A.R College of Pharmacy affiliated to Sardar Patel University, Vallabh Vidyanagar, Dist. Anand, Gujarat - 388 120, India.
Indian J Pharmacol. 2008 Mar;40(2):49-58. doi: 10.4103/0253-7613.41038.
Traditional medicines, including Chinese herbal formulations, can serve as the source of potential new drugs, and initial research focuses on the isolation of bioactive lead compound(s). The development of novel plant-derived natural products and their analogs for anticancer activity details efforts to synthesize new derivatives based on bioactivity- and mechanism of action-directed isolation and characterization coupled with rational drug design - based modification. Also, the anticancer activity of certain natural products and their analogs can be enhanced by synthesizing new derivatives based on active pharmacophore models; drug resistance and solubility and metabolic limitations can be overcome by appropriate molecular modifications; and new biological properties or mechanisms of action can be added by combining other functional groups or molecules. Preclinical screening for in vitro human cell line panels and selected in vivo xenograft testing then identifies the most promising drug development targets.
传统药物,包括中草药制剂,可以作为潜在新药的来源,初步研究集中在生物活性先导化合物的分离上。为了开发具有抗癌活性的新型植物源性天然产物及其类似物,人们根据生物活性和作用机制导向的分离和表征以及合理的药物设计进行了基于合理药物设计的新衍生物的合成。此外,通过基于活性药效团模型合成新的衍生物,可以增强某些天然产物及其类似物的抗癌活性;通过适当的分子修饰,可以克服药物耐药性、溶解度和代谢限制;通过结合其他官能团或分子,可以增加新的生物学特性或作用机制。体外人细胞系筛选和选定的体内异种移植试验然后确定最有前途的药物开发靶点。