Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines. Part 2
- Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines. Part 2
- 정명호; 모하메드엘가말; 모하메드 사미르; 심태보; 유경호; 오창현
- Pyrrolo[3,2-c]pyridine; A375P; Antiproliferative activity; Melanoma; Diarylurea; Diarylamide
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 22, NO 13, 4362-4367
- A new series of diarylureas and diarylamides possessing 1H-pyrrolo[3,2-c]pyridine scaffold was designed
and synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and
NCI-9 human melanoma cell line panel were tested. All the target compounds, except three amino derivatives
8g, h and 9h, demonstrated superior potencies against A375P to Sorafenib. In addition, compounds
8a and 9b–f demonstrated higher potencies than Vemurafenib against A375P. Compounds 8c and 9b
were 7.50 and 454.90 times, respectively, more selective towards A375P melanoma cells over NIH3T3
fibroblasts. Furthermore, compounds 8d, e and 9a–d, f demonstrated very high potencies against the nine
tested melanoma cell lines at the NCI. The bisamide derivatives 9a–c, f showed 2-digit nanomolar IC50
values over different cell lines of the NCI-9 melanoma cell lines.
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