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1.
Curr Drug Deliv ; 2023 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-37818568

RESUMO

The majority of deadly cancers that afflict the female reproductive system occur in the ovary. Around 1,40,000 women worldwide die from ovarian cancer each year, making it the sixth most common cancer-associated deceases among females in the United States. Modern, cutting-edge treatments like chemotherapy and surgery frequently produce full remissions, but the recurrence rate is still very high. When this crippling condition is diagnosed, there are frequently few therapeutic choices available because of how quietly it manifests. Healthcare practitioners must have a fundamental grasp of the warning signs and symptoms of ovarian cancer, as well as the imaging techniques and treatment choices available, to give the patient the best care possible. The discipline of medical nanotechnology has gained a lot of momentum in recent years in resolving issues and enhancing the detection and treatment of different illnesses, including cancer. This article gives a brief summary of types, risk factors and approaches to ovarian cancer treatment. We subsequently discussed the pathophysiology of ovarian cancer with the risk factors. This review also emphasizes the various signalling pathways involved in ovarian cancer. Our comprehensive integration of recent findings in fundamental research in the nano arena reveals the strong interest in these nanomedicines in ovarian cancer treatment. However, these nanomedicines still require more research, as indicated by the comparatively small number of clinical trials ongoing. This article will provide a reference for ovarian cancer treatment.

2.
Mini Rev Med Chem ; 18(4): 369-379, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-28486908

RESUMO

BACKGROUND: Different 3-aroylpropionic acids and dihydropyrimidine hydrazine derivatives were condensed together to yield a series of dihydropyrimidine and pyridazinone hybrids (5a-u). OBJECTIVE: This was done in order to develop therapeutic agents for the treatment of breast cancer with improved Cycloxygenase-2 (COX-2) selectivity. In-vitro anticancer evaluation for these compounds was done against human breast cancer cell lines (MCF-7, MDA-MB-231) and normal human keratinocytes (HaCaT). CONCLUSION: Amongst all the developed analogs, compound 5l emerged as the most potent agent against both these cell lines with IC50 values of 3.43 and 2.56 µM respectively. The synthesized compounds were also evaluated for COX-2 selectivity. To observe the binding pattern of the compounds with COX-2, a docking study was performed using PDB ID: 1CX2.


Assuntos
Antineoplásicos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Inibidores de Ciclo-Oxigenase 2/farmacologia , Ciclo-Oxigenase 2/metabolismo , Piridazinas/farmacologia , Pirimidinas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Neoplasias da Mama/patologia , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Inibidores de Ciclo-Oxigenase 2/síntese química , Inibidores de Ciclo-Oxigenase 2/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Modelos Moleculares , Estrutura Molecular , Piridazinas/síntese química , Piridazinas/química , Pirimidinas/síntese química , Pirimidinas/química , Relação Estrutura-Atividade
3.
Acta Pharm ; 59(4): 441-51, 2009 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-19919933

RESUMO

Various N-(5-chloro-6-substituted-benzothiazol-2-yl)-N'-(substituted phenyl)-[1,3,4]thiadiazole-2,5-diamines (5a-t) were designed and synthesized starting from substituted acetophenones. Structures of all the compounds were confirmed on the basis of spectral and elemental analyses. All the newly synthesized compounds were screened for their anticonvulsant activity and were compared with the standard drug phenytoin sodium. Interestingly, all the compounds showed protections against seizures in the range 50-100% indicative of the promising nature of the compounds against seizure spread. Compounds 5b and 5c showed complete protection against MES induced seizures.


Assuntos
Anticonvulsivantes/química , Anticonvulsivantes/farmacologia , Tiadiazóis/química , Tiadiazóis/farmacologia , Acetofenonas , Animais , Anticonvulsivantes/síntese química , Avaliação Pré-Clínica de Medicamentos , Camundongos , Convulsões/tratamento farmacológico , Tiadiazóis/síntese química
4.
J Enzyme Inhib Med Chem ; 24(6): 1344-50, 2009 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-19912067

RESUMO

A number of new 8-substituted-4-(2/4-substituted phenyl)-2H-[1,3,5]triazino[2,1-b][1,3]benzothiazole-2-thiones (4a-t) were synthesized and evaluated for their anticonvulsant, anti-nociceptive, hepatotoxic, and neurotoxic properties. The titled compounds (4a-t) were obtained by cyclization of N-{[6-substituted-1,3-benzothiazol-2-yl)amino]carbonothioyl}-2/4-substituted benzamides (3a-t) by refluxing in n-butanol. All the newly synthesized compounds were screened for their anticonvulsant activity in a mouse seizure model and were compared with the standard drug phenytoin. Compounds 4a, 4c, 4f, and 4l showed complete protection after time periods of 0.5 h and 4 h. Some of the selected compounds were evaluated for their neurotoxic and hepatotoxic effects, and none of these showed any sign of neurotoxicity or hepatotoxicity. Compounds 4a-t were also evaluated for their anti-nociceptive activity by a thermal stimulus technique using diclofenac as standard. Compounds 4o, 4q, and 4t displayed highly potent analgesic activity with p < 0.01.


