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[Cancer Research 12, 399-406, June 1, 1952]
© 1952 American Association for Cancer Research

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Tissue Culture Screening of Purines and Purine Nucleosides for Selective Damage to Mouse Sarcoma Cells*

John J. Biesele, Ruth E. Berger and Marilyn Clarke

( Cell Growth Section of the Division of Experimental Chemotherapy, Sloan-Kettering Institute for Cancer Research, New York 21, N.Y.)

1. Comparative toxic effects of 96 purines and 28 purine nucleosides on embryonic mouse skin cells and Crocker mouse Sarcoma 180 cells in tissue culture are reported.
2. Compounds causing the greatest differential damage to Sarcoma 180 cells were most prominent among the adenines and the 2,6-diaminopurines. The 2-aminopurines, guanines, hypoxanthines, and xanthines were less effective.
3. The most effective compounds were certain 2-substituted adenines, particularly 2-chloroadenine, 2,6-diaminopurine, 2-methyladenine, 2-iodoadenine, and certain 2,6-diamino-8-arylpurines.
4. Additional substituents at other positions reduced the effectiveness of 2-substituted adenines.
5. The five nucleosides that caused more than slight damage in 1 day of exposure were ribofuranosyladenines or xylofuranosyladenines substituted, if at all, only in position 2 of adenine. The most toxic was 2-chloroadenosine.
6. Purine nucleosides, with the major exception of 2-hydroxyadenosine, tended to be less toxic to Sarcoma 180 cells than the corresponding free purines. For example, 2-aminoadenosine was about 1/40th as toxic to Sarcoma 180 cells as was 2,6-diaminopurine. Some nucleosides were more toxic to embryonic cells than were the free purines.
7. Consequently, embryonic and sarcomatous mouse cells were damaged to about the same extent by purine nucleosides.

* This work was supported in part by grants from the American Cancer Society; the National Cancer Institute, of the National Institutes of Health, Public Health Service; and the Damon Runyon Memorial Fund for Cancer Research.

Received 9/12/51.


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Copyright © 1952 by the American Association for Cancer Research.