DESIGN AND SYNTHESIS OF ANTI-BREAST CANCER AGENTSJournal: World Journal of Pharmaceutical Research (Vol.1, No. 1)
Publication Date: 2012-03-01
Authors : Kirti Gupta Vishal Malviya S.N.Sakarkar;
Page : 58-77
Keywords : Anti Breast Cancer Activity; SERMs; and Chalcones;
Breast cancer is a cancer of the glandular breast tissue. Worldwide, breast cancer is the fifth most common cause of cancer death (after lung cancer, stomach cancer, liver cancer, and colon cancer). In 2005, breast cancer caused 502,000 deaths (7% of cancer deaths; almost 1% of all deaths) worldwide. Among women worldwide, breast cancer is the most common cause of cancer death. The guidelines were based on studies of SERMs from the MORE, BCPT P-1, and Italian trials. In the MORE trial, the relative risk reduction for raloxifene was 76%. The P-1 preventative study demonstrated that tamoxifen can prevent breast cancer in high-risk individuals. The relative risk reduction was up to 50% of new breast cancers, though the cancers prevented were more likely estrogen-receptor positive (this is analogous to the effect of finasteride on the prevention of prostate cancer, in which only low-grade prostate cancers were prevented).The Italian trial showed benefit from tamoxifen. Selective Estrogen Receptor Modulators (SERMs) are a class of medication that acts on the estrogen receptor. A characteristic that distinguishes these substances from pure receptor agonists and antagonists is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues. Chalcones bearing non natural substituents have been synthesized during the recent years in order to develop drugs active against cancer. Chalcones are usually synthesized using the Claisen?Schmidt reaction in basic medium in polar solvent and purified by separation as the reaction led very often to a complex mixture. 2-Pyrazolines can be conveniently synthesized by the treatment of a, ß-unsaturated carbonyl compounds with hydrazine reagents in basic and acidic media. In this method, hydrazones are formed as intermediates, which can be subsequently cyclized to 2-Pyrazolines in the presence of a suitable cyclizing reagent like acetic acid. Pyrazoles act as agonists, which were re-examined using the ER-LBD-DES (agonist) structure. Spiro compounds represent an important class of naturally occurring substances characterized by highly pronounced biological properties.Spirooxindole ring systems are found in a number of alkaloids like horsifiline, spirotryprostatin and (+) elacomine. The derivatives of the Spirooxindole ring systems find wide biological applications as antimicrobial and antitumour agents.
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Last modified: 2012-09-24 23:10:01