【摘 要】
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Natural product (NP) leads are usually more potent than those identified from synthetic libraries and can possess distinctively valuable characteristics in
【机 构】
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Roche R&D Centre(China)Ltd. China
【出 处】
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中国上海第七届国际新药发明科技年会
论文部分内容阅读
Natural product (NP) leads are usually more potent than those identified from synthetic libraries and can possess distinctively valuable characteristics in structural diversity and in modulating difficult targets such as protein-protein interactions.For example,a particular structural feather that is much more common in natural products than in synthetic molecules is the macrocycle:a ring architecture of 12 or more atoms.These natural macrocyclic molecules often have well-balanced structural pre-organisation and flexibility,so that they are potent and selective on one hand,and orally bioavailable on the other hand although they are not "Rule-of-5" compliant.They can contain functional sub-domains that enable them to interact with two distinct proteins and offer unique modulations of therapeutically important targets.However their complex structures can limit the scope of optimization by total or semi synthesis.Moreover semi-synthetic approaches often lead to further increase in molecular size,resulting inevitably in the decrease of ligand efficiency.
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