New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies

Title
New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies
Authors
박진헌엘가말이용섭오창현
Keywords
Anticancer; Antiproliferative activity; Imidazo[2,1-b]thiazole; A375P; Melanoma
Issue Date
2011-12
Publisher
European journal of medicinal chemistry
Citation
VOL 46, NO 12, 5769-5777
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/41412
ISSN
0223-5234
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KIST Publication > Article
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