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首页> 美国卫生研究院文献>other >Sequential cytotoxicity: A theory examined using a series of 35-bis(benzylidene)-1-diethylphosphono-4-oxopiperidines and related phosphonic acids
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Sequential cytotoxicity: A theory examined using a series of 35-bis(benzylidene)-1-diethylphosphono-4-oxopiperidines and related phosphonic acids

机译：序贯细胞毒性：使用一系列35-双（苄基）-1-二乙基膦酰基-4-氧哌啶和相关膦酸检查的理论

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The concept of sequential cytotoxicity, which states that successive chemical attacks on cellular constituents can be more deleterious to neoplasms than normal cells, was evaluated using a series of 3,5-bis(benzylidene)- 1-diethylphosphono-4-oxopiperidines >1 and related phosphonic acids >2, which were screened against a panel of malignant and normal cell lines. The compounds proved to be not only potent cytotoxins (71% of the CC50 figures are submicromolar) but to display greater cytotoxicity to the neoplastic cells. QSAR revealed that both cytotoxic potencies and selective toxicity were increased by a rise in the electron-with-drawing properties and a decrease in the hydrophobicity of the aryl substituents. Utilisation of the PL10 concept and evaluation of druglike properties revealed >1c as the lead tumour-specific cytotoxin. This molecule activated caspase-3 in HL-60 cells but not in the HSC-2 cell line. While >1c caused internucleosomal DNA fragmentation in HL-60 cells, it did not elicit this effect in either HSC-2 and HSC-4 cells. Clearly >1c exerts its cytotoxic potencies by different mechanisms and such pleiotropy is likely the principal reason for the remarkable display of preferential toxicity towards malignant cells of the compounds in series >1 and >2.

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