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天然产物化学在药物发现中的作用。

The role of natural product chemistry in drug discovery.

作者信息

Butler Mark S

机构信息

MerLion Pharmaceuticals, 1 Science Park Road, The Capricorn #05-01, Singapore Science Park II, 117528, Singapore.

出版信息

J Nat Prod. 2004 Dec;67(12):2141-53. doi: 10.1021/np040106y.

Abstract

Although traditionally natural products have played an important role in drug discovery, in the past few years most Big Pharma companies have either terminated or considerably scaled down their natural product operations. This is despite a significant number of natural product-derived drugs being ranked in the top 35 worldwide selling ethical drugs in 2000, 2001, and 2002. There were 15 new natural product-derived drugs launched from 2000 to 2003, as well as 15 natural product-derived compounds in Phase III clinical trials or registration at the end of 2003. Recently, there has been a renewed interest in natural product research due to the failure of alternative drug discovery methods to deliver many lead compounds in key therapeutic areas such as immunosuppression, anti-infectives, and metabolic diseases. To continue to be competitive with other drug discovery methods, natural product research needs to continually improve the speed of the screening, isolation, and structure elucidation processes, as well addressing the suitability of screens for natural product extracts and dealing with issues involved with large-scale compound supply.

摘要

尽管传统上天然产物在药物研发中发挥了重要作用,但在过去几年里,大多数大型制药公司要么终止了天然产物业务,要么大幅缩减了规模。尽管在2000年、2001年和2002年,有相当数量的天然产物衍生药物跻身全球最畅销的35种处方药之列。2000年至2003年期间有15种新的天然产物衍生药物上市,2003年底还有15种天然产物衍生化合物处于III期临床试验或注册阶段。最近,由于替代药物研发方法未能在免疫抑制、抗感染和代谢疾病等关键治疗领域提供许多先导化合物,人们对天然产物研究重新产生了兴趣。为了继续与其他药物研发方法竞争,天然产物研究需要不断提高筛选、分离和结构解析过程的速度,同时解决针对天然产物提取物的筛选适用性问题以及处理大规模化合物供应所涉及的问题。

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