Synthesis and investigation of new crystalline forms of antineoplastic agents

• Grant number: 21/03640-7
• Support Opportunities: Regular Research Grants
• Start date: December 01, 2021
• End date: November 30, 2023
• Field of knowledge: Physical Sciences and Mathematics - Physics - Condensed Matter Physics
• Principal Investigator: Fabio Furlan Ferreira
• Grantee: Fabio Furlan Ferreira
• Host Institution: Centro de Ciências Naturais e Humanas (CCNH). Universidade Federal do ABC (UFABC). Santo André , SP, Brazil
• City of the host institution: Santo André
• Associated researchers: Cristiane Cabral de Melo ; Fernando Luiz Affonso Fonseca ; Francesco Punzo ; Paula Silvia Haddad Ferreira
• Associated research grant(s): 23/01502-1 - Synthesis, characterization, and solubility study of new crystalline forms of antineoplastic agents, AP.R

Abstract

This project's primary goal is to optimize the antineoplastic drug melphalan's performance and the lead compound LASSBio-1735 by developing new crystalline forms and drug release methods. Since melphalan - an antineoplastic drug used to treat breast and ovarian cancer and multiple myeloma - has no known crystal structure, the first stage of this project and, consequently, the first result to be obtained will be the determination of its crystal structure. The analysis of the crystal structure and the packing of melphalan as well as LASSBio-1735 - an N-acylhydrazone derivative that has displayed in vitro antiproliferative activity against HL-60 (human leukemia), SF-295 (human glioblastoma), MDA-MB435 (melanoma), and HCT-8 (ileocecal adenocarcinoma) tumor cells - will be the basis for the synthesis and investigation of the physicochemical properties of the new crystalline forms (salts, hydrates, solvates, and/or co-crystals). This project also aims to synthesize and functionalize magnetite nanoparticles for the controlled release of antineoplastic compounds. The evaluation of antineoplastic action will be carried out based on the relationship between the gene expression of inflammatory markers and oxidative stress, tumor growth, and toxicity assessment. For this, Balb/c mice will be used, inoculated with Ehrlich tumor cells. These animals will be treated in different periods and groups. (AU)

Scientific publications

(8)

(The scientific publications listed on this page originate from the Web of Science or SciELO databases. Their authors have cited FAPESP grant or fellowship project numbers awarded to Principal Investigators or Fellowship Recipients, whether or not they are among the authors. This information is collected automatically and retrieved directly from those bibliometric databases.)

PINHEIRO, LUCAS BARBOZA MOREIRA; TAO, SONGSHENG; CULBERTSON, ELIZABETH; DE ARAUJO, GABRIEL LIMA BARROS; BILLINGE, SIMON J. L.; FERREIRA, FABIO FURLAN. Evaluation of the polymorphic forms of ritonavir and lopinavir in raw materials and co-milled systems. International Journal of Pharmaceutics, v. 628, p. 9-pg., 2022-10-28. (17/16499-5, 21/03640-7)

DA SILVA, JULIANA PEREIRA; BATISTA, CARIN CRISTINA DA SILVA; SCHUMACHER, MARIA LUCIA; RODRIGUEZ, SANTIAGO; TALEVI, ALAN; HADDAD, PAULA; CASTRO, GUILLERMO RAUL; FERREIRA, FABIO FURLAN. Crystal Structure of Melphalan Hydrochloride and Its Association with Caffeine Improves Its Antineoplastic Action. ACS OMEGA, v. 10, n. 20, p. 13-pg., 2025-05-15. (23/14132-8, 21/03640-7, 23/01502-1)

O'NEILL, NICHOLE; LIMA, THAMIRES A.; FERREIRA, FABIO FURLAN; ALVAREZ, NICOLAS J.; SCHWEITZER-STENNER, REINHARD. Determining the nanostructure and main axis of gly-his-gly fibrils using the amide I' bands in FTIR, VCD, and Raman spectra. SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY, v. 306, p. 16-pg., 2023-11-11. (21/03640-7)

MORAIS, ELIANE A.; CATURELLO, NAIDEL A. M. S.; LEMES, MAYKON A.; FERREIRA, HENRIQUE; FERREIRA, FABIO F.; ACUNA, JOSE J. S.; BROCHSZTAIN, SERGIO; DALPIAN, GUSTAVO M.; SOUZA, JOSE A.. Rashba Spin Splitting Limiting the Application of 2D Halide Perovskites for UV-Emitting Devices. ACS APPLIED MATERIALS & INTERFACES, v. 16, n. 3, p. 10-pg., 2024-01-13. (21/03640-7, 20/11560-0, 23/10982-7, 19/21656-8, 23/08771-8, 21/11446-6, 21/14422-0)

FERREIRA, FABIO F.; PEREIRA, ALINE P. C.; REIS, IANNY B.; SASAKI, BIANCA R. S.; FAVARO, WAGNER J.; DURAN, NELSON. Quantitative phase analysis of commercial ammonium phosphates by PXRD for application in biological systems. Powder Diffraction, v. N/A, p. 12-pg., 2023-05-18. (18/10052-1, 20/03419-6, 21/03640-7)

BARBOSA, KARLA KARINY F.; ARISTIZABAL-GIRALDO, DEISY; OSORIO-GUILLEN, JORGE M.; ACUNA, JOSE JAVIER S.; FERREIRA, FABIO F.. Green-chemistry synthesis and optical properties of lead-free Cs₂AgSbCl₆ double perovskite by a mechanochemical method. RSC MECHANOCHEMISTRY, v. 1, n. 1, p. 9-pg., 2024-03-12. (23/01502-1, 21/03640-7)

MELO, BARBRA POLY-ANNA VERA; GREGORIO JUNIOR, DENIS FERNANDO; DE OLIVEIRA, MATHEUS TROILO; TRINDADE, FABIANE DE JESUS; VAN DE STREEK, JACCO; FERREIRA, FABIO FURLAN; BROCHSZTAIN, SERGIO. Synthesis and Characterization of Two Novel Naphthalenediimide/Zinc Phosphonate Crystalline Materials Precipitated from Different Solvents. ACS OMEGA, v. 9, n. 1, p. 9-pg., 2023-12-20. (16/05496-2, 21/03640-7, 23/08771-8)

BEZZON, VINICIUS DANILO NONATO; CATURELLO, NAIDEL ANTONIO MOREIRA DOS SANTOS; DALPIAN, GUSTAVO MARTINI; FERREIRA, FABIO FURLAN. Crystal structure determination and DFT analysis of doxorubicin hydrochloride for controlled-release drug formulations. Journal of Molecular Structure, v. 1294, p. 7-pg., 2023-08-17. (21/03640-7, 18/11990-5)