New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies
- New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies
- 박진헌; 엘가말; 이용섭; 오창현
- Anticancer; Antiproliferative activity; Imidazo[2,1-b]thiazole; A375P; Melanoma
- Issue Date
- European journal of medicinal chemistry
- VOL 46, NO 12, 5769-5777
- A series of 18 new imidazo[2,1-b]thiazole derivatives was synthesized. Their in vitro antiproliferative
activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds
15, 16, 18, 22, 26-28, and 31 showed superior potency against A375P to sorafenib. In addition,
compounds 26 and 27 showed selectivity toward melanoma cell lines than for other cancer types. Both
compounds exerted sub-micromolar IC50 values over 7 (including A375P) and 6 melanoma cell lines,
respectively. In silico studies are also reported. ADME profiling, in silico toxicity, drug-likeness, and drugscore
data of compounds 26 and 27 are promising.
- 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.