2. Academic Validation
  3. Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors

Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors

  • Bioorg Med Chem Lett. 2008 Sep 1;18(17):4907-12. doi: 10.1016/j.bmcl.2008.06.042.
Yihan Wang 1,  William C Shakespeare,  Wei-Sheng Huang,  Raji Sundaramoorthi,  Scott Lentini,  Sasmita Das,  Shuangying Liu,  Geeta Banda,  David Wen,  Xiaotian Zhu,  Qihong Xu,  Jeffrey Keats,  Frank Wang,  Scott Wardwell,  Yaoyu Ning,  Joseph T Snodgrass,  Mark I Broudy,  Karin Russian,  David Dalgarno,  Tim Clackson,  Tomi K Sawyer
Affiliations

Affiliation

  • 1 ARIAD Pharmaceuticals, Inc., 26 Landsdowne Street, Cambridge, MA 02139, USA.
PMID: 18691885 DOI: 10.1016/j.bmcl.2008.06.042
Abstract

Novel N(9)-arenethenyl purines, optimized potent dual Src/Abl tyrosine kinase inhibitors, are described. The key structural feature is a trans vinyl linkage at N(9) on the purine core which projects hydrophobic substituents into the selectivity pocket at the rear of the ATP site. Their synthesis was achieved through a Horner-Wadsworth-Emmons reaction of N(9)-phosphorylmethylpurines and substituted benzaldehydes or Heck reactions between 9-vinyl purines and aryl halides. Most compounds are potent inhibitors of both Src and Abl kinase, and several possess good oral bioavailability.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z