative agents. The in vitro antiproliferative activity evaluation of title compounds using MTT assay revealed that most compounds showed significant activity against tested cancer cell lines (A549, MOLT-4, and HeLa). The 2-fluoro-aniline derivatives 6e and 6l were the most active compounds against A549 and MOLT-4 cells, respectively. The benzylamine analog 6h showed superior activity against HeLa cells. However, compound 6l with IC50 values of 5.2-6.9 μM had the best profile of activity against all tested cell lines. The morphological and flow cytometric analyses showed that compound 6l can induce apoptosis in the MOLT-4 cells | ||
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| 650 | 4 | |a Benzochromene | |
| 650 | 4 | |a Cytotoxic agents | |
| 650 | 4 | |a Polycyclic compounds | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Pyrimidines |2 NLM | |
| 700 | 1 | |a Safavi, Maliheh |e verfasserin |4 aut | |
| 700 | 1 | |a Mirjalili, Bibi Fatemeh |e verfasserin |4 aut | |
| 700 | 1 | |a Dehghani Ashkezari, Mahmood |e verfasserin |4 aut | |
| 700 | 1 | |a Dadfar, Farhang |e verfasserin |4 aut | |
| 700 | 1 | |a Mohaghegh, Najme |e verfasserin |4 aut | |
| 700 | 1 | |a Emami, Saeed |e verfasserin |4 aut | |
| 700 | 1 | |a Salehi, Fahimeh |e verfasserin |4 aut | |
| 700 | 1 | |a Nadri, Hamid |e verfasserin |4 aut | |
| 700 | 1 | |a Ardestani, Sussan K |e verfasserin |4 aut | |
| 700 | 1 | |a Firoozpour, Loghman |e verfasserin |4 aut | |
| 700 | 1 | |a Khoobi, Mehdi |e verfasserin |4 aut | |
| 700 | 1 | |a Foroumadi, Alireza |e verfasserin |4 aut | |
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