# Photochemical synthesis of bioactive molecules

> **NIH NIH R01** · UNIVERSITY OF MICHIGAN AT ANN ARBOR · 2021 · $414,893

## Abstract

PROJECT SUMMARY
The overarching theme of this proposal is the development and application of new and enabling photocatalytic
methods for the preparation of compounds capable of mimicking the structure of aniline motifs commonly
found in drug molecules. These approaches provide strategy-level advantages in their respective synthetic
applications due to broad functional group compatibility, mild reaction conditions, scalability, and operational
simplicity while simultaneously incorporating metabolism-based design criteria early in the drug discovery
process. New methods using visible light, a non-toxic 'reagent' that does not generate chemical waste, are
attractive strategies for chemical synthesis circumventing the reliance upon expensive and synthetically
challenging starting material preparation, further enabling synthesis in an environmentally conscious fashion.
The major goals of this proposal leverage strain-releasing ring-opening reactions for the preparation of
previously inaccessible motifs and the demonstration of their utility as replacements of metabolically-labile
aniline functionality in drug discovery. Specifically we will leverage these chemical findings to address modern
challenges in therapeutic development, namely: 1) novel KCNQ agonists for unmet needs in hearing disorders
(i.e. tinnitus; cyclodextrin-induced ototoxicity); and 2) metabolically-inert analogs of lapatinib which will
represent new leads in cancer therapy and antimicrobial research while also serving as biological probes for
studying the immunogenicity of hepatotoxic drugs.. These goals translate creativity in reaction science into
immediately-impactful and multi-faceted applications in drug discovery and are intended to demonstrate the
broad-reaching influence that can arise from investment in synthetic innovation.

## Key facts

- **NIH application ID:** 10252005
- **Project number:** 5R01GM127774-04
- **Recipient organization:** UNIVERSITY OF MICHIGAN AT ANN ARBOR
- **Principal Investigator:** Corey Stephenson
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $414,893
- **Award type:** 5
- **Project period:** 2018-09-20 → 2022-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10252005

## Citation

> US National Institutes of Health, RePORTER application 10252005, Photochemical synthesis of bioactive molecules (5R01GM127774-04). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10252005. Licensed CC0.

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