Abstract
This research proposal aims the preparation and unambiguous structural characterization of about 100 natural and synthetic organic compounds belonging to the δ-lactone and δ-lactam families (mostly, α, β-unsaturated ones), butenolide diterpenes, 1,4-quinones of the caulibugulone family and (β-hydroxy-α-methylenic esters together with their biological evaluation against: i) a panel of nine human cancer cell lines (lung/NCI-H460; breast/MCF-7; ovary/OVCAR-3; ovary with resistance to adriamycin/NCI-ADR/Res; colon/HT-29; prostate/PC-3; melanoma/UACC-62; kidney/786-0 and leukemia/K-562); ii) as fosfatase inhibitors (CD45, SHP2, LMWPTP, CDC25 and PTP1B, PPl, PP2A e PP2B) and, iii) their effect on the interaction of Hsp70 and Hsp90 human proteins with their client co-chaperones and protein clients and on the ATPase activity. The proposal is based on preliminary biological evaluation of some representatives of the structural classes proposed to be investigated in this study and the research team is composed by investigators with solid background in the areas of Synthetic Organic Chemistry, structural elucidation by X-ray diffraction analysis, pharmacological evaluation and enzimatic activity determination, and more than 10 students, who will contribute with their expertise to acquire a coherent body of information from their experimental work in order to identify lead compounds and their mode of action which will allow the design of new compounds with better profile for further in vivo biological evaluation. (AU)
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