Design, synthesis and antitumor activities of phthalazinone derivatives as PARP-1 inhibitors and PARP-1/HDAC-1 inhibitors.

In recent years, poly(ADP-ribose)polymerase-1 (PARP-1) and histone deacetylase (HDAC) have emerged as significant targets in tumor therapy, garnering widespread attention. In this study, we designed and synthesized two novel phthalazinone PARP-1 inhibitors and dual PARP-1/HDAC-1 inhibitors, named DLC-1-46 containing dithiocarboxylate fragments and DLC-47-63 containing hydroxamic acid fragments, and evaluated their inhibitory activities on enzymes and cells. Among the PARP-1 inhibitors, most compounds exhibited high inhibitory activity against the PARP-1 enzyme, with DLC-1-6 being particularly notable, showing IC values <0.

Spatial Differences of Ecological Well-Being Performance in the Poyang Lake Area at the Local Level.

Maintaining low ecological consumption and high well-being while making economic progress and thus achieving sustainable development is a significant issue facing the world today. Ecological well-being performance (EWP) is one indicator that tracks this progress. Although EWP has been typically assessed at the national, provincial and urban levels, investigations into EWP units in the Great Lakes region are lacking.

Research on Spatial Differences and Driving Effects of Ecological Well-Being Performance in China.

The essential requirement of sustainable development is to maximize economic prosperity and well-being while remaining within natural boundaries. This study focused on three aspects. First, a unique ecological well-being performance (EWP) evaluation model was developed by combining subjective and objective well-being indicators to assess China's EWP from 2006 to 2018.