Quinazoline antifolates inhibiting thymidylate synthase. Variation of the amino acid
β Scribed by Jones, Terence R.; Smithers, Michael J.; Betteridge, Richard F.; Taylor, Michael A.; Jackman, Ann L.; Calvert, A. Hilary; Davies, Lawrence C.; Harrap, Kenneth R.
- Book ID
- 126035569
- Publisher
- American Chemical Society
- Year
- 1986
- Tongue
- English
- Weight
- 692 KB
- Volume
- 29
- Category
- Article
- ISSN
- 0022-2623
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## Abstract 2βAminoβ6βmethylβ5β(pyridinβ4βylsulfanyl)β3__H__βquinazolinβ4βone (**3**, AG337) a lipophilic thymidylate synthase inhibitor, is currently in clinical trials as an antitumor agent. On the basis of the crystal structure of **3** and the classical inhibitor 10βpropargylβ5,8βdideazafolic a
CB30865 (p-[N-(7-bromo-3,4-dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl+ ++)-N-(prop-2-ynyl)amino]-N-(3-pyridylmethyl)benzamide) is a quinazoline-based pyridine-containing compound that emerged from a programme aimed at the development of thymidylate synthase (TS) inhibitors as anticancer agents. Its