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1.
Pharmaceutics ; 14(11)2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-36432650

RESUMO

Breast cancer is the most frequent cause of cancer death in women, representing the fifth leading cause of cancer death overall. Therefore, the growing search for the development of new treatments for breast cancer has been developed lately as well as drug delivery systems such as biocompatible metal-organic Frameworks (bio-MOFs). These may be promising and attractive for drug incorporation and release. The present study aims to develop a drug carrier system RCA (bioMOF-100 submitted to the activation process) containing incorporated curcumin (CCM), whose material surface is coated with folic acid molecules (FA) to promote the targeting of drug carrier systems to the tumor region. They were synthesized and characterized using several characterization techniques. The materials were submitted to drug encapsulation tests, whose encapsulation efficiency was 32.80% for CCM@RCA-1D. Using the 1H nuclear magnetic resonance (NMR) spectroscopy technique, it was possible to verify the appearance of signals referring to folic acid, suggesting success in the functionalization of these matrices. In vitro tests such as cell viability and type of cell death were evaluated in both series of compounds (CCM@RCA-1D, CCM@RCA-1D/FA) in breast tumor lines. The results revealed low toxicity of the materials and cell death by late apoptosis. Thus, these results indicate that the matrices studied can be promising carriers in the treatment of breast cancer.

2.
Eur J Med Chem ; 214: 113166, 2021 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-33550181

RESUMO

Metal-based drugs are privileged motifs that act as primary pharmacophores in bioactive compounds for various diseases, including tuberculosis (TB). This potentially life-threatening and extremely contagious infectious disease is caused by Mycobacterium tuberculosis (Mtb). In 2018, TB infected about 10 million people and caused 1.2 million deaths worldwide. A large number of ligands are promising scaffolds in drug design, including heterocyclic, phosphines, schiff bases, thio and semicarbazones, aliphatic amines, cyclopalladated, cyanometallates and miscellaneous. Moreover, several metal-based complexes have been studied for the treatment of numerous illnesses, including infectious diseases. To contribute to drug design, we identified the metal-based organometallic complexes against Mtb. Thus, in this review article, we analysed the recent contributions of metal-based scaffolds for design of new anti-Mtb drugs in the last decade (2011-2020). Besides, metal-based approaches will be presented in order to find out new antitubercular agents.


Assuntos
Antituberculosos/farmacologia , Descoberta de Drogas , Mycobacterium tuberculosis/efeitos dos fármacos , Compostos Organometálicos/farmacologia , Animais , Antituberculosos/síntese química , Antituberculosos/química , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Compostos Organometálicos/síntese química , Compostos Organometálicos/química
3.
Acta Crystallogr E Crystallogr Commun ; 71(Pt 3): o208-9, 2015 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-25844252

RESUMO

In the title compound, C12H15N3O2S, the 1,3-benzdioxole fragment is nearly planar [the maximum deviation being 0.0515 (14) Å], the N-N-C(=S)-N fragment is also nearly planar [the maximum deviation being 0.0480 (10) Å], and the dihedral angle between their mean planes is 23.49 (10)°. In the crystal, mol-ecules are linked by pairs of N-H⋯S hydrogen bonds, forming inversion dimers. The dimers are stacked along the a axis with neighbouring columns having the same direction; however, the mol-ecules show different orientations leading to a centrosymmetric arrangement. In the crystal, the methyl-ene group of the ethyl substituent and the terminal methyl H atoms are disordered over two sets of sites and were refined using a split model with an occupancy ratio of 0.5:0.5.

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