Synthesis of new indole-based bisphosphonates and evaluation of their chelating ability in PE/CA-PJ15 cells.

作者: Francesco Tartacca , Michela Mazzoni , Letizia Granieri , Laura Goracci , Angela Scrascia

DOI: 10.1016/J.EJMECH.2015.08.019

关键词:

摘要: Bisphosphonates are the most important class of antiresorptive agents used against osteoclast-mediated bone loss, and, more recently, in oncology. These compounds have high affinity for calcium ions (Ca(2+)) and therefore target mineral, where they appear to be internalized selectively by bone-resorbing osteoclasts inhibit osteoclast function. They extensively healthcare, however affected severe side effects; pharmacological properties bisphosphonates depend on their molecular structure, which is frequently cause poor intestinal adsorption low distribution. In this work we synthesized six novel bisphosphonate having a variably substituted indole moiety evaluate extra- intracellular chelating ability PE/CA-PJ15 cells. Preliminary silico vitro ADME studies were also performed results suggested that plays an role cell permeability metabolism properties.

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