TK
Thomas Kurz
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TK
Heinrich Heine Universität Düsseldorf

Methyl ester derivatives of cinnamic acid as key intermediates for HDAC inhibitor synthesis

Specialized chemical intermediates (methyl ester derivatives of cinnamic acid) designed as precursors for novel alkoxyamide and alkoxyurea analogs of the HDAC inhibitor panobinostat. Supports research into antiproliferat...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

N-Hydroxyphthalimide and phthalimide precursors for novel DXR-targeting antibiotic development

Synthetic chemistry platform offering N-hydroxyphthalimide and phthalimide compounds as precursors to inhibitors of DXR (1-Deoxy-D-xylulose-5-phosphate reductoisomerase), a key enzyme in the bacterial non-mevalonate path...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Biarylic precursor compounds for novel cIAP inhibitor development

Specialized biarylic scaffold compounds designed as precursors for dual inhibitors of apoptosis proteins (cIAP). These intermediates enable the connection of two pharmacophores, supporting targeted research in apoptosis ...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Phthalimide-based precursors for fluorophore-drug conjugates

Novel substituted phthalimide compounds synthesized as precursors for fluorescent tags in fluorophore-drug conjugates. Leverages the known bright fluorescence of substituted phthalimides to enable development of theranos...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

4H-Chromen-4-one and quinazolin-4(3H)-one heterocycles as novel cap groups for HDAC inhibitor development

Synthesis and investigation of chromen-4-one and quinazolin-4(3H)-one heterocycles as cap groups for histone deacetylase (HDAC) inhibitors. These novel heterocyclic scaffolds aim to enhance selectivity and activity of HD...

TechnologyUniversity
TK
Heinrich Heine Universität Düsseldorf

Phthaloyl-based hydroxamic acid derivatives for HDAC inhibitor synthesis

Specialized hydroxamic acid intermediates featuring phthaloyl substitution at the para position of the aromatic ring, designed for the synthesis of histone deacetylase (HDAC) inhibitors used in pharmaceutical research an...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

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 i...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Hexadodecane Derivative Compounds Designed as HDAC11 Inhibitors

Novel small-molecule HDAC11 inhibitors designed as derivatives of the selective inhibitor SIS17, replacing the hydrazine moiety to improve selectivity and safety. Targets epigenetic regulation with potential applications...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Biarylic-ethyl-ester building blocks for selective Histone deacetylase inhibitor design

Early precursor compounds that enable the design of selective Histone deacetylase (HDAC) inhibitors by modifying the cap group. These biarylic ethyl ester building blocks offer a versatile chemical foundation for develop...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

5-Benzamido-pyrimidone/pyrimidine-2-methylcarboxylates monomeric building blocks for alpha-helix mimetics targeting HSP90

Monomeric building blocks that can be combined via peptide synthesis into dimeric or trimeric structures to mimic hot spot regions and amino acid side chains of HSP90, enabling inhibition of its dimerization process for ...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Chromene-2-carboxamide compounds as potential antimalarial agents

A chemistry-driven approach to designing novel chromene-2-carboxamide compounds with improved activity against Plasmodium falciparum, the parasite responsible for malaria. This research offers promising candidates for an...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Hydrazonamides, hydroxypropaneamidines and secondary alcohols as potential antimalarial agents

Chemistry-driven synthesis of hydrazonamide, hydroxypropaneamidine, and secondary alcohol compounds designed as potential antimalarial drug candidates. This medicinal chemistry research explores novel molecular scaffolds...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Flavonol-based inhibitors targeting acetohydroxyacid synthase in Mycobacterium tuberculosis

Computationally designed flavonol and 5-hydroxyflavonol compounds intended to inhibit acetohydroxyacid synthase (AHAS) in M. tuberculosis, leveraging cross-species herbicide activity as a starting point for novel antitub...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Isoxazole-5-carboxylic acid derivatives as precursors to HDAC6-selective inhibitors

Novel isoxazole-5-carboxylic acid scaffolds designed as metal-chelating precursors for selective histone deacetylase 6 (HDAC6) inhibitors. Targets epigenetic regulation by blocking deacetylation of acetylated histones, w...

TechnologyConceptualUniversity
TK
Heinrich Heine Universität Düsseldorf

Phosphonic acid derivatives as inhibitors of the non-mevalonate pathway

Designed analogs of the natural antibiotic fosmidomycin targeting DXR, a key rate-limiting enzyme in the non-mevalonate isoprenoid biosynthesis pathway. These phosphonic acid derivatives offer a promising approach to dev...

TechnologyConceptualUniversity
TK
Thomas Kurz
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General ChemistryMedicinal ChemistryOrganic ChemistryPharmaceutical Chemistry
Last updated Feb 2022
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