Nanduri Srinivas, Nyavanandi Vijay Kumar, Thunuguntla Siva Sanjeeva Rao, Kasu Sridevi, Pallerla Mahesh Kumar, Ram P Sai, Rajagopal Sriram, Kumar R Ajaya, Ramanujam Rajagopalan, Babu J Moses, Vyas Krishnamurthi, Devi A Sivalakshmi, Reddy G Om, Akella Venkateswarlu
Discovery Chemistry, Dr. Reddy's Laboratories Ltd, Discovery Research, Bollaram Road, Miyapur, Hyderabad 500 049, India.
Bioorg Med Chem Lett. 2004 Sep 20;14(18):4711-7. doi: 10.1016/j.bmcl.2004.06.090.
Andrographolide 1, the cytotoxic agent of the plant Andrographis paniculata was subjected to semi-synthetic studies leading to the preparation of a number of potent and novel analogues. Of the analogues synthesized, while 8,17-epoxy andrographolide 6 retained the cytotoxic activity of 1, ester derivatives of 6 exhibited considerable improvement in activity. Lower activity was observed when the epoxy moiety in the triacetate 9, derived from 6 was modified. Synthesis and structure-activity relationships are discussed.
穿心莲内酯1是植物穿心莲的细胞毒性剂，对其进行了半合成研究，从而制备了许多强效且新颖的类似物。在合成的类似物中，虽然8,17-环氧穿心莲内酯6保留了1的细胞毒性活性，但6的酯衍生物在活性方面有显著提高。当对由6衍生的三乙酸酯9中的环氧部分进行修饰时，观察到活性较低。本文讨论了合成方法及构效关系。
