Comparative structure-activity relationships of antifolate triazines inhibiting murine tumor cells sensitive and resistant to methotrexate

CD Selassie, C Hansch, TA Khwaja…

Index: Selassie, Cynthia Dias; Hansch, Corwin; Khwaja, Tasneem A.; Dias, Cecilia B.; Pentecost, Stephanie Journal of Medicinal Chemistry, 1984 , vol. 27, # 3 p. 347 - 357

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Citation Number: 13

Abstract

The inhibitory effect of 108 4, 6-diamino-1, 2-d~ y~~ 2, 2-dimethyl-l-(substitu~ d-phenyl)-s- tri~ ines on murine L5178Y tumor cells, resistant and sensitive to methotrexate (MTX), has been studied. From the pIm values, quantitative structureactivity relationships have been formulated which show that the lipophilic triazines are much more inhibitory against resistant cells than methotrexate or hydrophilic triazines. The results are compared with the ...