# Late-stage functionalization and bioactivity investigation of azaphilone compounds

> **NIH NIH F31** · UNIVERSITY OF MICHIGAN AT ANN ARBOR · 2024 · $42,348

## Abstract

PROPOSAL SUMMARY
Traditional medicines relies on plants and fungi to provide treatments for various diseases. These treatments
have withstood the test of time with active ingredients that are natural products, compounds generated by these
organisms. Natural products are a successful source of inspiration for medicines and therapeutics today.
However, due to the complex structures of many natural products, synthetic routes toward these compounds are
often long and difficult. Thus, there is a need for new approaches to enable the synthesis of these compounds
in an efficient and high throughput manner to be able to test their viability as therapeutics. One natural product
class that has promise as therapeutics, but has little research due to the difficulty of synthesis, are azaphilone
natural products. Azaphilones have been used in China for over 1000 years in a health food remedy call “red
mold rice”. These molecules have shown antibacterial, antifungal, antiviral, anti-inflammatory, cholesterol
synthesis inhibition, and cytotoxic activity. Azaphilones are a large, structurally diverse class of natural products.
Development of a high throughput, efficient route to a large variety of azaphilones would enable access to
potentially life-saving therapeutics. Two subclasses that are prevalent in this natural product family are dimerized
and reduced azaphilones. I aim to use biocatalysis to synthesize these two subclasses of azaphilones in a high
throughput manner using P450 enzymes and reductase enzymes. Once these natural products are synthesized,
in combination with azaphilones I have previously made, I aim to investigate the biological activity using a
fluorescence polarization assay exploring azaphilone effects on protein-protein interactions. This will impact the
development of novel medicine alternatives for treating major human health concerns such as viral infections,
bacterial infections, fungal infections, high cholesterol, and cancer.

## Key facts

- **NIH application ID:** 10998541
- **Project number:** 1F31AT013031-01
- **Recipient organization:** UNIVERSITY OF MICHIGAN AT ANN ARBOR
- **Principal Investigator:** Katherine Jane Torma
- **Activity code:** F31 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2024
- **Award amount:** $42,348
- **Award type:** 1
- **Project period:** 2024-08-01 → 2026-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10998541

## Citation

> US National Institutes of Health, RePORTER application 10998541, Late-stage functionalization and bioactivity investigation of azaphilone compounds (1F31AT013031-01). Retrieved via AI Analytics 2026-05-27 from https://api.ai-analytics.org/grant/nih/10998541. Licensed CC0.

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