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Norcantharidin derivatives as inhibitors in the development of breast cancer drugs.

NORCANTHARIDIN DERIVATIVES AS INHIBITORS IN THE DEVELOPMENT OF BREAST CANCER DRUGS. DARSHIL M. PATEL, W.P. DAVIDSON HIGH SCHOOL, MOBILE, AL 36609. DAVID C. FORBES, DEPT. OF CHEMISTRY, UNIV. OF S. ALA., MOBILE, AL 36688

In recent studies, the overexpression of serine/threonine protein phosphatase 4 (PP4) and 5 (PP5) is associated with breast cancer. If PP4 or PP5 is inhibited, it is hypothesized that the cancer will be terminated. Through previous studies, it is known that the Norcantharidin, a derivative of the Cantharidin, inhibits 1 [micro]M of PP5; however, it is not selective towards PP5. If the active moiety of Fostriecin, which has shown to be an effective inhibitor of PP4 and a weak inhibitor of PP5, is appended to the Norcantharidin, then theoretically the Norcantharidin derivative should be selective towards PP4 and PP5. The synthesis of the target compound is achievable through a new reaction pathway that will effectively merge the Norcantharidin and Fostriecin to form a selective and potent inhibitor. Two methods for the chiral resolution of oxirane were tested to determine the optimal strategy. The hydrolytic kinetic resolution method and the water epoxidation method were tested through the reagent, 2-(4-chlorophenyl) oxirane. Three trials were conducted with the water epoxidation method. The percent yield for the three trials was 67%, 60%, and 65%.The study revealed that the water epoxidation method was more optimal due to its percent conversion, ecological factors, and reliance on inexpensive feedstock materials. If this method is adopted into the reaction pathway, the target compound should be capable of synthesis as supported by literature.

The Efficacy of Gold and Silver Nanoparticles for Skin Cancer Chemoprevention and Therapy. Rohan Palanki, W.P. Davidson High School, Mobile, AL 36608

The effect of size and concentration of gold and silver nanoparticles was tested for skin cancer chemoprevention and therapy. Results indicate that gold and silver nanoparticles in the size range 10-100 nm and concentration range 1-10 mg/L are not toxic to nontumerigenic HaCaT cells. Dot-blot assay and apoptosis results indicate that DNA damage due to UVB exposure is significantly reduced in the presence of silver nanoparticles in the size range 10-40 nm, thereby proving the chemopreventive effect of silver nanoparticles. On the other hand, gold nanoparticles do not show any chemopreventive effect in dot-blot assay studies. Cell cycle studies suggest that silver nanoparticles in the size range 10-40 nm arrest the cells at the first checkpoint prior to DNA duplication to facilitate repair of UVB-induced CPD formation. Toxicity studies indicate that while gold nanoparticles are not toxic to A431-NS epidermoid carcinoma skin cancer cells, silver nanoparticles in the size range 10-40 nm are toxic to A431-NS cells with cell viability ranging from 10-30%, thereby proving their therapeutic value for skin cancer. Western blot analysis confirmed that the expression of anti-apoptotic proteins decreased and the pro-apoptotic proteins increased in the presence of UV radiation. This expression was neutralized in the presence of 10 nm silver nanoparticles. Thus, while gold nanoparticles are not chemopreventive or therapeutic, silver nanoparticles have both a chemopreventive effect against UVB-induced damage and a therapeutic effect against skin cancer cells.

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Title Annotation:Gorgas Posters Competition
Author:Patel, Darshil M.
Publication:Journal of the Alabama Academy of Science
Article Type:Report
Date:Apr 1, 2015
Words:519
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