The Ohio State University

The University of Oklahoma

John C Hackett

Robert Brueggemeier

Young-Woo Kim

Pui-Kai Li

J Thomas Pento

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.

Growing community of inventors

Dublin, OH, United States of America

John C Hackett