Design and synthesis of novel 6, 7-imidazotetrahydroquinoline inhibitors of thymidylate synthase using iterative protein crystal structure analysis
SH Reich, MAM Fuhry, D Nguyen, MJ Pino…
Index: Reich, Siegfried H.; Fuhry, Mary Ann M.; Nguyen, Dzuy; Pino, Mark J.; Welsh, Katherine M.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 5 p. 847 - 858
Full Text: HTML
Citation Number: 53
Abstract
Antifolate inhibitors of thymidylate synthase (TS) have primarily been based on the structure of folic acid. This paper describes the identification and development of novel 6, 7- imidazotetrahydrcquinoline TS inhibitors by iterative ligand design, synthesis, and crystallographic analysis of protein-inhibitor complexes. Beginning with a high-resolution crystal structure of E. coli TS (TS, EC 2.1. 1.451, an imidazotetrahydroquinoline inhibitor ...
Related Articles:
[Kantam, M. Lakshmi; Neelima; Sreedhar; Chakravarti, Rajashree Synlett, 2008 , # 10 p. 1455 - 1458]
[Cacchi, Sandro; Fabrizi, Giancarlo; Goggiamani, Antonella; Parisi, Luca M.; Bernini, Roberta Journal of Organic Chemistry, 2004 , vol. 69, # 17 p. 5608 - 5614]
[Cacchi, Sandro; Fabrizi, Giancarlo; Goggiamani, Antonella; Parisi, Luca M.; Bernini, Roberta Journal of Organic Chemistry, 2004 , vol. 69, # 17 p. 5608 - 5614]
[Cacchi, Sandro; Fabrizi, Giancarlo; Goggiamani, Antonella; Parisi, Luca M. Organic Letters, 2002 , vol. 4, # 26 p. 4719 - 4721]
[Cacchi, Sandro; Fabrizi, Giancarlo; Goggiamani, Antonella; Parisi, Luca M.; Bernini, Roberta Journal of Organic Chemistry, 2004 , vol. 69, # 17 p. 5608 - 5614]