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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 5
BKCSDE 32(5)
May 20, 2011 

A Highly Selective Staurosporine Derivative Designed by a New Selectivity Filter
Ibrahim M. El-Deeb, Su Jin Jung, Byung Sun Park, Young Jun Yoo, Kihang Choi, Young Mok Yang, Sang Woo Lee,¶ In Tae Kim,¶ Dong Keun Han,*, So Ha Lee*,
Staurosporine derivative, Selectivity filter, Kinase selectivity, Cancer
KIST301135 was semi-synthetically prepared by the reaction of Staurosporine with triphosgene in anhydrous dichloromethane. The structure of KIST301135 was confirmed by 1H NMR, 13C NMR, and high resolution mass spectrum. KIST301135 was initially tested in a single dose duplicate mode at a concentration of 20 nM over a panel of 53 kinases against Staurosporine as a positive control. KIST301135 has showed inhibitions above 75% in only 2 kinases (FLT3 and JAK3 kinases) of the 53 tested kinases, while Staurosporine has showed inhibitions above 80% in about 62% of the tested kinases. KIST301135 was retested at a 5-dose testing mode over the 9 kinases inhibited by percentages over 20 at the single dose testing in order to determine its IC50 values. KIST301135 has shown much improved kinase inhibitory selectivity relative to Staurosporine in its potency at JAK3 kinase and CAMK2b kinase.
1709 - 1714
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