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A series of novel amide-linked 18β-glycyrrhetinic acid derivatives were developed by incorporating substituted piperazine amide fragments into the C30–COOH of 18β-glycyrrhetinic acid scaffold. The synthesized compounds were evaluated for their anticancer activity against Karpas299, A549, HepG2, MCF-7, and PC-3 cell lines by MTT assay. Besides, some compounds with electron-withdrawing groups on phenyl moieties exhibited noticeable antiproliferative activity. The most potent compound 4a was also found to be non-toxic to normal human hepatocytes LO2 cells. The compound 4a exhibited moderate inhibitory activity against wild-type ALK with an IC50 value of 203.56 nM and relatively weak potent activity to c-Met (IC50 > 1000 nM). Molecular docking studies were performed to explore the diversification in bonding patterns between the compound 4a and Crizotinib.

Objective: Diffusion tensor imaging (DTI) was used to analyze the changes of white matter fiber FA in patients with schizophrenia of different ages and genders, and to explore the reference of clinical imaging. Methods: Retrospective analysis of the clinical diagnosis of schizophrenia patients and healthy subjects in all 50 cases, were given routine examination of brain MRI parallel diffusion tensor imaging, comparison of different age and gender in different parts of the brain white matter changes of FA value. Results : (1) the FA values of white matter in different age groups were different between the patients and the normal group ( P < 0.05). The normal group right superior frontal gyrus, left parietal lobe and left anterior cingulate gyrus of the cerebral white matter fiber FA value increased gradually before the age of 30, at the age of 30 and reached the peak gradually decreased after 30 years old. The left frontal gyrus and corpus callosum in patients with group pressure (after) of cerebral white matter fiber FA value increased gradually before the age of 30, at the age of 30 and reached the peak gradually decreased after 30 years old. (2) the FA values of white matter in different parts of male and female patients were different (P < 0.05). The white matter fiber FA in the left anterior capsule of the normal group was higher in males than in females. The FA value of bilateral occipital white matter in male patients was lower than that in female; the FA values of the central white matter in the left and right sides of the brain stem were higher in males than in females. Conclusion : the changes of FA value in the white matter of some parts of the brain in the normal group and the patient group are influenced by age and sex.