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Poor aqueous solubility is one of the recurrent drawbacks of many compounds in medicinal chemistry. To overcome this limitation, the dilution of drug candidates from stock solutions of an organic solvent is common practice. However, the precise characterisation of these compounds in aqueous solutions is often neglected, leading to some uncertainties regarding the nature of the actual active species. In this communication, we demonstrate that two ruthenium complexes previously reported by our group for their chemotherapeutic potential against cancer, namely [Ru(DIP)2(sq)](PF6) and [Ru(DIP)2(3-methoxysq)](PF6), where DIP is 4,7-diphenyl-1,10-phenanthroline, sq=semiquinonate and 3-methoxysq=3-methoxysemiquinonate, form colloids in water-DMSO (1 % v/v) mixtures that are invisible to the naked eyes. [Ru(DIP)2(3-methoxysq)](PF6) was found to form a highly stable and monodispersed colloid with nanoaggregates of ∼25 nm. In contrast, [Ru(DIP)2(sq)](PF6) was found to form large reticulates of mostly spherical aggregates which size was found to increase over time. The difference in size and shape distribution of drug candidates is of tremendous significance as the study of their biological activity might be severely affected. Overall, we strongly believe that these observations should be taken into account by the scientific community working on the development of metal-based drugs with poor water solubility. 相似文献
74.
Fermanelli Carla S. Galarza Emilce D. Pierella Liliana B. Renzini María S. Saux Clara 《Topics in Catalysis》2019,62(12-16):918-930
Topics in Catalysis - In this work, a simple thermal-catalytic system was used to valorize peanut shells (Arachis hypogaea), the residual biomass from the peanut industry. To accomplish this... 相似文献
75.
Gomes A. C. S. A. Costa L. C. Brito D. C. Frana R. J. Marques Mnica R. C. 《Polymer Bulletin》2020,77(4):1969-1981
Polymer Bulletin - In this study, we synthesized a new ion-imprinted polymer (IIP) based on introduction of amidoxime groups in acrylonitrile, complexation with Cd2+ ions and polymerization with... 相似文献
76.
Michael A. Clegg Prof. Nicholas C. O. Tomkinson Dr. Rab K. Prinjha Dr. Philip G. Humphreys 《ChemMedChem》2019,14(4):362-385
The bromodomain and extra terminal (BET) family of bromodomain-containing proteins (BCPs) have been the subject of extensive research over the past decade, resulting in a plethora of high-quality chemical probes for their tandem bromodomains. In turn, these chemical probes have helped reveal the profound biological role of the BET bromodomains and their role in disease, ultimately leading to a number of molecules in active clinical development. However, the BET subfamily represents just 8/61 of the known human bromodomains, and attention has now expanded to the biological role of the remaining 53 non-BET bromodomains. Rapid growth of this research area has been accompanied by a greater understanding of the requirements for an effective bromodomain chemical probe and has led to a number of new non-BET bromodomain chemical probes being developed. Advances since December 2015 are discussed, highlighting the strengths/caveats of each molecule, and the value they add toward validating the non-BET bromodomains as tractable therapeutic targets. 相似文献
77.
Science China Technological Sciences - Accurate modelling of lithium ion batteries is crucial for battery management in electric vehicles. Recent studies have revealed the fractional order nature... 相似文献
78.
Bankov S. E. Vesnik M. V. Kravchenko V. F. 《Journal of Communications Technology and Electronics》2020,65(4):398-405
Journal of Communications Technology and Electronics - Abstract—The article presents a rigorous numerical solution, using the Wiener–Hopf method, to the problem of plane wave... 相似文献
79.
Wireless Personal Communications - The rapid development of Information and Communication Technology and the growing number of devices connected to the Internet make the Internet of Things (IoT) as... 相似文献
80.