title: Antroquinonol A: Scalable Synthesis and Preclinical Biology of a Phase 2 Drug Candidate.
abstract: 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.
authors.affiliation: Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
authors.forename: Matthew T
authors.initials: MT
authors.lastname: Villaume
authors.affiliation: Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
authors.forename: Eran
authors.initials: E
authors.lastname: Sella
authors.affiliation: Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
authors.forename: Garrett
authors.initials: G
authors.lastname: Saul
authors.affiliation: 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.
authors.forename: Robert M
authors.initials: RM
authors.lastname: Borzilleri
authors.affiliation: 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.
authors.forename: Joseph
authors.initials: J
authors.lastname: Fargnoli
authors.affiliation: 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.
authors.forename: Kathy A
authors.initials: KA
authors.lastname: Johnston
authors.affiliation: 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.
authors.forename: Haiying
authors.initials: H
authors.lastname: Zhang
authors.affiliation: 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.
authors.forename: Mark P
authors.initials: MP
authors.lastname: Fereshteh
authors.affiliation: 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.
authors.forename: T G Murali
authors.initials: TG
authors.lastname: Dhar
authors.affiliation: Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
authors.forename: Phil S
authors.initials: PS
authors.lastname: Baran