Synthesis of pyrrolo[2,3-d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line

  • Jung, Myung-Ho; 
  • Kim, Hwan; 
  • Choi, Won-Kyoung; 
  • El-Gamal, Mohammed I.; 
  • Park, Jin-Hun; 
  • ... Hah, Jung-Mi; 
  • 외 6명
Citations

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48
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50

초록

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. (C) 2009 Published by Elsevier Ltd.

키워드

Pyrrolo[2,3-d]pyrimidine; A375; HS 27; Antiproliferative activity; Melanoma; REFRACTORY SOLID TUMORS; FACTOR RECEPTOR INHIBITOR; RAF KINASE; SUBSTITUTED UREAS; PHASE-I; BAY-43-9006; THERAPY; PHARMACOKINETICS; INTERLEUKIN-2; PATHWAY
제목
Synthesis of pyrrolo[2,3-d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line
저자
Jung, Myung-Ho; Kim, Hwan; Choi, Won-Kyoung; El-Gamal, Mohammed I.; Park, Jin-Hun; Yoo, Kyung Ho; Sim, Tae Bo; Lee, So Ha; Baek, Daejin; Hah, Jung-Mi; Cho, Jung-Hyuck; Oh, Chang-Hyun
DOI
10.1016/j.bmcl.2009.10.051
발행일
2009-12
유형
Article
저널명
Bioorganic & Medicinal Chemistry Letters
권
19
호
23
페이지
6538 ~ 6543