Novel Kinase Inhibitors

Advanced Anti-Cancer Therapy

Victoria University of Wellington Researchers have designed and synthesized a family of novel metabolites which demonstrate effective kinase inhibition properties

Innovation overview

VUW researchers have designed an synthesized a family of novel analogues based on furo[3,4-ß]pyran, a fungal secondary metabolite shown to have src-kinase inhibition activity.
The family of derivative compounds exhibit improved kinase inhibition, showing desirable selectivity between the kinase classes.
The furo[3,4-ß]pyran scaffold lends itself to multiple sites for chemical modification, structure-activity studies and the creation of new composition of matter intellectual property. Our current family of compounds based on the scaffold have very strong inhibition against BMX and BTK, which have been implicated in a range of auto-immune and oncology therapy applications.

Features

Natural Analogue
Compounds are analogues derived from a secondary fungal metabolite with excellent kinase inhibition properties
Selective Inhibition
Kinome screening shows that the first generation of compounds inhibit less than 10 kinases
BMX & BTK inhibition
Compounds demonstrate highly effective inhibition of BMX and BTK kinases
Low μM IC50 results
Low μM IC50 results in human leukaemia, ovarian and breast cancer cell lines
Strong IP Position
Clear ISR on novelty and inventive step for patent compound claims

Applications

Treating Malignant Cancers
Effective BMX and BTK kinase inhibition properties to prevent cancerous cell growth and division
Treatment for Osteoporosis
Inhibition of bone formation regulation kinases can enable treatment of conditions like osteoporosis

Kinase Inhibitor Scaffold

Technology Diagram

Research leader

Dr Joanne Harvey

A Senior Lecturer in chemistry at Victoria University of Wellington’s School of Chemical and Physical Sciences, Dr Joanne Harvey’s research focuses on organic synthesis.  Her research contributes to the activities of the Centre for Biodiscovery. Chemical synthesis and the extraction of natural products from plants, algae and bacteria are complementary methods for discovering novel and bioactive mo...