31061-79-7Relevant articles and documents
Oxadiazole based Os(IV) compounds as potential DNA intercalator and cytotoxic agents
Bhatt, Bhupesh S.,Patel, Mohan N.,Pathak, Chandramani,Pursuwani, Bharat H.,Vaidya, Foram U.
, (2020/07/10)
Os(IV) compounds and ligands have been synthesized and well characterized. DNA cleavage tendency of compounds has been evaluated using gel electrophoresis and binding behavior has been evaluated by viscosity measurements, absorption titration, fluorescenc
2,5-Diaryloxadiazoles and their precursors as novel inhibitors of cathepsins B, H and L
Garg, Shweta,Raghav, Neera
, p. 64 - 74 (2016/07/06)
High levels of cathepsins indicated in various pathological conditions like arthritis, cancer progressions, and atherosclerosis explains the need to explore potential inhibitors of these proteases which can be of great therapeutic significance. We, in the present work, report the synthesis of some 2,5-diaryloxadiazoles from N-subsitutedbenzylidenebenzohydrazides. The synthesized compounds were screened for their inhibitory potential on cathepsins B, H and L. Structure Activity Relationship studies show that 2,5-diaryloxadiazoles were less inhibitory than their precursors. 1i and 2k have been found to be most inhibitory to cathepsins B and L. Their Ki values have been calculated as 11.38 × 10-8 M and 66.4 × 10-8 M for cathepsin B and 4.2 × 10-9 M and 47.31 × 10-9 M for cathepsin L, respectively. However, cathepsin H activity was maximally inhibited by compounds, 1e and 2c with Ki values of 4.4 × 10-7 M and 5.6 × 10-7 M, respectively. Enzyme kinetic studies suggest that these compounds are competitive inhibitors to the enzymes. The results have been compared with docking results obtained using iGemDock.
Training a Constitutional Dynamic Network for Effector Recognition: Storage, Recall, and Erasing of Information
Holub, Jan,Vantomme, Ghislaine,Lehn, Jean-Marie
supporting information, p. 11783 - 11791 (2016/10/07)
Constitutional dynamic libraries (CDLs) of hydrazones, acylhydrazones, and imines undergo reorganization and adaptation in response to chemical effectors (herein metal cations) via component exchange and selection. Such CDLs can be subjected to training by exposition to given effectors and keep memory of the information stored by interaction with a specific metal ion. The long-term storage of the acquired information into the set of constituents of the system allows for fast recognition on subsequent contacts with the same effector(s). Dynamic networks of constituents were designed to adapt orthogonally to different metal cations by up- and down-regulation of specific constituents in the final distribution. The memory may be erased by component exchange between the constituents so as to regenerate the initial (statistical) distribution. The libraries described represent constitutional dynamic systems capable of acting as information storage molecular devices, in which the presence of components linked by reversible covalent bonds in slow exchange and bearing adequate coordination sites allows for the adaptation to different metal ions by constitutional variation. The system thus performs information storage, recall, and erase processes.
