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

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

  • Bioorg Med Chem Lett. 2009 Dec 1;19(23):6538-43. doi: 10.1016/j.bmcl.2009.10.051.
Myung-Ho Jung 1,  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
Affiliations

Affiliation

  • 1 Biomaterials Research Center, Korea Institute of Science and Technology, Cheongryang, Seoul 130-650, Republic of Korea.
PMID: 19857963 DOI: 10.1016/j.bmcl.2009.10.051
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.

Figures