2. Academic Validation
  3. Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity

Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity

  • ACS Med Chem Lett. 2017 Jul 26;8(8):875-880. doi: 10.1021/acsmedchemlett.7b00222.
Chengbin Yang 1,  Xi Zhang 2,  Yi Wang 2,  Yongtai Yang 1,  Xiaofeng Liu 1,  Mingli Deng 1,  Yu Jia 1,  Yun Ling 1,  Ling-Hua Meng 2,  Yaming Zhou 1
Affiliations

Affiliations

  • 1 Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai 200433, China.
  • 2 Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
PMID: 28835805 DOI: 10.1021/acsmedchemlett.7b00222
Abstract

The phosphoinositide 3-kinase (PI3K) inhibitors potently inhibit the signaling pathway of PI3K/Akt/mTOR, which provides a promising new approach for the molecularly targeted Cancer therapy. In this work, a novel series of 7-azaindole scaffold derivatives was discovered by the fragment-based growing strategy. The structure-activity relationship profiles identified that the 7-azaindole scaffold derivatives exhibit potent activity against PI3K at molecular and cellular levels as well as cell proliferation in a panel of human tumor cells.

Keywords

1H-pyrrolo[2,3-b] pyridine; PI3K; PI3K/mTOR; cancer therapy; oncology.

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