Research Progress on Structure-Activity Relationship of 1,8-Naphthalimide DNA Chimeras Against Tumor.

The development of 1,8-naphthalimide derivatives as cell probes, DNA targeting agents, and anti-tumor drugs is one of the research hotspots in the field of medicine. Naphthalimide compounds are a kind of DNA embedder, which can change the topological structure of DNA by embedding in the middle of DNA base pairs, and then affect the recognition and action of topoisomerase on DNA. Aminofide and mitonafide are the first 2 drugs to undergo clinical trials. They have good DNA insertion ability, can embed DNA double-stranded structure, and induce topoisomerase II to cut part of pBR322DNA, but not yet entered the market due to their toxicity. In this paper, the design and structure-activity relationship of mononaphthalimide and bisaphthalimide compounds were studied, and the relationship between the structure of naphthalimide and anti-tumor activity was analyzed and discussed. It was found that a variety of structural modifications were significant in improving anti-tumor activity and reducing toxicity.

Development and validation of a risk score for predicting mortality after resection of primary hepatocellular carcinoma.

BACKGROUND: Primary hepatocellular carcinoma (PHCC) has a poor prognosis and high short-term mortality rate, even after resection. Thus, early diagnosis in PHCC cases can help improve quality of life via personalized management strategies. RESULTS: The risk score system (RSS) were classified as low risk (<5 points), medium risk (5-10 points), or high risk (>10 points). The areas under the receiver operating characteristic curves were 0.80 in the training cohort and 0.69 in the validation cohort, which indicated satisfactory prognostic performance. The Hosmer-Lemeshow goodness of fit test (P>0.05) revealed consistent performance in both groups. The concordance index (C-index: 0.663, 95% CI: 0.618-0.708) revealed excellent discrimination and good calibration in the validation cohort. CONCLUSIONS: This simple RSS, which is based on clinical and laboratory data from patients undergoing resection of PHCC, might allow clinicians and medical staff to better manage PHCC. MATERIALS AND METHODS: A total of 672 PHCC cases were retrospectively obtained from the First Affiliated Hospital of Wenzhou Medical University between January 2007 and February 2015. Cox proportional hazard models were used to identify independent predictors of mortality. Kaplan-Meier curves and the log-rank test were used to examine the relationships between the prognostic factors and overall mortality.