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  • Title: Potential antitumor agents. 19. Multiply substituted 4'-(9-acridinylamino)methanesulfonanilides.
    Author: Cain BF, Atwell G.
    Journal: J Med Chem; 1976 Sep; 19(9):1124-9. PubMed ID: 978676.
    Abstract:
    A series of 42 multiply substituted 4'-(9-acridinylamino)methanesulfonanilides has been prepared and evaluated in the L1210 system. In addition to biologic activity changes resulting from altered agent lipophilic-hydrophilic balance variants containing both acridine 4-CH3 and 3-NH2, NHCOCH3 or NO2 substituents have reduced activity. Variants 3,6-disubstituted, using functions of differing electronic character, have depressed activity, suggesting that there is limited site bulk tolerance. Asymmetric 3,5-disubstitution should then be the preferred pattern; the 3-ND-5CH-3'-OCH variant is the most dose potent (optimum dose qd 1-5, 1.25 mg/kg/day) of the high activity agents of this series so far prepared.
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