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Synthesis of Dihydropyranones, evaluation of the inhibitory activity of CDC25 and cytotoxicity in tumor cells and structural studies

Grant number: 11/00457-5
Support Opportunities:Scholarships in Brazil - Post-Doctorate
Effective date (Start): May 01, 2011
Effective date (End): April 30, 2014
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Organic Chemistry
Principal Investigator:Ronaldo Aloise Pilli
Grantee:Vânia Maria Teixeira Carneiro
Host Institution: Instituto de Química (IQ). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil


The project aims the preparation of homologues of the natural product RK-682, isolated from Streptomyces strain 88-682, which is a potent inhibitor of the protein phosphatase CDC25B. The preparation of five diferent analogues of RK-682 will be carried out in racemic form for the evaluation of their CDC25 inhibitory activities and their cytotoxic activities against a panel of nine human cancer cell strains. The results will be compared with those obtained using RK-682 as positive control and the interaction enzyme-substrate will be studied by computacional methods as well as attempts to co-crystallizate the complex enzyme-substrate for X-ray studies. The most promissing analogues will be also prepared in enantiomerically pure form for evaluation of the two enantiomers in the inhibition of phosphatase CDC25.

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Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
PILLI, RONALDO ALOISE; TONETO NOVAES, LUIZ FERNANDO; TEIXEIRA CARNEIRO, VANIA MARIA; DREKENER, ROBERTA LOPES; AVILA, CAROLINA MARTINS. Total Synthesis of Natural Dihydropyranones: A Contribution to the Structural Elucidation of Natural Products. Coibacins A and B, Cryptomoscatones D1, D2 and E3. CURRENT ORGANIC SYNTHESIS, v. 12, n. 5, p. 523-529, . (11/00457-5, 09/51602-5, 10/08673-6)
CARNEIRO, VANIA M. T.; AVILA, CAROLINA M.; BALUNAS, MARCY J.; GERWICK, WILLIAM H.; PILLI, RONALDO A.. Coibacins A and B: Total Synthesis and Stereochemical Revision. Journal of Organic Chemistry, v. 79, n. 2, p. 630-642, . (11/00457-5, 09/51602-5, 10/08673-6)
CARNEIRO, VANIA M. T.; TRIVELLA, DANIELA B. B.; SCORSATO, VALERIA; BERALDO, VIVIANE L.; DIAS, MARIANA P.; SOBREIRA, TIAGO J. P.; APARICIO, RICARDO; PILLI, RONALDO A.. Is RK-682 a promiscuous enzyme inhibitor? Synthesis and in vitro evaluation of protein tyrosine phosphatase inhibition of racemic RK-682 and analogues. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v. 97, p. 42-54, . (11/00457-5, 10/17544-5, 09/51602-5, 13/07607-8)

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