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1.
Nat Prod Res ; : 1-5, 2024 Sep 08.
Artigo em Inglês | MEDLINE | ID: mdl-39244773

RESUMO

Cancer is a complex and widespread disease affecting various organs and tissues, with an expected significant increase in reported cases. Current treatments like chemotherapy and radiation therapy have limited efficacy and adverse side effects. This study investigated the multi-target therapeutic potential of seven phytochemicals against critical cancer-associated proteins. Computational docking studies analysed the binding interactions between phytochemicals and proteins, supported by in-vitro experiments on cancer cell lines. Vero cells assessed cytotoxicity, and the A549 cancer cell line evaluated anticancer activity. Cytotoxicity assessment on Vero cells revealed concentration-dependent effects of phytochemicals. Anticancer activity evaluation on the A549 cell line demonstrated the ability of certain phytochemicals to inhibit cancer cell proliferation and induce apoptosis. Cancer, Therapeutic agents, Phytochemicals, Computational docking studies, In-vitro experiments, Cytotoxicity, Anticancer activity, Chemotherapy, Vero cells, A549 cell line, multi-targeted therapeutic potential, Critical cancer-associated proteins.

2.
Pharmaceuticals (Basel) ; 16(6)2023 May 29.
Artigo em Inglês | MEDLINE | ID: mdl-37375752

RESUMO

In this innovative research, a novel series of thiazolidin-4-one analogues having a 1,3,4-oxadiazole/thiadiazole moiety were derived and the structures of all the newly obtained molecules were established using different physicochemical and analytical means (1H-NMR, FTIR, mass spectra, and elemental analyses). The synthesized molecules were then investigated for their antiproliferative, antimicrobial, and antioxidant potential. The cytotoxicity screening studies revealed that analogues D-1, D-6, D-15, and D-16 possessed comparable efficacy, within the IC50 range (1 to 7 µM), when taking doxorubicin as a reference drug (IC50 = 0.5 µM). The antimicrobial activity was assessed using different Gram-(+) and Gram-(-) bacterial and fungal strains and the results revealed that molecules D-2, D-4, D-6, D-19, and D-20 possessed potent activity against selective strains of microbes with MIC ranges of 3.58 to 8.74 µM. The antioxidant evaluation was performed using the DPPH assay and the screening results revealed that analogue D-16 was the most potent derivative (IC50 = 22.3 µM) when compared with the positive control, ascorbic acid (IC50 = 111.6 µM). Structure-activity relationship (SAR) studies of the synthesized novel derivatives revealed that para-substituted halogen and hydroxy derivatives have remarkable potential against the MCF-7 cancer cell line and antioxidant potential. Similarly, electron-withdrawing groups (Cl/NO2) and -donating groups at the para position possess moderate to promising antimicrobial potential.

3.
Mini Rev Med Chem ; 22(6): 927-948, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34579634

RESUMO

Quinoxaline (C8H6N2), commonly called 1,4-diazanaphthalene, 1,4-benzodiazine, or benzopyrazine, is a very potent nitrogenous heterocyclic moiety consisting of a benzene ring fused with the pyrazine ring. A number of different methods for the synthesis of quinoxaline derivatives have been reported in the literature, but the most effective method, commonly used for the synthesis of quinoxaline analogues involves the condensation of substituted o-phenylenediamines with 1, 2- dicarbonyl compounds in the presence of different catalyst(s). The presence of different types of catalysts and their concentration affects the overall yield of the product. Quinoxaline not only plays an important role as an organic reaction intermediate but also has a wide spectrum of interesting biological activities viz. antibacterial, antifungal, anticancer, anti-inflammatory, antiviral, and antiprotozoal activity, etc. Some commercially available drug molecules containing quinoxaline moiety are echinomycin (as antibacterial, antineoplastic, and nucleic acid inhibitor), triostins (cyclic desipeptide as an antibacterial agent), dioxidine and mequindox (as antibacterial agents), carbadox (controlling swine dysentery), desoxycarbadox (as swine growth promoter) and panadipion (as hepatoprotective agent), etc. A large number of quinoxaline analogues possessing different biological activities and their synthetic procedures have been patented worldwide.


Assuntos
Antineoplásicos , Antiprotozoários , Animais , Antibacterianos/farmacologia , Antifúngicos , Antineoplásicos/química , Antineoplásicos/farmacologia , Quinoxalinas , Suínos
4.
Indian J Dermatol Venereol Leprol ; 84(4): 424-430, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29327698

RESUMO

Eruptive pseudoangiomatosis is a rare viral exanthem characterized by acute onset of hemangiomata-like lesions, however, histological findings are distinct from that of true angiomas. This entity has been reported from Europe, North America, Japan, and Korea till date. Here, we report 12 cases of eruptive pseudoangiomatosis from a tertiary care hospital in Punjab.


Assuntos
Angiomatose/complicações , Angiomatose/diagnóstico , Hemangioma/complicações , Hemangioma/diagnóstico , Neoplasias Cutâneas/complicações , Neoplasias Cutâneas/diagnóstico , Adolescente , Adulto , Angiomatose/virologia , Pré-Escolar , Feminino , Hemangioma/virologia , Humanos , Masculino , Pessoa de Meia-Idade , Neoplasias Cutâneas/virologia , Adulto Jovem
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