2. Academic Validation
  3. Design, synthesis and evaluation of 2, 6, 8-substituted Imidazopyridine derivatives as potent PI3K α inhibitors

Design, synthesis and evaluation of 2, 6, 8-substituted Imidazopyridine derivatives as potent PI3K α inhibitors

  • J Enzyme Inhib Med Chem. 2023 Dec;38(1):2155638. doi: 10.1080/14756366.2022.2155638.
Rui Chen 1,  Zhongyuan Wang 2,  Lijie Sima 3,  Hu Cheng 1,  Bilan Luo 1,  Jianta Wang 1,  Bing Guo 4,  Shunyi Mao 5,  Zhixu Zhou 5,  Jingang Peng 1,  Lei Tang 1,  Xinfu Liu 3,  Weike Liao 1
Affiliations

Affiliations

  • 1 Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang, China.
  • 2 Department of Pharmacy, Guizhou Provincial People's Hospital, Guiyang, China.
  • 3 Department of Hematology and Oncology, The Affiliated Shaoyang Hospital, Hengyang Medical School, University of South China (Shaoyang Central Hospital), China.
  • 4 Guizhou Provincial Key Laboratory of Pathogenesis and Drug Research on Common Chronic Diseases, Guizhou Medical University, Guiyang, China.
  • 5 School of Pharmaceutical Sciences, Guizhou University, Guiyang, China.
PMID: 36650905 DOI: 10.1080/14756366.2022.2155638
Abstract

Inhibition of PI3K pathway has become a desirable strategy for Cancer treatment. In this work, a series of 2, 6, 8-substituted Imidazo[1,2-a]pyridine derivatives were designed and screened for their activities against PI3Kα and a panel of PI3Kα-addicted Cancer cells. Among them, compound 35 was identified as a PI3Kα inhibitor with nanomolar potency as well as acceptable antiproliferative activity. Flow cytometry analysis confirmed 35 induced cell cycle arrest and Apoptosis in T47D cells. In addition, it also showed desirable in vitro ADME properties. The design, synthesis, and SAR exploration of 35 are described within.

Keywords

Imidazo[12-a]pyridine derivatives; PI3Kα; antitumor activity; synthesis.

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