Bongkrekic acid (BKA) is a strong inhibitor of adenine nucleotide translocase (ANT), inducing inhibition of adenosine triphosphate synthesis. We designed and synthesized simplified benzene-ring-containing BKA analogs. The key reaction is the one-pot double Sonogashira reaction, which forms the main skeleton. The analogs were efficiently synthesized in 8–10 longest linear sequence steps. This synthetic method can be applied for the preparation of other analogs having different combinations of carbon chain lengths. Furthermore, the allyloxy group on the benzene ring can be easily replaced by other functional groups. Our preliminary biological evaluation based on mitochondrial inhibitory effects revealed the high potency of the analogs bearing the same carbon chain length as that of BKA. In particular, the prefunctionalized analogs are potential ANT inhibitors.

邦克里克酸（BKA）是腺嘌呤核苷酸转位酶（ANT）的强抑制剂，可诱导三磷酸腺苷合成的抑制。我们设计并合成了简化的含苯环的BKA类似物。关键反应是一锅法双重Sonogashira反应，它形成了主要骨架。这些类似物以8–10个最长的线性序列步长有效合成。该合成方法可用于制备具有不同碳链长度组合的其他类似物。此外，苯环上的烯丙氧基可以容易地被其他官能团取代。我们基于线粒体抑制作用的初步生物学评估表明，具有与BKA相同碳链长度的类似物具有很高的效价。尤其是，