Sesquiterpene derivatives, represented by the following formulae (I) and (II), having progesterone receptor binding inhibitory activity are disclosed. They can be used as therapeutic and prophylactic agents for progesterone-related diseases, for example, as a carcinostatic agent for breast cancer or ovarian cancer, a therapeutic agent for hysteromyoma, endometriosis, meningioma, or myeloma, an abortifacient, an oral contraceptive pill, or a therapeutic or prophylactic agent for osteoporosis or climacteric disturbance. These compounds have no steroid skeleton and, hence, are considered to be advantageously free from side effect inherent in steroid such as found in conventional progesterone receptor binding inhibitors having a steroid skeleton. ##STR1## wherein R.sup.1 represents a hydrogen atom, a halogen atom, C.sub.1 -C.sub.5 alkoxy, or phenylthio; R.sup.2 represents C.sub.1 -C.sub.5 alkoxy or C.sub.2 -C.sub.5 alkanoyloxy; and ---- with letters a, b, c, d, and e attached thereto represent a double bond or a single bond; R.sup.3 has the same meaning as R.sup.2 ; and R.sup.4 represents C.sub.1 -C.sub.5 alkoxy.

Meiji Seika Kaisha, Ltd.

Sesquiterpene derivatives having progesterone receptor binding inhibitory activity

A new class of sesquiterpene derivative useful for treating cancerous and inflammatory diseases are disclosed. These deoxyelephantopin derivatives are effective in suppressing proliferation, migration, mobility, invasion, growth, and/or metastasis of cancer cells in a patient, or useful for enhancing an anti-proliferative effect of another anti-cancer drug on cancer cells when treating a patient, or for sensitizing and/or enhancing an anti-cancer effect of a gluthathione synthesis blocker on inhibition of triple negative breast cancer cell activity, or for treatment and/or prophylaxis of lipopolysaccharide-stimulated inflammatory response in a patient, or for all of the above. Also disclosed are methods of preparing the deoxyelephantopin derivatives.

Academia Sinica

Sesquiterpene derivatives and their use in inflammation or cancer treatment

This subject invention is directed to a method for inhibition of cancer cells, comprising administrating an effective amount of a compound of formula I (Sesquiterpene lactones, antrocin) or pharmaceutically acceptable salts thereof, together with a pharmaceutically acceptable carrier, wherein the cancer cells are selected from colorectal cancer cells, liver cancer cells, lung cancer cells or breast cancer cells.

sesquiterpene/brustkrebs

Sesquiterpene derivatives having progesterone receptor binding inhibitory activity

Sesquiterpene derivatives and their use in inflammation or cancer treatment

Antrocin containing pharmaceutical compositions for inhibiting cancer cells

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