Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines
- Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines
- 엘가말; 정명호; 이웅산; 심태보; 유경호; 오창현
- Pyrrolo[3,2-c]pyridine; A375P; Antiproliferative activity; Melanoma; Diarylurea; Diarylamide
- Issue Date
- European journal of medicinal chemistry
- VOL 46, NO 8, 3218-3226
- Synthesis of a new series of diarylureas and diarylamides having 1H-pyrrolo[3,2-c]pyridine scaffold is
described. Their in vitro antiproliferative activity against A375P human melanoma cell line was tested
and the effect of substituents on pyrrolo[3,2-c]pyridine nucleus was investigated. The newly synthesized
compounds, except three N-tolyl derivatives (8f, 9f, and 9h), generally showed superior activity against
A375P to Sorafenib. Among all of these derivatives, compounds 8b, 8g, and 9aee showed the highest
potency against A375P with IC50 in nanomolar range. In addition, compounds 8d, 8e, 8h, 9g, 9i, and 9j
were more potent than Sorafenib but with IC50 in micromolar range. Compounds 8b, 8g, 9bed, and 9i
demonstrated higher selectivity towards A375P compared with NIH3T3 fibroblasts. The most potent
diarylurea 8g and diarylamide 9d were further tested and showed high potency over nine melanoma cell
lines at the NCI.
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