2-氨基-4-氧-6-取代吡咯并[2,3-d]嘧啶的合成及其体外抗肿瘤生物活性研究

来源 :全国药物化学学术会议暨第四届中英药物化学学术会议 | 被引量 : 0次 | 上传用户:whitesharke
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  选择性差,毒副作用大仍是目前绝大多数抗肿瘤化学治疗药物的主要缺点。能够选择性的抑制或杀死肿瘤细胞一直是抗肿瘤化疗药物研发的首要目标。传统的叶酸拮抗剂如甲氨蝶呤和培美曲塞作为抗肿瘤化疗药物,在临床上已经取得了巨大成功,但仍具有选择性差、毒副作用大的缺陷。研究表明还原叶酸转运蛋白(Reduced Folate Carrier,RFC),叶酸受体(Folate Receptors,FR)和质子偶联叶酸转运体(Proton-Coupled Folate Transporters,PCFT)是转运叶酸和叶酸拮抗剂的三种转运体。
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