The compounds herein disclosed are N-substituted tetrahydroisoquinoline benzamide and benzene sulfonamide compounds that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-substituted tetrahydroisoquinoline compounds have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC.sub.50 values against the breast cancer cells that are 6- to 10-fold less than the IC.sub.50 of Tamoxifen.

Florida A&amp;M University

N-substituted tetrahydroisoquinoline benzamides/benzene sulfonamides as anti-cancer agents

Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: ##STR00001## wherein R.sup.1 may be alkyl, cycloalkyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; R.sup.2 is H, alkyl, aryl, alkylaryl, arylalkyl, and cycloalkyl; R.sup.3, with the base nitrogen, forms an amide or sulfonamide; R.sup.4 is selected from nitro, amine, amide, and benzamide; or a pharmaceutically acceptable salts thereof. Also provided are small molecule selective aromatase inhibitors having a molecular weight of less 500 g/mol. In some embodiments, the small molecule selective aromatase inhibitors described herein have a molecular weight of less than 450 g/mol. Also provided are methods for suppressing aromatase activity expression in cancer cells comprising the step of administering a pharmaceutically effective amount of a small molecule aromatase inhibitor to a subject in need of such treatment. In one embodiment, the cancer cells are breast cancer cells.

benzamide/rinnavähk

N-substituted tetrahydroisoquinoline benzamides/benzene sulfonamides as anti-cancer agents

Sulfonanilide analogs as selective aromatase modulators (SAMs)

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