# Identification of Dual CSF-1R/Aurora B Kinase Inhibitors as a Novel Breast Cancer Treatment Paradigm

> **NIH NIH K00** · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · 2020 · $78,427

## Abstract

Abstract
 Drug discovery and development is undergoing rapid change toward an increasing dependency on
academic institutions providing sources of new potential treatment. With this change, there is a growing need
for academic researchers who are knowledgeable in all steps of translational research in order to progress
compounds far into the drug discovery pipeline. It is my goal to become a professor focused on translational
research and developing new treatments for cancer therapy. Dr. Hong-yu Li and I have devised a training plan
that address my goals and provides a clear path to achieve them.
 The first portion of the training plan is the dissertation work already completed, which focused on
developing a strong foundation in organic and medicinal chemistry. In the first project, we identified TrkA
kinase inhibitors using a pyrazine based scaffold. The second project was centered on developing a library of
Flt3 kinase inhibitors using novel synthetic methodology developed in the lab. Additional side projects also
focused on developing new synthetic methodology to access biologically relevant molecules.
 The dissertation work to be completed is a comprehensive translational project aiming to develop lead
compounds with dual activity against the CSF-1R and Aurora B kinases. Recently published findings suggest
an indirect link between both kinases that could result in synergistic anti-cancer activity. Both kinases are
validated targets for breast cancer, and developing dual inhibitors with balanced activity against both serves to
unveil a novel treatment paradigm for breast cancer patients. Preliminary data has identified compounds with
potent activity against CSF-1R, Aurora B, and c-Kit kinases. The proposed work aims to develop compounds
optimized to have selectivity for CSF-1R and Aurora B over c-Kit.
 The postdoctoral research direction is focused on continuing to develop lead compounds through in
vivo efficacy studies. In line with this work, cell based assays will be utilized to study the biological interplay of
dual CSF-1R and Aurora B inhibition. Additionally, new projects will be pursued to develop additional skills in
cancer biology and immunotherapy. The work described in this proposal highlights the steps for technical and
career skill development I plan to take to achieve my goal of becoming an academic independent investigator
and helping cancer patients in need.

## Key facts

- **NIH application ID:** 10004578
- **Project number:** 5K00CA212480-05
- **Recipient organization:** UNIVERSITY OF CALIFORNIA, SAN FRANCISCO
- **Principal Investigator:** Nicholas Matthew McConnell
- **Activity code:** K00 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $78,427
- **Award type:** 5
- **Project period:** 2018-09-01 → 2021-01-11

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10004578

## Citation

> US National Institutes of Health, RePORTER application 10004578, Identification of Dual CSF-1R/Aurora B Kinase Inhibitors as a Novel Breast Cancer Treatment Paradigm (5K00CA212480-05). Retrieved via AI Analytics 2026-05-26 from https://api.ai-analytics.org/grant/nih/10004578. Licensed CC0.

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