Chaenomeles sinensis has been used as a food and traditional medicines. However, most of research on discovering bioactive constituents from this plant have been focused on its yellow fruit, Chinese quince, due to its wide usage. Here, we isolated and characterized three new phenolic compounds (1, 9, and 11) and 21 known compounds (2−8, 10, and 12−24) from the twigs of C. sinensis. Their chemical structures were established by spectroscopic and spectrometric data analysis including 1D and 2D NMR, high-resolution mass spectrometry (HRMS), electronic circular dichroism (ECD), and LC-MS analysis. Some of the isolated compounds (1−24) showed anti-neuroinflammatory effects on nitric oxide (NO) production in lipopolysaccharide (LPS)-activated BV-2 cells, neurotrophic activity in C6 cells through the secretion of nerve growth factor (NGF) and/or cytotoxicity against four human cancer cell lines (A549, SK-OV-3, SK-MEL-2, MKN-1).