Synthesis and biological evaluation of 4H-benzo[e][1,3]oxazin-4-ones analogues of TGX-221 as inhibitors of PI3Kβ

被引：1

作者：

Mohammed, Ehtesham U. R. ^{[1
]}

Porter, Zoe J. ^{[2
]}

Jennings, Ian G. ^{[2
]}

Al-Rawi, Jasim M. A. ^{[1
]}

Thompson, Philip E. ^{[2
]}

Angove, Michael J. ^{[1
]}

机构：

[1] La Trobe Univ, La Trobe Inst Mol Sci, Pharm & Biomed Sci, POB 199, Bendigo, Vic 3552, Australia

[2] Monash Univ, Monash Inst Pharmaceut Sci, Med Chem, 381 Royal Parade, Parkville, Vic 3052, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2022年 / 69卷

关键词：

1,3-Benzoxazin-4-ones; Anticancer; PI3K beta; DEPENDENT PROTEIN-KINASE; DNA-PK; SELECTIVE INHIBITOR; ANTIPLATELET; PI3K; DISCOVERY; ELUCIDATION; POTENT; TARGET;

D O I：

10.1016/j.bmc.2022.116832

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A novel series of TGX-221 analogues was prepared that include isosteric replacement of the 4H-pyrido[1,2-a] pyrimidin-4-one with a 4H-benzo[e][1,3]oxazin-4-one scaffold. The compounds that included an -CH(CH3) NH- type linker showed comparable activity to TGX-221 analogues with the isosterism supported by the comparative SAR analysis. The analogues containing an -CH(CH3)O- linker were less active but still showed useful SAR including a favoured o-methyl substitution.

引用

页数：5

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