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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
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50초록
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
- 발행일
- 2009-12
- 유형
- Article
- 권
- 19
- 호
- 23
- 페이지
- 6538 ~ 6543
- 언어
- ENG
- 출판사
- PERGAMON-ELSEVIER SCIENCE LTD
- 발행국가
- 영국
- 분량
- 6 페이지
- ISSN
- E 1464-3405
P 0960-894X