Assuntos
Analgésicos/síntese química , Analgésicos/uso terapêutico , Anticonvulsivantes/síntese química , Anticonvulsivantes/uso terapêutico , Tiadiazóis/síntese química , Tiadiazóis/toxicidade , Tionas/síntese química , Tionas/toxicidade , Analgésicos/toxicidade , Animais , Anticonvulsivantes/toxicidade , Avaliação Pré-Clínica de Medicamentos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Camundongos , Síndromes Neurotóxicas/patologia , Fenitoína/síntese química , Fenitoína/uso terapêutico , Fenitoína/toxicidade , Convulsões/tratamento farmacológico , Convulsões/metabolismo , Convulsões/patologia , Espectroscopia de Infravermelho com Transformada de Fourier , Tiadiazóis/uso terapêutico , Tionas/uso terapêutico , Fatores de Tempo
5.
Eur J Med Chem ; 43(5): 1114-22, 2008 May.
Artigo em Inglês | MEDLINE | ID: mdl-17826870

RESUMO

A series of 1,3-benzothiazol-2-yl benzamides (11-30) were prepared in satisfactory yield and evaluated for their anticonvulsant, neurotoxicity, CNS depressant study and other toxicity studies. All the synthesized compounds were in good agreement with elemental and spectral data. Majority of the compounds were active in MES and scPTZ screen and showed the decrease in the immobility time. None of the compounds had shown neurotoxicity or liver toxicity.


Assuntos
Anticonvulsivantes/síntese química , Benzamidas/síntese química , Benzotiazóis/síntese química , Depressores do Sistema Nervoso Central/síntese química , Sulfetos/síntese química , Animais , Anticonvulsivantes/farmacologia , Anticonvulsivantes/toxicidade , Benzamidas/farmacologia , Benzamidas/toxicidade , Benzotiazóis/farmacologia , Benzotiazóis/toxicidade , Depressores do Sistema Nervoso Central/farmacologia , Depressores do Sistema Nervoso Central/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Doença Hepática Induzida por Substâncias e Drogas/patologia , Doença Hepática Induzida por Substâncias e Drogas/fisiopatologia , Testes de Função Hepática , Masculino , Camundongos , Ratos , Ratos Wistar , Convulsões/tratamento farmacológico , Convulsões/etiologia , Relação Estrutura-Atividade , Sulfetos/farmacologia , Sulfetos/toxicidade
6.
Bioorg Med Chem Lett ; 17(15): 4178-82, 2007 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-17572089

RESUMO

A series of 1,3-benzothiazol-2-yl semicarbazones (1-15) were prepared in satisfactory yield and evaluated for their anticonvulsant, neurotoxicity and other toxicity studies. All the synthesized compounds were in good agreement with elemental and spectral data. Majority of the compounds were active in MES screen. Selected compounds were checked for their lipophilic character.


Assuntos
Anticonvulsivantes/síntese química , Semicarbazonas/síntese química , Animais , Anticonvulsivantes/química , Anticonvulsivantes/toxicidade , Avaliação Pré-Clínica de Medicamentos , Feminino , Fígado/efeitos dos fármacos , Fígado/patologia , Fígado/fisiologia , Masculino , Camundongos , Sistema Nervoso/efeitos dos fármacos , Semicarbazonas/química , Semicarbazonas/toxicidade
7.
Bioorg Med Chem Lett ; 17(1): 255-9, 2007 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-17046248

RESUMO

A series of sulphonamide derivatives (1-11) were synthesized in good yield and evaluated for their possible anticonvulsant activity and neurotoxic study. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. Majority of the compounds were active in MES and scPTZ tests. All the compounds were less toxic than the standard drug phenytoin.


Assuntos
Anticonvulsivantes/química , Anticonvulsivantes/farmacologia , Sulfonamidas/química , Animais , Anticonvulsivantes/síntese química , Interações Hidrofóbicas e Hidrofílicas , Masculino , Camundongos , Camundongos Endogâmicos , Ratos , Ratos Sprague-Dawley , Ratos Wistar , Sulfonamidas/síntese química , Sulfonamidas/farmacologia
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