Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold
- Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold
- 모하메드엘가말; 모하메드 사미르; 마흐무드 가말엘딘; 유경호; 백대진; 오창현
- Anticancer; Bisamide; Diarylamide; FMS kinase; Pyrrolo[3,2-c]pyridine
- Issue Date
- Archiv der Pharmazie
- VOL 347, NO 9, 635-641
- A bisamide compound 1 possessing the pyrrolo[3,2-c]pyridine nucleus was synthesized and biologically evaluated. It was tested for kinase inhibitory activity over a panel of 47 kinases, and its selectivity toward the FMS kinase was accidentally discovered. Compound 1 was tested over a panel of seven ovarian, two prostate, and six breast cancer cell lines at a single dose concentration of 10 µM and showed high activity. It was further tested in a 5-dose mode to determine its IC50 and total growth inhibition (TGI) values over the 15 cell lines. Compound 1 showed high potency on the submicromolar scale and good efficacy. The cytotoxic effect of compound 1 over peritoneal macrophages was also investigated. Compound 1 demonstrated higher selectivity against different cancer cell lines compared with HS-27 fibroblasts.
- Appears in Collections:
- KIST Publication > Article
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.