67980-67-0Relevant academic research and scientific papers
Design, synthesis and molecular modeling study of iminodiacetyl monohydroxamic acid derivatives as MMP inhibitors
Amelia Santos,Marques, Sergio M.,Tuccinardi, Tiziano,Carelli, Paolo,Panelli, Laura,Rossello, Armando
, p. 7539 - 7550 (2006)
As the matrix metalloproteinases (MMPs) can be massively up-regulated in degenerative tissues and degrade the extracellular matrix, these key enzymes are promising targets for the therapy of cancer and other degenerative diseases. Here, we are presenting a series of new non-peptidic hydroxamate-based matrix metalloproteinase inhibitors, MMPIs, incorporating the iminodiacetic (IDA) hydroxamic acid scaffold, as mimics of truncated peptidic MMPIs. A series of alkylaryl and sulfonylaryl groups, on the IDA basic scaffold, was investigated with the aim of improving potency and selectivity against MMPs involved in degenerative diseases. The sulfonamide based IDA derivatives studied (compounds B1-B3) showed to be potent (nM range) against deep S1′ pocket MMPs enzymes (i.e., MMP-2).
Mass spectrum sensitivity enhanced isothiocyanate labeling reagent, and synthesis method and applications thereof
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Paragraph 0024; 0029; 0030; 0031, (2017/07/20)
The invention belongs to the technical field of organic micromolecular peptide markers, and specifically relates to a mass spectrum sensitivity enhanced isothiocyanate labeling reagent, and a synthesis method and applications thereof. The labeling reagent is 1-(3-isothiocyanopropyl)-4-phenyl piperazine. The synthesis method comprises the following steps: reacting 1,3-dibromopropane with KOH and N-phenyl piperazine to generate an intermediate namely 1-(3-bromopropyl)-phenyl piperazine; and then adding potassium thiocyanate, polyethylene glycol, and dichloromethane into the intermediate to carry out reactions to generate the target product namely 1-(3-isothiocyanopropyl)-4-phenyl piperazine. The provided isothiocyanate labeling reagent can rapidly, accurately, and sensitively label peptide compounds, is especially suitable for the separation and detection of trace micromolecular peptide compounds in a complicated system, and has a wide application prospect.
Substituted pyridazino[3,4-b][1,5] benzoxazepin-5(6H)ones as multidrug-resistance modulating agents
Ott, Ingo,Kircher, Brigitte,Heinisch, Gottfried,Matuszczak, Barbara
, p. 4627 - 4630 (2007/10/03)
Pyridazino[3,4-b][1,5]benzoxazepin-5(6H)ones substituted with propylene-linked basic side chains were synthesized and investigated for the ability to reverse multidrug resistance (MDR) at vincristine-pretreated HeLa-MDR1 cells. The substances were found t
