2. Academic Validation
  3. Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives

Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives

  • Bioorg Med Chem Lett. 2020 Jun 15;30(12):127194. doi: 10.1016/j.bmcl.2020.127194.
Hao-Yue Xiang 1,  Yan-Hong Chen 2,  Yi Wang 2,  Xi Zhang 2,  Jian Ding 2,  Ling-Hua Meng 3,  Chun-Hao Yang 4
Affiliations

Affiliations

  • 1 College of Chemistry and Chemical Engineering, Central South University, Changsha, Hunan 410083, PR China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.
  • 2 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China.
  • 3 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. Electronic address: lhmeng@simm.ac.cn.
  • 4 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, PR China. Electronic address: chyang@simm.ac.cn.
PMID: 32317209 DOI: 10.1016/j.bmcl.2020.127194
Abstract

A series of 6-aminocarbonyl pyrrolo[2,1-f][1,2,4]triazine derivatives were designed by scaffold hopping strategy. The IC50 values of compound 14a against PI3Ks were measured, showing selective activity against p110α and p110δ with IC50s of 122 nM and 119 nM respectively. All the synthesized compounds were evaluated for their antiproliferative activity against human Cancer cells by SRB assay. Compounds 14a, 14p and 14q exhibited potent antiproliferative activity against five types of human Cancer cells and the PK property of 14q was also investigated here.

Keywords

Antiproliferative; Cancer; Kinase; PI3K inhibitors; Pyrrolo[2,1-f][1,2,4]triazine; Therapy.

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