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Sci Rep ; 10(1): 4827, 2020 03 16.
Article in English | MEDLINE | ID: mdl-32179835

ABSTRACT

Owing to the involvement of cyclooxygenase-2 (COX-2) in carcinogenesis, COX-2-selective inhibitors are increasingly studied for their potential cytotoxic properties. Moreover, the incorporation of carboranes in structures of established anti-inflammatory drugs can improve the potency and metabolic stability of the inhibitors. Herein, we report the synthesis of carborane-containing derivatives of rofecoxib that display remarkable cytotoxic or cytostatic activity in the micromolar range with excellent selectivity for melanoma and colon cancer cell lines over normal cells. Furthermore, it was shown that the carborane-modified derivatives of rofecoxib showed different modes of action that were dependent on the cell type.


Subject(s)
Antineoplastic Agents , Boron Compounds/chemistry , Colonic Neoplasms/etiology , Colonic Neoplasms/pathology , Cyclooxygenase 2 Inhibitors/chemical synthesis , Cyclooxygenase 2 Inhibitors/pharmacology , Cyclooxygenase 2/physiology , Lactones/chemical synthesis , Lactones/pharmacology , Melanoma/etiology , Melanoma/pathology , Sulfones/chemical synthesis , Sulfones/pharmacology , Carcinogenesis/genetics , Cell Line, Tumor , Drug Design , Humans , Hydrophobic and Hydrophilic Interactions
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