Antitumour/Thymidylate Synthase Inhibitors: Novel Quinazoline Derivatives as Thymidylate Synthase Inhibitors

Summary

Novelty: Novel quinazoline derivatives are disclosed. The compounds exhibit antitumour activity in animals and human patients. These compounds are useful in the treatment of breast, ovarian and liver cancer.

Biology: The compounds are tested in vitro for inhibition of thymidylate synthase (IC₅₀ = 0.1-10 μM); for inhibition of growth of L1210-cells (IC₅₀ = 0.1-100 μM); and for inhibition of growth of MCF-7 breast cancer cells (IC₅₀ = 0.1-100 μM). A dose of 1-100 mg/kg is considered therapeutically effective.

Chemistry: The compounds are prepared in simple one or two step processes experimental details are given. p-N[-(3,4 Dihydro-2-methyl-4-oxoquinazoline-6-ylmethyl)-N-(prop-2-ynyl)amino]N-propylbenzamide is one of the eighteen compounds which are specifically claimed.