Kinase inhibition

Vollenhoven, Ronald F. van

doi:10.1016/b978-0-323-09138-1.00064-4

Cited by 3 publications

(2 citation statements)

References 30 publications

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“…There are about 90s enzymes named as Protein Tyrosine Kinases (PTKs) and which have been identified as having crucial roles in cells, including controlling cell proliferation, differentiation, and morphogenesis. 1 Protein Tyrosine Kinases (PTKs) come in a variety of forms, with RTKs (Receptor Tyrosine Kinases) and NRTKs (Non-receptor Tyrosine Kinases) being two of the more well-known examples (NRTKs). Examples of RTKs and NRTKs include insulin receptors and Growth Factor Receptors (GFRs) such as Epidermal Growth Factor Receptor (EGFR) and A Basic kinase Ligand 1 (ABL1).…”

Section: Introductionmentioning

confidence: 99%

“…The exploration of the fact that TK was involved in CML, this has led to the studies on several small molecules which results in identification and optimization leading to imatinib (1). Imatinib, is marketed as Gleevec or Glivec (by Novartis), is an effective oral chemotherapeutic medication for cancer treatment, and earliest drug effective in PTK BCR-ABL1 mediated cancers.…”

Section: Introductionmentioning

confidence: 99%

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Antiproliferative Activity of Novel Imatinib Analogue as Potential Anticancer Agents, Synthesis and in vitro Screening

Sangwan¹,

Singh²

2023

Ind. J. Pharm. Edu. Res

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Background: A series of N-(2,5-dimethylphenyl)-4-pyridin-3-ylpyrimidin-2-amine derivatives were synthesized as Imatinib derivatives, bearing 2-chloroquinoline as a heteroaryl motif. Materials and Methods:The compounds were synthesized by reducing in situ prepared azomethine intermediate using NaBH4 as a reducing agent in methanol as a solvent. Fourier transformation-IR, proton-NMR along with mass spectrometry were used to determine the structures of the compounds. The antiproliferative activity of the compounds against cell lines A549 and MCF7 was evaluated in vitro using the MTT assay protocol. Results: The compounds showed moderate cell growth inhibition at a concentration of 10 µM. Among the test compounds, the compound with a dimethoxy group at the 6 and 8 positions of the 2-chloroquinoline ring displayed the highest antiproliferative activity. Conclusion: The synthesized Imatinib derivatives exhibited moderate antiproliferative activity against A549 and MCF7 cell lines, and the compound with a dimethoxy group at the 6 and 8 positions of the 2-chloroquinoline ring showed the highest activity. These findings suggest that further studies can be performed to optimize the antiproliferative activity of these compounds.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Antiproliferative Activity of Novel Imatinib Analogue as Potential Anticancer Agents, Synthesis and in vitro Screening

Sangwan¹,

Singh²

2023

Ind. J. Pharm. Edu. Res

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New Imatinib Derivatives with Antiproliferative Activity against A549 and K562 Cancer Cells

et al. 2022

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Tyrosine kinase enzymes are among the primary molecular targets for the treatment of some human neoplasms, such as those in lung cancer and chronic myeloid leukemia. Mutations in the enzyme domain can cause resistance and new inhibitors capable of circumventing these mutations are highly desired. The objective of this work was to synthesize and evaluate the antiproliferative ability of ten new analogs that contain isatins and the phenylamino-pyrimidine pyridine (PAPP) skeleton, the main pharmacophore group of imatinib. The 1,2,3-triazole core was used as a spacer in the derivatives through a click chemistry reaction and gave good yields. All the analogs were tested against A549 and K562 cells, lung cancer and chronic myeloid leukemia (CML) cell lines, respectively. In A549 cells, the 3,3-difluorinated compound (3a), the 5-chloro-3,3-difluorinated compound (3c) and the 5-bromo-3,3-difluorinated compound (3d) showed IC50 values of 7.2, 6.4, and 7.3 μM, respectively, and were all more potent than imatinib (IC50 of 65.4 μM). In K562 cells, the 3,3-difluoro-5-methylated compound (3b) decreased cell viability to 57.5% and, at 10 µM, showed an IC50 value of 35.8 μM (imatinib, IC50 = 0.08 μM). The results suggest that 3a, 3c, and 3d can be used as prototypes for the development of more potent and selective derivatives against lung cancer.

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Management of rheumatoid arthritis: Impact and risks of various therapeutic approaches

Negrei

Bojincă

Bălănescu

et al. 2016

Experimental and Therapeutic Medicine

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Rheumatic diseases are highly prevalent chronic disorders and the leading cause of physical disability worldwide, with a marked socio-economic impact. Rheumatoid arthritis (RA) is a chronic systemic inflammatory disease of unknown etiology with an autoimmune pathogenesis, characterised by arthropathy with chronic, deforming, destructive evolution and multiple systemic manifestations. The management of RA has undergone significant changes as far as objectives and approaches are concerned, ending in the current strategy known as ‘treat to target’. The therapeutic array of RA includes several categories of medicinal products, of varying potential. There are several criteria for the classification of medicinal products used against this disease, one of the most important and modern of which divides such substances according to their effects on the progress of the disease: symptom-modifying antirheumatic drugs (including non-steroidal anti-inflammatory drugs and corticoids), disease-modifying antirheumatic drugs (including various substances, such as gold salts, antimalarials, sulfasalazine, D-penicillamine; non-specific immunosuppressive medication, such as methotrexate, cyclophosphamide, azathioprine and leflunomide) and biological therapy is a recent addition, providing new insight into the treatment of this disease. The selection of the optimal therapy for RA should be based on guidelines and recommendations, but also on clinical particular aspects and patient preferences.

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Kinase inhibition

Cited by 3 publications

References 30 publications

Antiproliferative Activity of Novel Imatinib Analogue as Potential Anticancer Agents, Synthesis and in vitro Screening

Antiproliferative Activity of Novel Imatinib Analogue as Potential Anticancer Agents, Synthesis and in vitro Screening

New Imatinib Derivatives with Antiproliferative Activity against A549 and K562 Cancer Cells

Management of rheumatoid arthritis: Impact and risks of various therapeutic approaches

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