Bifidenone is an anticancer compound that Sequoia discovered in tiny quantities in a Gabonese tree. A synthetic route was previously developed to produce the compound without harvesting the tree. Using those methods, Sequoia worked with scientists at AMRI to synthesize analogues and examine the structure–activity relationship of bifidenone derivatives. That work, now published in the Journal of Medicinal Chemistry, identified an optimized lead compound with promising antitumor activity in mice. The optimized compound is also significantly more potent than paclitaxel against taxane-resistant cell lines in vitro.
Citation: Bifidenone: Structure–Activity Relationship and Advanced Preclinical Candidate. Zhongping Huang, Russell B. Williams, Steven M. Martin, Julie A. Lawrence, Vanessa L. Norman, Mark O’Neil-Johnson, Jim Harding, John E. Mangette, Shuang Liu, Peter R. Guzzo, Courtney M. Starks, and Gary R. Eldridge. Journal of Medicinal Chemistry, 2018, 61 (15), pp 6736–6747.