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Synthesis and discovery of molecular mechanisms of some novel conjugated unsaturated ketones designed as anticancer agents

Grant number: 18/50008-1
Support type:Regular Research Grants
Duration: July 01, 2018 - June 30, 2020
Field of knowledge:Biological Sciences - Biochemistry
Cooperation agreement: Consortium of Alberta, Laval, Dalhousie and Ottawa (CALDO)
Principal Investigator:Mozart de Azevedo Marins
Grantee:Mozart de Azevedo Marins
Principal investigator abroad: Jonathan Richard Dimmock
Institution abroad: University of Saskatchewan (USASK), Canada
Home Institution: Universidade de Ribeirão Preto (UNAERP). Campus Ribeirão Preto. Ribeirão Preto, SP, Brazil
Associated research grant:17/03237-2 - Bioscreening of polyphenols with anticancer activity and investigation of the molecular mechanisms involving the p53 transcription factor, AP.R

Abstract

A number of candidate anticancer agents have been designed and discovered in the laboratory of Professor Dimmock. These compounds display potent inhibitory effects on cell proliferation or are lethal to tumours. It is important to find the modes of action of representative lead molecules. The research group of Professor Marins has considerable experience in finding the ways in which cytotoxin exert their effects. When this information is to hand, then analogs may be discovered keeping in mind the shape and electronic properties of the molecular targets. The goal is that these compounds can be constructed with greater interaction of the drug molecule with the target enzyme or gene. The focus of this proposal is therefore to find compounds which have some (ideally all) of the following characteristics which (I) display greater toxicity to tumours than non-malignant cells (II) have low in vivo toxicity (III) possess desirable physicochemical properties and (IV) tumours are not resistant to them. (AU)