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Coffee is the food source of cafestol and kahweol (C&amp;K), a pair of furanoditerpenoids that have antitumor, anticarcinogenic and anti-inflammatory properties. These diterpenes act on hallmarks of cancer such as resistance cell death, inducing angiogenesis, and activating migration &amp; metastasis. Cafestol and kahweol have a wide antiproliferative and pro-apoptotic profile reported for different cell lines and reduce cancer cell resistance to antineoplastic drugs. Up to now, studies show that these diterpenes are the only bioactive compounds in coffee that show significant antitumor activity in specific cancer cell lines. The pharmacokinetics studies of C&amp;K performed with different animal models demonstrate that they have a complex distribution and biotransformation. Besides the structure-activity relationship of C&amp;K is not fully understood. This narrative review aims to highlight the potential of C&amp;K in cancer chemoprevention and chemotherapy, pharmacokinetics, and the perspectives of the structure-activity relationship of these furanoditerpenoids.

Cafestol, Kahweol and Their Acylated Derivatives: Antitumor Potential, Pharmacokinetics, and Chemopreventive Profile