Purdue Research Foundation

Industrial Technology Research Institute

International Technology Research Institute

Ching-jer Chang

Curtis L Ashendel

Thomas Chan

David Waters

Fen-Lan Lin

Chen-Tao Lee

Darrick Kim

Robert L Geahlen

Jih-Dar Tsai

Shieh-Shung T Chen

Ching Te Chang

Ching Tien Chang

Xiao-jie Tong

A high yield, economical process for purifying taxanes from yew biomass is disclosed. The process does not require initial liquid:liquid portioning of the crude extract to separate highly polar substances. The organic solvent extract of the biomass is adsorbed onto and selectively desorbed from an adsorption resin to provide a taxane enriched eluate. Substantially pure individual taxanes may be further isolated from the eluate by hydrophobic-interaction chromatography.

Production of taxol and taxanes

Novel selenophene compounds useful as anti-tumor agents are described. Preferred compounds include compounds of formula I:

Selenophene anti-tumor agents

A biotransformation process for the production of hydroxylated derivatives of taxol and new derivatives of taxol and cephalomannine are described. A method for converting taxol to L-760,006 and L-760,007, and a method for converting cephalomanine to L-745,596 are provided.

Microbial transformation of taxol and cephalomannine

Novel polythiophene compounds useful as anti-tumor agents are described. Preferred compounds of the formula: ##STR1## wherein n is 0-2 and R.sub.2 and R.sub.3 are optionally substituted 2-thienyl or 3-thienyl have been found to exhibit selective cytotoxic activity against transformed human cells. Pharmaceutical compositions containing the described polythiophene compounds are expected to exhibit good chemotherapeutic activity against slow growing tumors based on tumor cell line assays. A method for treating patients having tumors utilizing the disclosed polythiophene compounds is also described.

Polythiophene anti-tumor agents

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West Lafayette, IN, United States of America

Ching-jer Chang