Chemical Space Exploration of Oxetanes

Author(s)

Alves, Fernando Rodrigues de Sa ^[1] ; Counago, Rafael M. ^[2] ; Laufer, Stefan ^{[1, 3]}

Affiliation

^[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

• Document type: Journal article
• Source: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES; v. 21, n. 21 NOV 2020.
• Web of Science Citations: 0

Abstract

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. (AU)

• FAPESP's process: 14/50897-0 - INCT 2014: Open-acess Medicinal Chemistry Centre (OpenMedChem)
• Grantee: Katlin Brauer Massirer
• Support Opportunities: Research Projects - Thematic Grants
• FAPESP's process: 13/50724-5 - Protein Kinase Chemical Biology Center: supporting drug development through open-access research
• Grantee: Paulo Arruda
• Support Opportunities: Research Grants - Research Partnership for Technological Innovation - PITE