Singh Pragya, Faridi Uzma, Srivastava Suchita, Kumar Jonnala Kotesh, Darokar Mahender Pandurang, Luqman Suaib, Shanker Karuna, Chanotiya Chandan Singh, Gupta Atul, Gupta Madan Mohan, Negi Arvind Singh
Central Institute of Medicinal and Aromatic Plants (CIMAP-CSIR), P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow-226 015, India.
Chem Pharm Bull (Tokyo). 2010 Feb;58(2):242-6. doi: 10.1248/cpb.58.242.
A series of novel podophyllotoxin (PDT) analogues was synthesized in which the lactone moiety was shifted to C ring. Some of the derivatives were also synthesized with modified A ring. Analogues 23 and 25 exhibited potent in vitro cytotoxicity against colon cancer (CaCO(2)) cell line. p-Demethylated E-ring analogues exhibited better potency than the corresponding methylated analogues. These analogues showed toxicity comparable to PDT against human erythrocytes albeit at much higher concentrations (100 microg/ml) than their cytotoxicity values.
合成了一系列新型鬼臼毒素（PDT）类似物，其中内酯部分转移至C环。还合成了一些A环经修饰的衍生物。类似物23和25对结肠癌细胞系（CaCO(2)）表现出强大的体外细胞毒性。对E环去甲基化的类似物比相应的甲基化类似物表现出更好的活性。这些类似物对人红细胞显示出与PDT相当的毒性，尽管其浓度（100微克/毫升）比细胞毒性值高得多。
