The Ohio State University

Other

The University of Oklahoma

Robert Brueggemeier

Young-Woo Kim

John C Hackett

Pui-Kai Li

Chenglong Li

Harold E Fisk

Yasuro Sugimoto

Edgar S Diaz-Cruz

Serena Landini

J Thomas Pento

Bin Su

Disclosed herein are novel compounds that are Mps1/TTK inhibitors. Also disclosed are compositions comprising the compounds and methods of using the compounds in treating various diseases.

Pyrrolopyrimidine derivatives as Mps1/TTK kinase inhibitors

Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO, and S(CH), wherein n=1-10; Rand Rmay be the same or different and are selected from H, OH, OCH, OCHCH, OCHCH, NH, NHCH, N(CH), CH, CHCH, CHCHCH, CH(CH), C(CH), NO, F, Cl, Br, CF, SH, SCH, SCHCH, OCOCH, OCOC(CH), OCOCHCOOH, and CN; and Ris a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.

Heteroaryl-containing isoflavones as aromatase inhibitors

Compounds and methods for treating, inhibiting, or delaying the onset of cancer in a subject by administering a therapeutically effective amount of a keratinocyte growth factor receptor tyrosine kinase (KGFR TK) inhibitor to the subject in need of such treatment. Also provided are compounds and methods for the treating, inhibiting, or delaying the onset of metastasis in a subject with cancer by administering a therapeutically effective amount of a KGFR TK inhibitor to the subject in need of such treatment.

Keratinocyte growth factor receptor&#x2014;tyrosine specific inhibitors for the prevention of cancer metastatis

The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient conditions. This invention further provides a method of synthesis of the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one from a 2-(alkylthio)isoflavone. The invention further provides methods of using the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of breast cancer in mammals.

2-heterosubstituted 3-aryl-4H-1-benzopyran-4-ones as novel therapeutics in breast cancer

Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: wherein Rmay be alkyl, cycloalkyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; Ris H, alkyl, aryl, alkylaryl, arylalkyl, and cycloalkyl; R, with the base nitrogen, forms an amide or sulfonamide; Ris selected from nitro, amine, amide, and benzamide; or a pharmaceutically acceptable salts thereof. Also provided are small molecule selective aromatase inhibitors having a molecular weight of less 500 g/mol. In some embodiments, the small molecule selective aromatase inhibitors described herein have a molecular weight of less than 450 g/mol. Also provided are methods for suppressing aromatase activity expression in cancer cells comprising the step of administering a pharmaceutically effective amount of a small molecule aromatase inhibitor to a subject in need of such treatment. In one embodiment, the cancer cells are breast cancer cells.

Sulfonanilide analogs as selective aromatase modulators (SAMs)

2-Heterosubstituted 3-aryl-4H-1-benzopyran-4-ones as novel therapeutics in breast cancer

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Dublin, OH, United States of America

Robert Brueggemeier