Arizona State University

Arizona Board of Regents, a Body Corporate

Arizona Board of Regents, a Body Corporate Acting on Behalf of Arizona

Other

The United States of America As Represented by the Department of Health

University Patents, Inc.

Basf Aktiengesellschaft

Baylor University

George R Pettit

Noeleen Melody

Yoshiaki Kamano

Cherry L Herald

Jayaram K Srirangam

Michael D Williams

Jozsef Barkoczy

Sheo B Singh

Rui Tan

Zbigniew A Cichacz

Robin K Pettit

Jun-Ping Xu

Mathew D Minardi

Feng Gao

Andreas Haupt

Bernd Janssen

Kevin G Pinney

Teresa Barlozzari

Vani P Mocharla

Darko Kantoci

Steven Toms

Anupama Shirali

Fiona Hogan

Matthew P Grealish

Monte R Rhodes

Heidi J Rosenberg

John C Knight

Andreas Kling

Thomas H Smith

Peter M Blumberg

Zoltan Szallasi

Jayaram Kasturi Srirangam

Kieran P M Durkin

Yoshitatsu Ichihara

Christian Griesinger

Daniel Belik

Michael Boretzky

Pablo Arce

Maria Del Pilar Mejia

Maria Del Mejia

Yuping Tang

Cedric W Holzapfel

Sally Freeman

Jeremiah C Collins

Junping Xu

Donald P Gieschen

Delbert Herald

Yoskiaki Kamano

John E Leet

William E Pettit

Bryan R Moser

John W Lippert, Iii

Monie R Rhodes

Justin Searcy

Brian Toki

Erik J Flahive

John W Lippert

The present disclosure relates to Betulastatin compounds, pharmaceutical compositions and kits comprising such compounds, and methods for using such compounds or pharmaceutical compositions.

Betulastatin compounds

The present disclosure relates to Emetine Auristatin compounds, pharmaceutical compositions and kits comprising such compounds, and methods for using such compounds or pharmaceutical compositions.

Emetine auristatin compounds

The present disclosure relates to Silstatin compounds, pharmaceutical compositions comprising such compounds, kits, and methods for using such compounds or pharmaceutical compositions.

Silstatin compounds

The present disclosure relates to 4-azapodophylotoxins compounds, pharmaceutical compositions comprising such compounds, kits, and methods for using such compounds or pharmaceutical compositions.

4-azapodophylotoxins compounds

The present disclosure relates to Quinstatin compounds, pharmaceutical compositions comprising such compounds, kits, and methods for using such compounds or pharmaceutical compositions.

Quinstatin compounds

The present invention relates to new auristatin compounds and prodrugs thereof, compositions comprising them and uses thereof.

Auristatin tyramine phosphate salts and auristatin aminoquinoline derivatives and prodrugs thereof

The present invention relates to the crystal structures of dolastatin 16, dolamethylleuine and dolaphenvaline. The present invention also relates to processes for preparing dolamethylleuine and dolaphenvaline. The present invention further relates to computer readable medium with crystal structural data and/or information stored thereon.

Crystal structures of dolastatin 16, dolamethylleuine and dolaphenvaline, and methods for preparing dolamethylleuine and dolaphenvaline

The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.

Cyclodepsipeptides with antineoplastic activity and methods of using to inhibit cancer and microbial growth

Described herein are novel cerebroside compounds, designated as Turbostatin 1, Turbostatin 2, Turbostatin 3, and Turbostatin 4. These compounds were extracted and isolated from the marine mollusk, and their structures elucidated. The new compounds exhibit significant cancer cell growth inhibition activity against a variety of murine and human cancer cell lines, and as such appear will be useful in the treatment of various forms of neoplastic disease.

Isolation and structure of turbostatins 1-4

The present invention provides prodrugs derived from the sparingly soluble anticancer isocarbostyril narciclasine, a component of variousspecies, said prodrugs having potential for use against animal and human cancers. Also disclosed is an efficient procedure for the synthetic conversion of narciclasine to several more soluble cyclic phosphate compounds, including 'narcistatin'. 

Narcistatin prodrugs

The present invention involves use of the compounds narciclasine (2a) and 7-deoxy-narciclasine (2c), which are obtained via isolation from the medicinal plant species(Amaryllidaceae), as precursors in a novel synthesis method in which each of these compounds are selectively hydrogenated to produce trans-dihydronarciclasine (1a) and 7-deoxy-trans-dihydronarciclasine (1c). Also described herein is a novel synthesis method for producing sodium narcistatin (11) from narciclasine (2a). Further described herein are certain novel 3,4-cyclic phosphate prodrugs, including sodium-7-deoxynarcistatin (8), sodium-7-deoxy-transdihydronarcistatin (9), and sodium transdihydronarcistatin (10).

Synthesis of sodium narcistatin and related compounds

Described herein are novel compounds having antineoplastic and antimicrobial activity, obtained via structural modifications of resveratrol and combretastatin A-4, methods for synthesis of these compounds, and their use in pharmaceutical composition and for use in the treatment of mammals having cancer. Examples of the novel compounds are: (Z)- and (E)-3,4',5-trimethoxystilbene (4a, 4b); (Z)- and (E)-3,5-dimethoxy-4&#x2032;-hydroxystilbene (14c, 14d); (Z)- and (E)-3-hydroxy-4&#x2032;,5-dimethoxystilbene (14g, 14h); (Z)- and (E)-3,5-dihydroxy-4&#x2032;-methoxy-stilbene (14k, 14l); sodium resverastatin dibenzyl phosphate ((Z)-3,5-dimethoxy-4-[O-bis(benzyl)phosphoryl]-stilbene) (14m); and sodium resverastatin phosphate (14n).

Structural modification of resveratrol: sodium resverastatin phosphate

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Paradise Valley, AZ, United States of America

George R Pettit