2. Academic Validation
  3. Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors

Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors

  • Bioorg Med Chem Lett. 2012 Jan 1;22(1):339-42. doi: 10.1016/j.bmcl.2011.11.003.
Jia Wang 1,  Xiang Wang,  Yanhong Chen,  Simeng Chen,  Guang Chen,  Linjiang Tong,  Linghua Meng,  Yuyuan Xie,  Jian Ding,  Chunhao Yang
Affiliations

Affiliation

  • 1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR China.
PMID: 22130133 DOI: 10.1016/j.bmcl.2011.11.003
Abstract

PI3K is a promising therapeutic target for Cancer. With PI-103 as the lead compound, we designed and synthesized 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl)morpholine derivatives. 9, 10a, 10d, 10e had the IC(50) against PI3Kα comparable with PI-103. All of the compounds showed selectivity over 15 tested protein kinases and anti-proliferative activity at micromolar concentration against several Cancer cell lines.

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