Insight on a new indolinone derivative as an orally bioavailable lead compound against renal cell carcinoma

Fouad, Marwa A.; Zaki, M. T. M.; Lotfy, Raghda A.; Mahmoud, Walaa R.

doi:10.1016/j.bioorg.2021.104985

Cited by 15 publications

(12 citation statements)

References 91 publications

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“…Fouad et al [ 58 ] developed a series of isatine–4-thiazolidinone conjugates as potential antimitotic agents. Compound 59 ( Figure 23 ) was effective against colorectal cancer cell line KM12, melanoma cell line UACC-62, ovarian cancer cell line IGROV1, cancer cell line SK-OV-3, and renal cell carcinoma lines (A498, ACHN, CAKI-1, RXF393, and UO-31).…”

Section: Privileged Heterocyclic Scaffolds–4-thiazolidinones Hybrid M...mentioning

confidence: 99%

4-Thiazolidinone-Bearing Hybrid Molecules in Anticancer Drug Design

Roszczenko

Holota

Szewczyk

et al. 2022

IJMS

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Oncological diseases have currently reached an epidemic scale, especially in industrialized countries. Such a situation has prompted complex studies in medicinal chemistry focused on the research and development of novel effective anticancer drugs. In this review, the data concerning new 4-thiazolidinone-bearing hybrid molecules with potential anticancer activity reported during the period from the years 2017–2022 are summarized. The main emphasis is on the application of molecular hybridization methodologies and strategies in the design of small molecules as anticancer agents. Based on the analyzed data, it was observed that the main directions in this field are the hybridization of scaffolds, the hybrid-pharmacophore approach, and the analogue-based drug design of 4-thiazolidinone cores with early approved drugs, natural compounds, and privileged heterocyclic scaffolds. The mentioned design approaches are effective tools/sources for the generation of hit/lead compounds with anticancer activity and will be relevant to future studies.

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Section: Privileged Heterocyclic Scaffolds–4-thiazolidinones Hybrid M...mentioning

confidence: 99%

4-Thiazolidinone-Bearing Hybrid Molecules in Anticancer Drug Design

Roszczenko

Holota

Szewczyk

et al. 2022

IJMS

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“…Whereas Compound 5m with two electron-withdrawing groups (NO2 and Cl) in the benzene ring exhibited the lowest antioxidant activity with IC50 = 32. 43 Sava et al conducted synthesis of thiazolidin-4-one-indometacin hybrids and evaluated their antioxidant activity with use of DPPH radical scavenging method [21]. The most active derivatives from whole series were Compounds 7 and 8 with IC50 values 0.54 ± 0.01 and 1.82 ± 0.05 mM, respectively (Figure 3).…”

Section: Biological Activities Of Thiazolidin-4-ones 21 Antioxidant Activitymentioning

confidence: 99%

“…The IC50 values were at submicromolar concentration 452.53 nM (VEGFR-2), 280.916 nM (PDGFRα) and 45.013 nM (PDGFRβ). In the case of PDGFRβ, enzyme activity was better than sunitinib (IC50 = 55 nM) [43].…”

mentioning

confidence: 97%

The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies

Mech

Kurowska

Trotsko

2021

IJMS

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Thiazolidin-4-ones is an important heterocyclic ring system of a pharmacophore and a privileged scaffold in medicinal chemistry. This review is focused on the latest scientific reports regarding biological activities of thiazolidin-4-ones published in 2020 and 2021. The review covers recent information about antioxidant, anticancer, anti-inflammatory, analgesic, anticonvulsant, antidiabetic, antiparasitic, antimicrobial, antitubercular and antiviral properties of thiazolidin-4-ones. Additionally, the influence of different substituents in molecules on their biological activity was discussed in this paper. Thus, this study may help to optimize the structure of thiazolidin-4-one derivatives as more efficient drug agents. Presented information may be used as a practical hint for rational design of new small molecules with biological activity, especially among thiazolidin-4-ones.

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“…These include, but are not limited to, sunitinib ( 1 ), vandetanib ( 2 ), lenvatinib ( 3 ), and sorafenib ( 4 ). [ 24–30 ]…”

Section: Introductionmentioning

confidence: 99%

New quinoxalin‐2(1H)‐one‐derived VEGFR‐2 inhibitors: Design, synthesis, in vitro anticancer evaluations, in silico ADMET, and docking studies

El‐Adl

Sakr

Yousef

et al. 2022

Archiv der Pharmazie

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More than 70% of cancer patients who are treated with chemotherapeutics do not show a durable response. As part of the global plan seeking new effective chemotherapeutics, here, we report the synthesis and in vitro and computational studies of new lenvatinib and sorafenib analog quinoxalines as vascular endothelial growth factor receptor II (VEGFR-2) tyrosine kinase inhibitors. The central quinolone and pyridine moieties of the Food and Drug Administration-approved anticancer agents lenvatinib and sorafenib were replaced with the versatile quinoxaline scaffold that has been exploited for developing potent cytotoxic agents. With some minor structural optimizations, all the other pharmacophoric features of lenvatinib and sorafenib were maintained. Accordingly, three new sets of quinoxalines were synthesized to evaluate their activity against liver, colorectal, and breast malignancies. The results obtained in the in vitro cytotoxicity evaluation study revealed the superior activity of three derivatives (20, 25, and 29) compared with that of doxorubicin and sorafenib. Absorption, distribution, metabolism, excretion, and toxicity (ADMET) profiling and docking of 20, 25, and 29 into the VEGFR-2 receptor were also performed. Results of in silico studies showed the potential of the designed compounds to bind effectively with a number of key residues. The obtained in vitro cytotoxic activity and ADMET profiles of compounds 20, 25, and 29 suggested that they should be subjected to further structural optimizations to develop new candidates in cancer treatment protocols.

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Insight on a new indolinone derivative as an orally bioavailable lead compound against renal cell carcinoma

Cited by 15 publications

References 91 publications

4-Thiazolidinone-Bearing Hybrid Molecules in Anticancer Drug Design

4-Thiazolidinone-Bearing Hybrid Molecules in Anticancer Drug Design

The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies

New quinoxalin‐2(1H)‐one‐derived VEGFR‐2 inhibitors: Design, synthesis, in vitro anticancer evaluations, in silico ADMET, and docking studies

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