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Deprecated: Implicit conversion from float 213.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Int+J+Oncol 2000 ; 16 (5): 971-8 Nephropedia Template TP
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Structure-activity relationships for G2 checkpoint inhibition by caffeine analogs #MMPMID10762633
Jiang X; Lim LY; Daly JW; Li AH; Jacobson KA; Roberge M
Int J Oncol 2000[May]; 16 (5): 971-8 PMID10762633show ga
Caffeine inhibits the G2 checkpoint activated by DNA damage and enhances the toxicity of DNA-damaging agents towards p53-defective cancer cells. The relationship between structure and G2 checkpoint inhibition was determined for 56 caffeine analogs. Replacement of the methyl group at position 3 or 7 resulted in loss of activity, while replacement at position 1 by ethyl or propyl increased activity slightly. 8-Substituted caffeines retained activity, but were relatively insoluble. The structure-activity profile did not resemble those for other known pharmacological activities of caffeine. The active analogs also potentiated the killing of p53-defective cells by ionizing radiation, but none was as effective as caffeine.