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A Highly Selective Staurosporine Derivative Designed by a New Selectivity Filter
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  • A Highly Selective Staurosporine Derivative Designed by a New Selectivity Filter
  • A Highly Selective Staurosporine Derivative Designed by a New Selectivity Filter
저자명
El-Deeb. Ibrahim M.,Jung. Su-Jin,Park. Byung-Sun,Yoo. Young-Jun,Choi. Ki-Hang,Yang. Young-Mok,Lee. Sang-Woo,Kim. In-Tae,Han. Don
간행물명
Bulletin of the Korean Chemical Society
권/호정보
2011년|32권 5호|pp.1709-1714 (6 pages)
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대한화학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

KIST301135 was semi-synthetically prepared by the reaction of Staurosporine with triphosgene in anhydrous dichloromethane. The structure of KIST301135 was confirmed by $^1H$ NMR, $^{13}C$ 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 $IC_{50}$ values. KIST301135 has shown much improved kinase inhibitory selectivity relative to Staurosporine in its potency at JAK3 kinase and CAMK2b kinase.