University of Kentucky Research Foundation

University of Colorado

Bioventures, LLC

University of Rochester

University of Arkansas

Craig T Jordan

Peter Anthony Crooks

Xiaochen Wei

Venumadhav Janganati

Narsimha Reddy Penthala

Jessica Ponder

Shobanbabu Bommagani

Philip Reigan

Xin Lu

Jeffrey A Moscow

Christopher J Matheson

Donald S Backos

Monica Guzman

Maria L Amaya

Shanshan Pei

Shama Nasim

Steffanie L Furtek

The present disclosure relates to compounds of Formula (I): stereoisomers thereof, prodrugs thereof, and pharmaceutically acceptable salts thereof. The present disclosure also relates to uses of the compounds, e.g., to inhibit AMP-Activated protein kinase (AMPK) and treat cancer in a subject.

AMP-activated protein kinase inhibitors and methods of making and using the same

Compounds that inhibit the activity of Signal transducer and activator of transcription 3 (STAT3), or pharmaceutically acceptable salts or prodrugs thereof, and methods of using these compounds to treat cancer and other diseases.

STAT3 transcription factor inhibitors and methods of using the same

Primitive or progenitor hematologic cancer cells have been implicated in the early stages and development of leukemia and malignant lymphoproliferative disorders, including acute myelogenous leukemia (AML), chronic myelogenous leukemia (CML) and chronic lymphoid leukemia (CLL). Interleukin-3 receptor alpha chain (IL-3R&#x3b1; or CD123) is strongly expressed on progenitor hematologic cancer cells, but is virtually undetectable on normal bone marrow cells. The present invention provides methods of impairing progenitor hematologic cancer (e.g., leukemia and lymphomic) cells by selectively targeting cells expressing CD123. These methods are useful in the detection and treatment of leukemias and malignant lymphoproliferative disorders. Also provided are compounds useful for selectively binding to CD123 and impairing progenitor hematologic cancer cells. These compounds may include cytotoxic moieties such as, for example, radioisotopes or chemotherapeutics.

Methods to impair hematologic cancer progenitor cells and compounds related thereto

The present disclosure relates to triazole derivatives of melampomagnolide B, their synthesis, and their use as anti-cancer compounds.

Triazole derivatives of melampomagnolide B and methods of use thereof

The present invention provides compounds of the formula (I) 

Use of parthenolide derivatives as antileukemic and cytotoxic agents

The present disclosure provides dimers of melampomagnolide B (MMB), including carbamate, carbonate, succinic amide, ester and carboxamide dimers of MMB. These derivatives are useful for treating cancer in humans, in particular in treating leukemia, including acute myelogenous leukemia (AML).

Melampomagnolide B dimers

The present disclosure provides dimers of melampomagnolide B (MMB), including carbamate, carbonate, succinic amide, ester and carboxamide dimers of MMB. These derivatives are useful for treating cancer in humans, in particular in treating leukemia, including acute myelogenous leukemia (AML). A compound comprising Formula (1) wherein: Z is independently selected from the group consisting of CH2, O, C(O), and CH, wherein when Z is CH, Z is connected to Y via a double bond and Y is N.

The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, thiocarbamates, ester and amide derivatives of MMB. These derivatives are useful for treating cancer in humans.

Melampomagnolide B derivatives

The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.

The present invention relates to compounds of the formulae herein, their acceptable salts, solvates, hydrates and polymorphs thereof. The compounds of this invention are useful in treatment of disease, particularly leukemia. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating disease, disorders, or symptoms thereof in a subject.

Thiadiazolidinone derivatives

Melampomagnolide B is disclosed as a new antileukemic sesquiterpene. A biotin-conjugated derivative of melampomagnolide B was prepared to elucidate its mechanism of action. Prodrugs of Melampomagnolide B are disclosed.

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Rochester, NY, United States of America

Craig T Jordan