Synthesis of quinazoline analogs of folic acid modified at position 10
- 1 November 1977
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 20 (11) , 1393-1396
- https://doi.org/10.1021/jm00221a008
Abstract
The quninazoline couterpart of folic acid (5,8-deazafolic acid) as well as its 10-methyl analog was an effective inhibitor of thymidylate synthetase from several sources. The synthesis of modifications in which the N atom at position 10 is replaced by S, O or methylene affording 10-thia-5,8-deazafolic acid, 10-oxa-5,8-deazafolic acid and 5,8,10-deazafolic acid, respectively, was described. In preliminary testing, each of the target compounds displayed marginal activity against L1210 leukemia in mice.This publication has 3 references indexed in Scilit:
- Folate analogues altered in the C9-N10 bridge region. 10-Oxafolic acid and 10-oxaaminopterinJournal of Medicinal Chemistry, 1976
- A new synthetic route to quinazoline analogs of folic acidJournal of Heterocyclic Chemistry, 1975
- Synthesis and antifolate activity of 10-deazaminopterinJournal of Medicinal Chemistry, 1974