Introduction

The invention relates to compounds and compositions containing said compounds having cytostatic (antiproliferative) activity against tumor cells, more specifically against T-cell lymphoma, hepatoma and prostate cancer cells.

Technical features

The invention relates to compounds and compositions containing said compounds having cytostatic (antiproliferative) activity against tumor cells. The invention further relates to the use of said compounds as biologically active ingredients, more specifically as a medicine for the treatment of cancer. The present invention is based on the unexpected finding that certain combinations of substituents at different positions of thiophenes and their derivatives are able to meet one or more of the medical needs and in particular have significant and selective anticancer activity.

Possible Applications

• Treatment of hyperproliferative disorders, including cancer, leukemia and lymphoma. 2-Amino thiophene-3-carboxylates display an unusual cytostatic selectivity for several T-cell (but not B-cell) lymphoma, prostate cancer, kidney carcinoma and hepatoma cell lines. These tumour selective compounds preferentially suppressed protein synthesis rather than DNA or RNA synthesis.

Advantages

• Several compounds of this series acted as novel and highly selective cytostatic agents. Among the synthesized compound, derivative 1 inhibited the growth of 15 cancer cell lines at nanomolar concentrations in the NCI-60 anticancer drug screen of US NIH. In addition, compound 1 was not comparable to any known antitumor drug present in the NIH database, suggesting a likely novel molecular mechanism of action of 1.