Antitumor agents. 25. Synthesis and antitumor activity of uracil and thymine .alpha.-methylene-.gamma.-lactones and related derivatives
- 1 July 1977
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 20 (7) , 911-914
- https://doi.org/10.1021/jm00217a009
Abstract
Uracil and thymine .alpha.-methylene-.gamma.-lactones and related derivatives were synthesized as novel potential alkylating antitumor agents. The synthesis of these compounds involved the convenient Reformatsky type reaction between ethyl .alpha.-(bromomethyl)acrylate and the proper pyrimidinyl ketones. Preliminary in vivo tumor assays indicated that these compounds were active against the Walker 256 carcinosarcoma in rats and the P-388 lymphocytic leukemia as well as the B-16 melanotic melanoma in mice at 2.5-25 mg/kg.This publication has 2 references indexed in Scilit:
- Bruceoside-A, a novel antileukaemic quassinoid glycoside from Brucea javanicaJournal of the Chemical Society, Chemical Communications, 1977
- Cysteine scavengers. 2. Synthetic .alpha.-methylenebutyrolactones as potential tumor inhibitorsJournal of Medicinal Chemistry, 1974