Design and synthesis of novel β‐carboline‐bisindole hybrids as potential anticancer agents

ChemMedChem
Tuan Dang1, Nguyễn Thị Thanh Huyền2, Ban Van Phuc3, Tran Thi Huyen4, Tran Thi Hong5, Hien Nguyen6, Van Ha Nguyen5, Minh Tho Nguyen7, Tran Quang Hung3, Chau Phi Dinh8
1Vietnam National University, Chemistry, 19 Le Thanh Tong Street, 100000 Hanoi, VIET NAM
2Vietnam National University Hanoi, chemistry, VIET NAM
3Vietnam Academy of Science and Technology, chemistry, VIET NAM
4Vietnam National University, chemistry, 19 Le Thanh Tong Street, Hanoi, 100000 Hanoi, VIET NAM
5Vietnam National University, chemistry, VIET NAM
6Hanoi National University of Education, chemistry, VIET NAM
7KU Leuven, chemistry, BELGIUM
8NuChem Therapeutics, chemistry, CANADA

Tóm tắt

We are reporting a short and convenient pathway for the synthesis of novel β‐carboline‐bisindole hybrid compounds from relatively cheap and commercially available chemicals such as tryptamine, dialdehydes and indoles. These newly designed compounds can also be prepared in high yields with the tolerance of many functional groups under mild conditions. Notably, these β‐carboline‐bisindole hybrid compounds exhibited some promising applications as anticancer agents against the three common cancer cell lines MCF‐7 (breast cancer), SK‐LU‐1 (lung cancer), and HepG2 (liver cancer). The two best compounds 5b and 5g inhibited the aforementioned cell lines with the same range of the reference Ellipticine at less than 2 µM. A molecular docking study to gain more information about the interactions between the synthesized molecules and the kinase domain of the EGFR was performed. Therefore, this finding can have significant impacts on the development of future research in medicinal chemistry and drug discovery.

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