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1、J.Nat.Prod.2004,67,2141-21532141ReviewsTheRoleofNaturalProductChemistryinDrugDiscovery²MarkS.Butler*MerLionPharmaceuticals,1ScienceParkRoad,TheCapricorn#05-01,SingaporeScienceParkII,Singapore117528ReceivedApril27,2004Althoughtraditionallynaturalproductshavepl
2、ayedanimportantroleindrugdiscovery,inthepastfewyearsmostBigPharmacompanieshaveeitherterminatedorconsiderablyscaleddowntheirnaturalproductoperations.Thisisdespiteasignificantnumberofnaturalproduct-deriveddrugsbeingrankedinthetop35worldwidesellingethicaldrugsin
3、2000,2001,and2002.Therewere15newnaturalproduct-deriveddrugslaunchedfrom2000to2003,aswellas15naturalproduct-derivedcompoundsinPhaseIIIclinicaltrialsorregistrationattheendof2003.Recently,therehasbeenarenewedinterestinnaturalproductresearchduetothefailureofalter
4、nativedrugdiscoverymethodstodelivermanyleadcompoundsinkeytherapeuticareassuchasimmunosuppression,anti-infectives,andmetabolicdiseases.Tocontinuetobecompetitivewithotherdrugdiscoverymethods,naturalproductresearchneedstocontinuallyimprovethespeedofthescreening,
5、isolation,andstructureelucidationprocesses,aswelladdressingthesuitabilityofscreensfornaturalproductextractsanddealingwithissuesinvolvedwithlarge-scalecompoundsupply.IntroductionbioticresearchwasprolificandincludedexamplessuchasForthousandsofyearsmedicineandna
6、turalproductsstreptomycin(6),chloramphenicol(7),chlortetracycline(8),(NPs)havebeencloselylinkedthroughtheuseoftradi-cephalosporinC(9),erythromycin(10),andvancomycintionalmedicinesandnaturalpoisons.1-5Clinical,pharma-(11).1,4,8,9Allofthesecompounds,orderivativ
7、esthereof,cological,andchemicalstudiesofthesetraditionalmedi-arestillinuseasdrugstoday.cines,whichwerederivedpredominantlyfromplants,wereOneofthenextbreakthroughsindrugdiscoverywasthethebasisofmostearlymedicinessuchasaspirin(1),useofmechanism-basedscreeningfo
8、rbioassay-guideddigitoxin(2),morphine(3),quinine(4),andpilocarpinefractionation.Throughcontinualimprovementofscreening(5).1-5formats,reagentproduction,robotics,anddatamanage-ment,mechanis
