Title |
Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies
|
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Published in |
Molecules, July 2016
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DOI | 10.3390/molecules21080977 |
Pubmed ID | |
Authors |
Hafiz Mansoor Ikram, Nasir Rasool, Muhammad Zubair, Khalid Mohammed Khan, Ghayoor Abbas Chotana, Muhammad Nadeem Akhtar, Nadiah Abu, Noorjahan Banu Alitheen, Abdallah Mohamed Elgorban, Usman Ali Rana |
Abstract |
The present study describes several novel 2,5-biaryl-3-hexylthiophene derivatives (3a-i) synthesized via a Pd(0)-catalyzed Suzuki cross-coupling reaction in moderate to good yields. The novel compounds were also analyzed for their anti-thrombolytic, haemolytic, and biofilm inhibition activities. In addition, the anti-tumor activity was also evaluated in vitro for newly-synthesized compounds, where 3-hexyl-2,5-bis(4-(methylthio)phenyl)thiophene exhibited the best anti-tumor activity against 4T1 cells with IC50 value of 16 μM. Moreover, 2,5-bis(4-methylphenyl)-3-hexylthiophene showed the highest activity against MCF-7 cells with an IC50 value of 26.2 μM. On the other hand, the compound 2,5-bis(4-chloropheny)-3-hexylthiophene exhibited excellent biofilm inhibition activity. Furthermore, the compound 2,5-bis(3-chloro-4-fluorophenyl)-3-hexylthiophene also exhibited better anti-thrombolytic and hemolytic activity results as compared to the other newly-synthesized compounds. |
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Demographic breakdown
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Scientists | 1 | 50% |
Members of the public | 1 | 50% |
Mendeley readers
Geographical breakdown
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Demographic breakdown
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Other | 2 | 8% |
Student > Master | 2 | 8% |
Professor | 2 | 8% |
Student > Bachelor | 1 | 4% |
Student > Doctoral Student | 1 | 4% |
Other | 5 | 20% |
Unknown | 12 | 48% |
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Chemistry | 5 | 20% |
Agricultural and Biological Sciences | 1 | 4% |
Biochemistry, Genetics and Molecular Biology | 1 | 4% |
Materials Science | 1 | 4% |
Engineering | 1 | 4% |
Other | 0 | 0% |
Unknown | 16 | 64% |