# New Methods and Strategies for the Scalable Synthesis of Complex Bioactive Molecules

> **NIH NIH R35** · UNIVERSITY OF TEXAS DALLAS · 2024 · $390,000

## Abstract

Abstract
To enable reliable access to meaningful quantities of bioactive natural and unnatural compounds with
higher complexity, it is vital to devise new synthesis logics and develop new chemical transformations.
In this context, we propose to investigate the highly coveted is the rapid assembly of polycyclic
frameworks adorned with several chiral centers. Our explorations focus on the synthesis and study of
complex natural products and their fully synthetic analogues with potentials for the treatment of cancer,
neurological disorders, and infectious diseases. The terpenes and alkaloids we identified as targets are
promising lead compounds for the development of new medicines, but their unknown or unclear
mechanism of actions and the lack of a dependable way to access them has severely hindered their
therapeutical development. We aim to solve this issue while also expanding and innovating the toolbox
available to medicinal and synthetic chemists. In fact, these molecules are not only important from a
biological standpoint, but they also represent state-of-the-art challenges for complex molecule
synthesis. Thus, these total synthesis efforts stimulate the invention of new chemicals methods and
serve as a proving ground for our new logics and existing transformations to solve critical synthesis
problems in complex settings. The expected outcome of the proposed research is a) the development
of new catalytic stereoselective methods that generate densely substituted polycyclic building blocks
for synthesis, b) the design of new synthesis logics that will facilitate the preparation of complex
functional molecules for which there are currently no efficient synthesis roadmaps, c) reliable access to
the chosen target molecules enabling their use as biological probes or as lead compounds for drug
discovery, d) a collection of medicinally relevant synthetic analogues for in-depth biological evaluations.

## Key facts

- **NIH application ID:** 10936422
- **Project number:** 1R35GM154682-01
- **Recipient organization:** UNIVERSITY OF TEXAS DALLAS
- **Principal Investigator:** Filippo Romiti
- **Activity code:** R35 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2024
- **Award amount:** $390,000
- **Award type:** 1
- **Project period:** 2024-08-01 → 2029-05-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10936422

## Citation

> US National Institutes of Health, RePORTER application 10936422, New Methods and Strategies for the Scalable Synthesis of Complex Bioactive Molecules (1R35GM154682-01). Retrieved via AI Analytics 2026-05-26 from https://api.ai-analytics.org/grant/nih/10936422. Licensed CC0.

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