Abstract
A series of novel cyclopent[b]indole analogues that hold isoxazolo-, pyrido-templates were designed and synthesized in good yields. The in vitro cytotoxicity was concerned for all the newly synthesized compounds by MTT assay against HeLa (cervix adeno carcinoma) and MCF-7 (breast cancer). These synthesized compounds were further compared with the standard drug ellipticine, 5-fluorouracil, cisplatin, and methotrexate. The synthesized heteroannulated cyclopent[b]indole compounds were found to show better cytotoxic activity against HeLa and MCF-7 with primary structure activity relationship studies. To identify with the nature of interactions of these molecules, we performed molecular docking studies using the protein kinase CK2 inhibitors. The docking results afforded some valuable information for the future design of more potent inhibitors.
| Original language | English |
|---|---|
| Pages (from-to) | 447-461 |
| Number of pages | 15 |
| Journal | Synthetic Communications |
| Volume | 48 |
| Issue number | 4 |
| Early online date | 24 Jan 2018 |
| DOIs | |
| Publication status | Published - 16 Feb 2018 |
Keywords
- CK2 inhibitors
- HeLa and MCF-7
- isoxazolo-cyclopent[b]indole
- pyrido-cyclopent[b]indole
Access to Document
- Full-text PDF (accepted author manuscript)
This is the author accepted manuscript (AAM). The final published version (version of record) is available online via Taylor and Francis at http://www.tandfonline.com/doi/full/10.1080/00397911.2017.1407792. Please refer to any applicable terms of use of the publisher.