从黄姜皂素和 22-表海普瑞醇合成新型细胞毒头孢菌素/里特嗪类似物。
Synthesis of a new cytotoxic cephalostatin/ritterazine analogue from hecogenin and 22-epi-hippuristanol.
机构信息
Departamento de Química Fundamental, Facultade de Ciencias, Universidade da Coruña, Campus da Zapateira, 15071 A Coruña, Spain.
出版信息
Bioorg Med Chem. 2010 Jan 1;18(1):58-63. doi: 10.1016/j.bmc.2009.11.018. Epub 2009 Nov 12.
A new cephalostatin/ritterazine analogue was prepared from the commercially available hecogenin acetate and the natural cytotoxic steroid 22-epi-hippuristanol. The method involved the reductive dimerization of enaminoketones (condensation of alpha-aminoketones) and condensation between an enaminoketone and an alpha-hydroxyketone. The new analogue showed higher cytotoxic activity than the cytotoxic 22-epi-hippuristanol against MDA-MB-231, A-549 and HT-29 cultured tumor cell lines.
一种新型的头孢菌素/里特嗪类似物由市售海柯吉宁乙酸酯和天然细胞毒性甾体 22-表-海普瑞醇制备。该方法涉及烯胺酮（α-氨基酮的缩合）的还原二聚化和烯胺酮与α-羟基酮之间的缩合。新型类似物对 MDA-MB-231、A-549 和 HT-29 培养肿瘤细胞系的细胞毒性比具有细胞毒性的 22-表-海普瑞醇更高。
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