Chinese Academy of Sciences

Zhejiang University

Jieyu Liu

Mengmeng Zhang

Jia Tao Li

Yubo Zhou

Yongzhou Hu

Weijuan Kan

Jun Wei

Dongyan Gu

Kaixiang Zhang

Rong Sheng

Provided by the present disclosure are an amino quinazolinone and amino isoquinolone derivatives. It is verified by numerous experiments that the compounds provided by the present disclosure have good inhibiting effects on PI3Kα and PI3Kγ, most of the compounds have prominent inhibiting effect on PI3Kα, and show strong growth inhibiting effect on PIK3CA mutant tumor cells such as human breast cancer cell strain (MCF7). Therefore, the amino quinazolinone and amino isoquinolone derivatives according to the present disclosure can be applied in the preparation of anti-tumor and anti-inflammatory medicines, and can be used as PI3Kα inhibitors in the preparation of medicines for treatment of human or animal cell proliferation related tumors, the medicines comprising the derivatives any one or more of pharmaceutically acceptable salts and solvates thereof as well as pharmaceutically acceptable carriers. Formulas a and b are shown as below:

Aminoquinazolinone and aminoisoquinolinone derivatives and application thereof

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Shanghai, China

Jieyu Liu