Synthesis of pyrrolo[2,3- d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line
Synthesis of a new series of diarylureas and amides having pyrrolo[2,3- d]pyrimidine scaffold is described. Their in vitro antiproliferative activities against A375 human melanoma cell line and HS 27 fibroblast cell line were tested and the effect of substituents on pyrrolo[2,3- d]pyrimidine was inv...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2009-12, Vol.19 (23), p.6538-6543 |
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Sprache: | eng |
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Zusammenfassung: | Synthesis of a new series of diarylureas and amides having pyrrolo[2,3-
d]pyrimidine scaffold is described. Their in vitro antiproliferative activities against A375 human melanoma cell line and HS 27 fibroblast cell line were tested and the effect of substituents on pyrrolo[2,3-
d]pyrimidine was investigated. The newly synthesized compounds, except
N-acetyl derivatives
(Id,
Ie, and
Im), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds
Iq and
Ir having imidazole and morpholine moieties, respectively, showed the most potent antiproliferative activity against A375.
Synthesis of a new series of diarylureas and amides having pyrrolo[2,3-
d]pyrimidine scaffold is described. Their in vitro antiproliferative activities against A375 human melanoma cell line and HS 27 fibroblast cell line were tested and the effect of substituents on pyrrolo[2,3-
d]pyrimidine was investigated. The newly synthesized compounds, except
N-acetyl derivatives (
Id,
Ie, and
Im), generally showed superior or similar activity against A375 to Sorafenib. Among all of these derivatives, compounds
Iq and
Ir having imidazole and morpholine moieties, respectively, showed the most potent antiproliferative activity against A375. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2009.10.051 |