Inhibition of telomerase by BIBR 1532 and related analogues

DK Barma, A Elayadi, JR Falck, DR Corey

Index: Barma; Elayadi, Anissa; Falck; Corey, David R. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 7 p. 1333 - 1336

Full Text: HTML

Citation Number: 32

Abstract

BIBR 1532 has been reported to be a potent, small molecule inhibitor of human telomerase, suggesting it as a lead for the development of anti-telomerase therapy. We confirm the ability of BIBR 1532 to inhibit telomerase and report the discovery of an equally potent analogue. Importantly, IC50 values in cell extract are considerably higher than those previously reported using assays for purified enzyme, indicating that substantial improvement may be ...