Rationale design of novel substituted 1,3,5-triazine candidates as dual IDH1(R132H)/ IDH2(R140Q) inhibitors with high selectivity against acute myeloid leukemia: In vitro and in vivo preclinical investigations

Bioorganic Chemistry, Год журнала: 2024, Номер 149, С. 107483 - 107483

Опубликована: Май 21, 2024

Язык: Английский

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Design and synthesis of novel chloropyridazine hybrids as promising anticancer agents acting by apoptosis induction and PARP-1 inhibition through a molecular hybridization strategy

RSC Medicinal Chemistry, Год журнала: 2024, Номер 15(3), С. 981 - 997

Опубликована: Янв. 1, 2024

Novel chloropyridazine hybrids as promising anticancer agents acting by apoptosis induction and PARP-1 inhibition through a molecular hybridization strategy.

Язык: Английский

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Synthesis of some new nanoparticles mixed metal complexes of febuxostat in presence of 2,2′-bipyridine: Characterization, DFT, antioxidant and molecular docking activities

Journal of Molecular Liquids, Год журнала: 2023, Номер 386, С. 122460 - 122460

Опубликована: Июнь 29, 2023

Язык: Английский

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Pyrazole, Pyrazoline, and Fused Pyrazole Derivatives: New Horizons in EGFR‐Targeted Anticancer Agents

Chemistry & Biodiversity, Год журнала: 2024, Номер 21(11)

Опубликована: Июль 26, 2024

Pyrazole and its derivatives remain popular heterocycles in drug research, design, development. Several drugs include the pyrazole scaffold, such as ramifenazone, ibipinabant, antipyrine, axitinib, etc. They have been extensively studied by scientific community are said to a wide range of biological activity, especially anticancer agents targeting EGFR. Overexpression EGFR signalling promotes tumor growth inhibiting apoptosis. dysfunction has described multiple cancers, including colon, head neck, NSCLC, liver, breast, ovarian cancer. As result, represents prospective target for cancer treatment. anti-EGFR thriving, notably dacomitinib, afatinib, erlotinib, gefitinib, osimertinib. However, almost all currently available limited therapeutic effectiveness due lack selectivity well substantial side effects. Furthermore, aberrant across numerous human malignancies/carcinomas is impeded gene amplification, protein overexpression, mutations, or in-frame deletions, making EGFR-induced treatment challenging. To overcome such, novel with high efficacy minimal toxicity required. battle resistance inhibitors, pyrazole, pyrazoline, their investigated viable pharmacophore development new better potency, lesser toxicity, favourable pharmacokinetic characteristics. The present investigation covers examination progress toward anti-cancer therapies via fused pyrazole-based compounds. current study also inclusive data on marketed candidates undergoing preclinical clinical Lastly, we discussed recent advances medicinal chemistry significance eradication various cancers provide direction structure-activity relationship (SAR), mechanistic studies.

Язык: Английский

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Antiangiogenic potential of phytochemicals from Clerodendrum inerme (L.) Gaertn investigated through in silico and quantum computational methods

Molecular Diversity, Год журнала: 2024, Номер 29(1), С. 215 - 239

Опубликована: Апрель 28, 2024

Язык: Английский

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