Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer

In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a-e and 7a-i) was designed and synthesised. The anticancer activity for compounds (5b-d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subject...

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Main Authors: Wagdy M. Eldehna (Author), Rofaida Salem (Author), Zainab M. Elsayed (Author), Tarfah Al-Warhi (Author), Hamada R. Knany (Author), Rezk R. Ayyad (Author), Thamer Bin Traiki (Author), Maha-Hamadien Abdulla (Author), Rehan Ahmad (Author), Hatem A. Abdel-Aziz (Author), Radwan El-Haggar (Author)
Format: Book
Published: Taylor & Francis Group, 2021-01-01T00:00:00Z.
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Summary:In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a-e and 7a-i) was designed and synthesised. The anticancer activity for compounds (5b-d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subjected to the five-dose screen where it showed excellent broad activity against almost all tested cancer subpanels. Furthermore, all conjugates (5a-e and 7a-i) showed a good anti-proliferative activity towards colorectal cancer SW-620 and HT-29 cell lines, with an excellent inhibitory effect for compounds 5a and 5d (IC50 = 8.7 and 9.4 µM (5a), and 6.5 and 9.8 µM for (5d), respectively). Both compounds displayed selective cytotoxicity with good safety profile. In addition, both compounds provoked apoptosis in a dose dependent manner in SW-620 cells. Also, they significantly inhibited the anti-apoptotic Bcl2 protein expression and increased the cleaved PARP level that resulted in SW-620 cells apoptosis.
Item Description:1475-6366
1475-6374
10.1080/14756366.2021.1944127