Twelve phosphonopropionates derived from 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid (3-IPEHPC) were synthesized and evaluated for their activity as inhibitors of protein geranylgeranylation. The nature of the substituent in the C6 position of imidazo[1,2-a]pyridine ring was responsible for the compound's activity against Rab geranylgeranyl transferase (RGGT). The most active inhibitors disrupted Rab11A prenylation in the human cervical carcinoma HeLa cell line. The esterification of carboxylic acid in the phosphonopropionate moiety turned the inhibitor into an inactive analog.

中文翻译：

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6-取代的咪唑并[1,2-a]吡啶-3-基-2-膦酰基丙酸作为Rab Geranylgeranyl转移酶的潜在抑制剂的合成

衍生自2-羟基-3-咪唑基[1,2-一种] pyridin-3-yl合成了-2-膦酰基丙酸（3-IPEHPC），并评估了其作为蛋白香叶基香叶基化的抑制剂的活性。咪唑并[1,2-的C6位置的取代基的性质一种]吡啶环负责该化合物对Rab geranylgeranyl转移酶（RGGT）的活性。活性最高的抑制剂可破坏人宫颈癌HeLa细胞系中的Rab11A异戊二烯化。膦酸丙酸酯部分中羧酸的酯化使抑制剂变成了无活性的类似物。