Bart I Roman
Affiliation: Ghent University
Verhasselt S, Roman B, De Wever O, Van Hecke K, Van Deun R, Bracke M, et al
. Discovery of (S)-3'-hydroxyblebbistatin and (S)-3'-aminoblebbistatin: polar myosin II inhibitors with superior research tool properties. Org Biomol Chem. 2017;15:2104-2118 pubmed publisher
..These molecules furthermore do not cause interference in (fluorescence) readouts. (S)-2 and (S)-3 thus are superior alternatives to (S)-blebbistatin as research tools to study myosin II. ..
Roman B. Essay: Avoiding unfounded health claims on small molecules in scientific literature. Bioorg Chem. 2019;86:273-276 pubmed publisher
..We therefore also introduce the idea of biological filters, a pattern recognition method to triage enigmatic compounds into valuable hits and false positives, based on the entirety of their biological effects in cell-based systems. ..
Roman B, De Ryck T, Verhasselt S, Bracke M, Stevens C. Further studies on anti-invasive chemotypes: An excursion from chalcones to curcuminoids. Bioorg Med Chem Lett. 2015;25:1021-5 pubmed publisher
..In the 1,3-diarylpenta-2,4-dien-1-one series, fluoro and/or trimethoxy substitution caused an increase in potency. This agrees with observations made earlier for the chalcone class. ..
Roman B, De Ryck T, Patronov A, Slavov S, Vanhoecke B, Katritzky A, et al
. 4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model. Eur J Med Chem. 2015;101:627-39 pubmed publisher
..Although the molecular mechanism(s) by which these substances mediate efficacy remain(s) unrevealed, we were able to eliminate the major targets commonly associated with antineoplastic chalcones. ..
Roman B, Verhasselt S, Mangodt C, De Wever O, Stevens C. Synthesis of C-ring-modified blebbistatin derivatives and evaluation of their myosin II ATPase inhibitory potency. Bioorg Med Chem Lett. 2018;28:2261-2264 pubmed publisher
..This and earlier reports suggest that rational design of potent myosin II inhibitors based on the architecture of the blebbistatin binding pocket is an ineffective strategy. ..
Verhasselt S, Roman B, Bracke M, Stevens C. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur J Med Chem. 2017;136:85-103 pubmed publisher
..Finally, all new and known D-ring modified (S)-blebbistatin analogs were compared and the most potent ones underwent a screening of their physicochemical properties. ..
Verhasselt S, Stevens C, Van den Broecke T, Bracke M, Roman B. Insights into the myosin II inhibitory potency of A-ring-modified (S)-blebbistatin analogs. Bioorg Med Chem Lett. 2017;27:2986-2989 pubmed publisher
..Our results indicate there are few possibilities for potency enhancement via ring A modification of the blebbistatin scaffold. ..