Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Departments of Discovery Chemistry, Oncology Discovery and Leads Discovery & Optimization, Preclinical Optimization, Bristol-Myers Squibb Co. , Route 206 and Province Line Road, Princeton, New Jersey 08543, United States.
ACS Cent Sci. 2016 Jan 27;2(1):27-31. doi: 10.1021/acscentsci.5b00345. Epub 2015 Dec 23.
The fungal-derived Taiwanese natural product antroquinonol A has attracted both academic and commercial interest due to its reported exciting biological properties. This reduced quinone is currently in phase II trials (USA and Taiwan) for the treatment of non-small-cell lung carcinoma (NSCLC) and was recently granted orphan drug status by the FDA for the treatment of pancreatic cancer and acute myeloid leukemia. Pending successful completion of human clinical trials, antroquinonol is expected to be commercialized under the trade name Hocena. A synthesis-enabled biological re-examination of this promising natural product, however, reveals minimal in vitro and in vivo antitumor activity in preclinical models.
真菌来源的台湾天然产物安特曲喹啉 A 因其报道的令人兴奋的生物学特性而引起了学术界和商业界的关注。这种还原醌目前正在进行非小细胞肺癌(NSCLC)的 II 期临床试验(美国和中国台湾),并最近被 FDA 授予孤儿药地位,用于治疗胰腺癌和急性髓系白血病。在成功完成人体临床试验之前,预计该产品将以商品名 Hocena 进行商业化。然而,对这种有前途的天然产物进行的基于合成的生物学重新检查表明,其在临床前模型中的体外和体内抗肿瘤活性很小。