Chemical Space Exploration of Oxetanes

被引：3

作者：

Alves, Fernando Rodrigues de Sa ^{[1
]}

Counago, Rafael M. ^{[2
]}

Laufer, Stefan ^{[1
,3
]}

机构：

[1] Eberhard Karls Univ Tubingen, Fac Sci, Inst Pharmaceut Sci, Dept Pharmaceut & Med Chem, D-72074 Tubingen, Germany

[2] Univ Estadual Campinas, Ctr Quim Med CQMED, Ctr Biol Mol & Engn Genet CBMEG,UNICAMP,Inst Biol, Struct Genom Consortium,Dept Genet & Evolucao, BR-13083875 Campinas, SP, Brazil

[3] Tubingen Ctr Acad Drug Discovery, D-72076 Tubingen, Germany

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2020年 / 21卷 / 21期

基金：

巴西圣保罗研究基金会;

关键词：

oxetane; chemical space; nonclassical isosterism; Buchwald– Hartwig reaction; kinases; PALLADIUM-CATALYZED AMINATION; KINASE; POTENT; REACTIVITY; INHIBITORS; CONVERSION; DISCOVERY; ANALOGS; DESIGN;

D O I：

10.3390/ijms21218199

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：

This paper focuses on new derivatives bearing an oxetane group to extend accessible chemical space for further identification of kinase inhibitors. The ability to modulate kinase activity represents an important therapeutic strategy for the treatment of human illnesses. Known as a nonclassical isoster of the carbonyl group, due to its high polarity and great ability to function as an acceptor of hydrogen bond, oxetane seems to be an attractive and underexplored structural motif in medicinal chemistry.

引用

页码：1 / 18

页数：18

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