Industrial Technology Research Institute

Purdue Research Foundation

Ching Te Chang

Yuh-Lin Allen Yang

Thomas Chan

Ching-jer Chang

Chen-Tao Lee

David Waters

Fen-Lan Lin

Curtis L Ashendel

Robert L Geahlen

Jih-Dar Tsai

Polyaryl antitumor agents

The present invention relates to a group of polyheterocyclic compounds covered by the following formula: ##STR1## wherein each of X.sub.1, X.sub.2, X.sub.3, and X.sub.4, independently, is O, S, NH, or N(C.sub.1-6 alkyl), but one of them must be O, NH, or N(C.sub.1-6 alkyl); each of R.sub.1, R.sub.2, R.sub.5, and R.sub.6, independently, is H or a substituent (e.g., halogen, CN, NO.sub.2, or C.sub.1-4 haloalkyl), but at least one of them must be a substituent; each of R.sub.3 and R.sub.4, independently, is H, C.sub.1-6 alkyl, CHO, CH.sub.2 OH, or CH.sub.2 NH.sub.2 ; and each of m and n, independently, is 0 or 1.

Polyheterocyclic compounds

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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Taipei, Taiwan

Ching Te Chang