englerin-a and Kidney-Neoplasms

In the decade since the discovery of englerin A (1) and its potent activity in cancer models, this natural product and its analogues have been the subject of numerous chemical, biological, and preclinical studies by many research groups. This review summarizes published findings and proposes further research directions required for entry of an englerin analogue into clinical trials for kidney cancer and other conditions.

Topics: Antineoplastic Agents, Phytogenic; Humans; Kidney Neoplasms; Molecular Structure; Sesquiterpenes, Guaiane

The chlorinated englerins (3-9) were isolated from Phyllanthus engleri and shown to selectively inhibit the growth of renal cancer cells. The compounds were shown to be extraction artifacts produced by exposure to chloroform decomposition products during their isolation. The most active compound, 3, was synthesized from englerin A (1).

Topics: Antineoplastic Agents, Phytogenic; Drug Screening Assays, Antitumor; Humans; Hydrocarbons, Chlorinated; Kidney; Kidney Neoplasms; Molecular Structure; National Cancer Institute (U.S.); Phyllanthus; Sesquiterpenes, Guaiane; Stereoisomerism; Tanzania; United States