2. Academic Validation
  3. Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity

Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity

  • Bioorg Med Chem Lett. 2002 Nov 4;12(21):3191-3. doi: 10.1016/s0960-894x(02)00568-1.
Hitoshi Ohki 1,  Kenji Hirotani,  Hiroyuki Naito,  Satoru Ohsuki,  Megumi Minami,  Akio Ejima,  Yukiko Koiso,  Yuichi Hashimoto
Affiliations

Affiliation

  • 1 Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co. Ltd., 16-13, Kita-kasai 1-chome, Edogawa-ku, 134, Tokyo, Japan. [email protected]
PMID: 12372531 DOI: 10.1016/s0960-894x(02)00568-1
Abstract

Pyrimidinyl pyrazole derivatives 1-4, prepared as a new scaffold of an anti-tumor agent, showed antiproliferative activity against human lung Cancer cell lines and inhibited tubulin polymerization. Furthermore, it was found that compound 2 bound at the colchicine site on tubulin, but the tubulin binding pattern was different from that of colchicine. Here, we describe the synthesis of the derivatives and the differences of the action mechanism on tubulin polymerization inhibition between compound 2 and colchicine.

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