2. Academic Validation
  3. Discovery of a new series of Aurora inhibitors through truncation of GSK1070916

Discovery of a new series of Aurora inhibitors through truncation of GSK1070916

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2552-5. doi: 10.1016/j.bmcl.2010.02.091.
Jesus R Medina 1,  Seth W Grant,  Jeffrey M Axten,  William H Miller,  Carla A Donatelli,  Mary Ann Hardwicke,  Catherine A Oleykowski,  Qiaoyin Liao,  Ramona Plant,  Hong Xiang
Affiliations

Affiliation

  • 1 Oncology Research, GlaxoSmithKline, Collegeville, PA 19426, USA. jesus.r.medina@gsk.com
PMID: 20335034 DOI: 10.1016/j.bmcl.2010.02.091
Abstract

Novel Aurora inhibitors were identified truncating clinical candidate GSK1070916. Many of these truncated compounds retained potent activity against Aurora B with good antiproliferative activity. Mechanistic studies suggested that these compounds, depending on the substitution pattern, may or may not exert their antiproliferative effects via inhibition of Aurora B. The SAR results from this investigation will be presented with an emphasis on the impact structural changes have on the cellular phenotype.

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