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Combretastatin:从天然产物到药物研发

Combretastatins: from natural products to drug discovery.

作者信息

Cirla Alessandra, Mann John

机构信息

School of Chemistry, Queen's University Belfast, Belfast BT9 5AG, Northern Ireland.

出版信息

Nat Prod Rep. 2003 Dec;20(6):558-64. doi: 10.1039/b306797c.

DOI:10.1039/b306797c
PMID:14700199
Abstract

The combretastatins are a group of anti-mitotic agents isolated from the bark of the South African tree Combretum caffrum. The most potent member is combretastatin A-4, and this compound together with a phosphate pro-drug form have already progressed through into clinical trails for the treatment of solid tumours. What makes this class of compounds rather more interesting than other anti-mitotic agents is that they are also angiogenesis inhibitors, and are being evaluated for their efficacy in the treatment of diabetic retinopathy which is the biggest single cause of blindness They are thus of considerable contemporary interest.

摘要

康普瑞他汀是从南非灌木非洲风车子树皮中分离出来的一组抗有丝分裂剂。其中活性最强的成员是康普瑞他汀A - 4,该化合物及其磷酸前药形式已进入实体瘤治疗的临床试验阶段。这类化合物比其他抗有丝分裂剂更具吸引力的地方在于,它们还是血管生成抑制剂,目前正在评估其治疗糖尿病性视网膜病变(失明的最大单一病因)的疗效。因此,它们在当代备受关注。

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