Jacek Chrzanowski
A5012888029- Immune cells in cancer
- Cancer Research and Treatments
- Adenosine and Purinergic Signaling
- Receptor Mechanisms and Signaling
- Neutrophil, Myeloperoxidase and Oxidative Mechanisms
- Organophosphorus compounds synthesis
- Asymmetric Hydrogenation and Catalysis
- X-ray Diffraction in Crystallography
- Asymmetric Synthesis and Catalysis
- Crystallization and Solubility Studies
- Monoclonal and Polyclonal Antibodies Research
- Amino Acid Enzymes and Metabolism
- Nanoplatforms for cancer theranostics
- Phosphorus compounds and reactions
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Cancer-related gene regulation
- Click Chemistry and Applications
- Inflammatory mediators and NSAID effects
- Cell Adhesion Molecules Research
- Advanced Synthetic Organic Chemistry
- S100 Proteins and Annexins
- Chemical Synthesis and Reactions
- Chalcogenide Semiconductor Thin Films
- Synthetic Organic Chemistry Methods
- Organic Chemistry Cycloaddition Reactions
Centrum Badań Molekularnych i Makromolekularnych Polskiej Akademii Nauk
2015-2025
Polish Academy of Sciences
2014-2025
Pharmacologic inhibition of the controlling immunity pathway enzymes arginases 1 and 2 (ARG1 ARG2) is a promising strategy for cancer immunotherapy. Here, we report discovery development OATD-02, an orally bioavailable, potent inhibitor. The unique pharmacologic properties OATD-02 are evidenced by targeting intracellular ARG1 ARG2, as well long drug-target residence time, moderate to high volume distribution, low clearance, which may jointly provide weapon against arginase-related tumor...
In order to expand the group of chiral thiourea structures, several optically active thioureas derived from (S)-1-(2-pyridyl)ethylamine enantiomer were prepared via its reaction with achiral or isothiocyanates. To show their synthetic potential as auxiliaries isolated tested an organocatalyst in asymmetric version selected aldol condensation and addition diethylzinc benzaldehyde. The observation induction these model reactions encourages further research on use this versions multicomponent...
Abstract The synthetic approaches for the preparation of non‐racemic tertiary phosphine oxides with particular attention to latest advances are discussed in this minireview.
A series of enantiomerically enriched tertiary phosphine oxides have been prepared via the Pd‐catalyzed cross‐coupling reactions pure tert ‐butylphenylphosphine oxide, with a variety aryl iodides and bromides. This new protocol under optimized reaction conditions [toluene, 110 0 C, Pd(PPh 3 ) 4 , K 2 CO (or Et N)] afforded highly functionalized P‐chiral yield 78% to 95% enantiomeric excesses above 98%. The stereoretentive outcome was proved by X‐ray crystallography selected oxides: ( S...
Abstract Simple, efficient, clean, and stereospecific protocols of protection phosphorus atom with borane deprotection from the complexes tertiary phosphines in mild conditions are reported. The proposed protection/deprotection reactions tolerate a range functional groups lead to pure products excellent yield no need for application chromatographic or crystallisation purification procedures. For first time mechanisms phosphine have been studied based on experimental kinetic data as well...
GRAPHICAL ABSTRACT
GRAPHICAL ABSTRACT Selected heterocycles with a stereogenic sulfur or phosphorus atom based on phenol residue containing chiral auxiliaryAll authorsJacek Chrzanowski, Dorota Krasowska, Aleksandra Jasiak & Jozef Drabowiczhttps://doi.org/10.1080/10426507.2017.1295048Published online:25 May 2017
This review presents synthetic procedures applied to the preparation of chiral (mainly optically active) hypervalent chalcogenuranes. The stereoisomerization mechanisms derivatives sulfur, selenium and tellurium their selected interconversions are also presented. Keywords: Hypervalency, chirality, sulfurane, selenurane, tellurane, Berry pseudorotation, turnstile rotation.
<p>Simulated human plasma concentration time profiles of OATD-02</p>
<p>PK and PD effects after intravenous administration of OATD-02 CB-1158 in Sprague-Dawley rats</p>
<p>The immunosuppressive character of ARG1 and ARG2 in the tumor microenvironment (TME)</p>
<p>Simulated human plasma concentration time profiles of OATD-02</p>
<p>Supplementary Figures 2 - 14 (Synthesis schemes).</p>
<p>Supplementary Materials and Methods not included in the main manuscript</p>
<p>Allometric scaling of human volume distribution (V-SAfu)</p>
<p>Analysis of B16F10 tumor growth in mice treated with OATD-02 all individuals subjected to the study.</p>
<p>Individual body weight changes in animals treated with OATD-02</p>
<p>Crystal structure of OATD-02 bound to hARG1</p>
<div>Abstract<p>Pharmacological inhibition of the controlling immunity pathway enzymes arginases 1 and 2 (ARG1 ARG2) is a promising strategy for cancer immunotherapy. Here, we report discovery development OATD-02, an orally bioavailable, potent inhibitor. The unique pharmacological properties OATD-02 are evidenced by targeting intracellular ARG1 ARG2, as well long drug-target residence time, moderate to high volume distribution, low clearance which may jointly provide weapon...
<p>Supplementary Materials and Methods not included in the main manuscript</p>