The Ohio State University

Institute of Molecular Genetics As Cr, V.v.i.

Werner Tjarks

Petr Bartunek

David Sedlak

Rolf F Barth

Abul K Anisuzzaman

Albert H Soloway

Iwona M Wyzlic

Fazlul Alam

Feng-Guang Rong

Disclosed herein are compounds comprising dicarba-closo-dodecaborane. The compounds can be, for example, estrogen receptor beta (ER&#x3b2;) agonists. In some examples, the compounds can be selective ER&#x3b2; agonists. Also provided herein are methods of treating, preventing, or ameliorating cancer in a subject, suppressing tumor growth in a subject, treating an inflammatory disease in a subject, treating a neurodegenerative disease in a subject, treating a psychotropic disorder in a subject, or a combination thereof, by administering to a subject a therapeutically effective amount of one or more of the compounds or compositions described herein, or a pharmaceutically acceptable salt thereof.

Carborane compounds and methods of use thereof

Disclosed herein are compounds comprising dicarba-closo-dodecaborane. The compounds can be, for example, estrogen receptor beta (ER&#x3b2;) agonists. In some examples, the compounds can be selective ER&#x3b2; agonists. Also provided herein are methods of treating, preventing, or ameliorating cancer in a subject, suppressing tumor growth in a subject, treating an inflammatory disease in a subject, treating a neurodegenerative disease in a subject, treating a psychotropic disorder in a subject, or a combination thereof by administering to a subject a therapeutically effective amount of one or more of the compounds or compositions described herein, or a pharmaceutically acceptable salt thereof.

The invention relates to novel boron-containing nucleosides and amino acids which can utilize the enzymatic systems in tumor cells for incorporating such boron-containing structures into nucleic acids and proteins. Subsequent use of boron neutron capture therapy provides a method for treating tumor cells.

Carboranyl uridines and their use in boron neutron capture therapy

There is disclosed a process for preparing carboranyl uridine nucleoside compounds and their diethyl ether adducts, which exhibit a tenfold increase in boron content over prior art boron containing nucleoside compounds. Said carboranyl uridine nucleoside compounds exhibit enhanced lipophilicity and hydrophilic properties adequate to enable solvation in aqueous media for subsequent incorporation of said compounds in methods for boron neutron capture therapy in mammalian tumor cells.

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Columbus, OH, United States of America

Werner Tjarks