Pharmacology Research Today is a free monthly online journal that collates and summarizes the latest research about Pharmacology, including details on pharmacogenomics, drug development, new medications.

Synthesis of the new pseudo-symmetrical tamoxifen derivatives and their anti-tumor activity.

Shiina I, Sano Y, Nakata K, Kikuchi T, Sasaki A, Ikekita M, Hasome Y

Department of Applied Chemistry, Faculty of Science, Tokyo University of Science, Kagurazaka, Shinjuku-ku, Tokyo 162-8601, Japan. shiina@rs.kagu.tus.ac.jp

Three new pseudo-symmetrical tamoxifen derivatives, RID-B (15), C (16), and D (17), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of the pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 15 strongly inhibits the viability of HL-60 human acute promyelocytic leukemia, whereas 16 possesses medium activity against the cell line and 17 has no effect on the cell viability. The agarose gel electrophoresis for DNA cleavage showed the cell death might be induced by apoptosis.

Published 6 April 2007 in Bioorg Med Chem Lett, 17(9): 2421-4.
Full-text of this article is available online (may require subscription).

© 2005-2008 Pharmacology Research Today. All Rights Reserved.