Alkoxyurea-based benzoic methyl esters and amides as key intermediates for selective HDAC6 inhibitors
A set of synthetic intermediates—alkoxyurea-based benzoic methyl esters and amides—developed as part of a rational medicinal chemistry program to create novel analogs of the HDAC6-selective inhibitor Nexturastat A with improved antiproliferative properties. Useful as building blocks for selective epigenetic drug discovery and HDAC6-targeted therapeutics.
Overview
This offering comprises a focused library of alkoxyurea-based benzoic methyl esters and amides designed as key synthetic intermediates toward novel analogs of Nexturastat A, a well-known selective inhibitor of histone deacetylase 6 (HDAC6). The compounds were prepared as part of a rational medicinal chemistry effort aimed at producing next-generation HDAC6 inhibitors with superior antiproliferative activity compared to the parent molecule. The intermediates are intended for partners interested in selective epigenetic modulation, with potential relevance to oncology, neurodegeneration, and inflammation research where HDAC6 plays a regulatory role.
Technical specifications
Key features:
- A defined set of alkoxyurea-based benzoic methyl ester and amide intermediates
- Designed around the pharmacophore of Nexturastat A, a known selective HDAC6 inhibitor
- Suitable as building blocks for further SAR (structure–activity relationship) exploration of selective HDAC6 inhibitors
- Synthetic route established at Heinrich Heine Universität Düsseldorf under the supervision of Thomas Kurz
- Applicable to medicinal chemistry programs targeting selective epigenetic regulators
Potential applications:
- Lead optimization of HDAC6-selective inhibitors
- Foundation for novel antiproliferative and anti-cancer agent development
- Starting point for analogs with improved selectivity or potency profiles
Technology readiness level
The compounds have been synthesized as part of an ongoing medicinal chemistry research program. They are at an early stage of development as discrete intermediates, with further biological validation and analog optimization expected to follow. The chemistry route has been established, positioning the intermediates for use in subsequent drug discovery campaigns and collaborative optimization efforts.
About Heinrich Heine Universität Düsseldorf
Heinrich Heine Universität Düsseldorf is a comprehensive public research university anchored by a major medical faculty and a modern science campus. An integrated university hospital and shared core facilities enable clinical translation and access to specialized instrumentation for joint studies. Companies collaborate through on‑campus spaces, contract research, and tailored partnership models, with quick reach to suppliers and manufacturing across North Rhine‑Westphalia’s Rhine‑Ruhr corridor. Research is supported by competitive funding from the German Research Foundation and federal and state ministries, alongside European Union programs. A dedicated technology transfer office manages IP, licensing, and startup support to accelerate industry uptake.
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