Combined ASL and DTI metrics of enhanced lesion and related edema are valuable noninvasive tools in differentiating residual/recurrent gliomas from postradiation changes.

Class I histone deacetylases (HDACs) are key regulators of cell proliferation and they are frequently dysregulated in cancer cells. We report here the synthesis of a novel series of class-I selective HDAC inhibitors (HDACi) containing a 2-aminobenzamide moiety as a zinc-binding group connected with a central (piperazin-1-yl)pyrazine or (piperazin-1-yl)pyrimidine moiety. Some of the compounds were additionally substituted with an aromatic capping group. Compounds were tested in vitro against human HDAC1, 2, 3, and 8 enzymes and compared to reference class I HDACi (Entinostat (MS-275), Mocetinostat, CI994 and RGFP-966). The most promising compounds were found to be highly selective against HDAC1, 2 and 3 over the remaining HDAC subtypes from other classes. Molecular docking studies and MD simulations were performed to rationalize the in vitro data and to deduce a complete structure activity relationship (SAR) analysis of this novel series of class-I HDACi. The most potent compounds, including 19f, which blocks HDAC1, HDAC2, and HDAC3, as well as the selective HDAC1/HDAC2 inhibitors 21a and 29b, were selected for further cellular testing against human acute myeloid leukemia (AML) and erythroleukemic cancer (HEL) cells, taking into consideration their low toxicity against human embryonic HEK293 cells. We found that 19f is superior to the clinically tested class-I HDACi Entinostat (MS-275). Thus, 19f is a new and specific HDACi with the potential to eliminate blood cancer cells of various origins.

The aim of this review was to review the basic background, technique, and clinical applications of arterial spin labeling in brain tumors. Arterial spin labeling is used for differentiation of brain tumors from nonneoplastic lesions such as infarction and infection. It has a role in the grading of gliomas and in the differentiation of gliomas from lymphomas and metastasis. It is used for detection of the best biopsy site and prediction of treatment response. Arterial spin labeling is used for the assessment of extra-axial tumors and pediatric tumors. Last, it has a role in the differentiation of tumor recurrence from postradiation changes and in monitoring patients after therapy.

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