【摘 要】
：
"Molecular Architecture" strategy focuses on the building of new compounds from scratch instead of the limited modifications starting from the natural products.It allows scientists to rationally desig
【机 构】
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College of Pharmacy and The State Key Laboratory of Elemento-organic Chemistry Nankai University Chi
【出 处】
：
BIT‘s2nd Annual World Cancer Congess-2009 (2009第二届癌症大会)
论文部分内容阅读
"Molecular Architecture" strategy focuses on the building of new compounds from scratch instead of the limited modifications starting from the natural products.It allows scientists to rationally design and synthesize many types of analogs, most of which are inaccessible through semi-synthesis.So it is a very powerful strategy in discovery of lead compounds with better pharmacological properties.However, in the subsequent preparation of hundreds of gram of API for the preclinical and clinical trials, the structural complexity of these compounds may exert high challenge to organic chemists.This challenge is especially overwhelming in the development of synthetic epothilone analogs as anti-cancer drug.Several efficient total syntheses ofepothilone natural products or analogs are demonstrated.Moreover, a novel, scalable, concise, convergent, and cost-effective and environmentally friendlily sequence is developed for KOS-1584, an epothilone analog in phase Ⅱ trial.The success of this sequence suggests that: with the development of modern organic synthesis, the application of"Molecular Architecture" strategy in drug R&D will be more feasible/promising.
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