1334660-40-0Relevant academic research and scientific papers
Identification of novel matrix metalloproteinase inhibitors by screening of phenol fragments library
Rubino, Maria Teresa,Maggi, Dariana,Laghezza, Antonio,Loiodice, Fulvio,Tortorella, Paolo
, p. 557 - 563 (2011)
In the last 20 years, a great variety of synthetic, low molecular weight MMP inhibitors (MMPIs) have been synthesized and tested, although none has reached clinical utility. Exploration of novel ZBGs and development of non-hydroxamate MMPI has become a focus in current research. It's well-known that polyphenols can produce beneficial effects on human health by their antioxidant properties as well as they have the ability to block gelatinase activity. In this work we tested a series of selected phenols as MMP inhibitors. The most interesting hit (B6) shows sub-micromolar activity against MMP-2 (IC50 0.59 ± 0.05 μM, LE = 1.07) and a fairly good selectivity spectrum. A screening of selected phenols against four matrix metalloproteinases is reported. Eight phenols showed a very interesting activity and selective profile. The most interesting hit (B6) presents a sub-micromolar activity against MMP-2 (IC50 0.59±0.05μM). Copyright
Synthesis and evaluation of C-ring aromatized analogues of phenanthridone alkaloids
Lee, Seokwoo,Hwang, Soonho,Yu, Shuai,Jang, Wonyoung,Lee, Yun Mi,Kim, Sanghee
, p. 1065 - 1070 (2012/07/14)
Phenanthridone alkaloids are envisaged as an attractive lead for the development of anticancer agents. We have prepared a series of aromatized analogues on the basis of the structure of this class of alkaloids with the hope of finding the simplified compounds with comparable activities. The obtained analogues were evaluated for their cytotoxic effect against several cancer cell lines and found to be virtually inactive. These observations together with molecular modeling studies strongly suggest that the stereochemistries of hydroxyl groups in C-ring of phenanthridone alkaloids are crucial to biological effects.
