Synthesis of pyrrolo[2,3-d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line |
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Authors: | Myung-Ho Jung Hwan Kim Won-Kyoung Choi Mohammed I. El-Gamal Jin-Hun Park Kyung Ho Yoo Tae Bo Sim So Ha Lee Daejin Baek Jung-Mi Hah Jung-Hyuck Cho Chang-Hyun Oh |
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Affiliation: | 1. Biomaterials Research Center, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea;2. Department of Biomolecular Science, University of Science and Technology, 113 Gwahangno, Yuseong-gu, Daejeon 305-333, Republic of Korea;3. Department of Chemistry, Hanseo University, Seosan 356-706, Republic of Korea |
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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. |
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