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Acta Chimica Sinica ›› 2001, Vol. 59 ›› Issue (10): 1633-1638. Previous Articles Next Articles
Original Articles
宋相志;刘广;杨屹;沈丽春;章士伟
发布日期:
Song Xiangzhi;Liu An;Yang Yi;Shen Lichun;Zhang Shiwei
Published:
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Four effective differentiation inducers, the derivatives of HMBA, N, N, N', N'-tetracetylhexamethylenediamine, N, N'-hexamethylenebis (3- pyridinecarboxamide), 4,4'-(hexane-1, 6-diyl)bis(piperazine-2,6-dione) and 3,3'-(hexane-1,6-diyl) bis (5,5-dimethylhydantoin), have been synthesized and identified by MS, NMR, IR and elemental analysis. The synthetic methods and routes have been optimized. The anticancer activity of 4,4'-(hexane-1,6-diyl)bis(piperazine-2,6-dione) against human erythroleukemia K562 cells was tested and its potency is ten times greater than ICRF-154[4,4'-(ethane-1,2-diyl)bis (piperazine- 2, 6-dione)].The structure of compound Ⅳ was determined by single crystal X-ray diffraction and compared with compoundsⅠ,Ⅱ, Ⅲ. In the structures of these compounds, the hexamethylene chain is fully extended, which can increase the flexibility of the molecule. There are hydrogen bonds in compounds Ⅱ,Ⅲ,Ⅳ. It is found that the hydrogen bonds and the ring structure of the functional groups can influence the activity of the compounds.
Key words: CRYSTAL STRUCTURE, ANTINEOPLASTIC ACTIVITY, ELEMENTAL ANALYSIS, MASS SPECTROGRAPHY, NMR SPECTROMETRY, PIPERAZINE P, HEXANE P
CLC Number:
O64
Song Xiangzhi;Liu An;Yang Yi;Shen Lichun;Zhang Shiwei. Synthesis and crystal structures of cancer cell differentiation inducers[J]. Acta Chimica Sinica, 2001, 59(10): 1633-1638.
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