Abstract
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.
Original language | English |
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Pages (from-to) | 6538-6543 |
Number of pages | 6 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 19 |
Issue number | 23 |
DOIs | |
Publication status | Published - 2009 Dec 1 |
Bibliographical note
Funding Information:We are grateful to the Korea Institute of Science and Technology (KIST) for financial support.
Keywords
- A375
- Antiproliferative activity
- HS 27
- Melanoma
- Pyrrolo[2,3-d]pyrimidine
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry