DNA Fragmentation, Cell Cycle Arrest, and Docking Study of Novel Bis Spiro-cyclic 2-oxindole of Pyrimido[4,5-b]quinoline-4,6-dione Derivatives Against Breast Carcinoma

Mohamed, Magda F.; Abdelmoniem, Amr M.; Elwahy, Ahmed H. M.; Abdelhamid, Ismail A.

doi:10.2174/1568009617666170630143311

Cited by 49 publications

(29 citation statements)

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“…Due to their vast pharmacological profile, the nitrogen and sulfur‐containing heterocycles present an important class in the life science industry and drug research areas . Among them, urea derivatives constitute the core structural element of many biologically active molecules such as Sorafenib and larotrectinib (VITRAKVI) which has urea moiety in its structure as shown in Figure .…”

Section: Introductionmentioning

confidence: 99%

Facile Synthesis, Structural Activity Relationship, Molecular Modeling and In Vitro Biological Evaluation of New Urea Derivatives with Incorporated Isoxazole and Thiazole Moieties as Anticancer Agents

2019

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A new series of isoxazolyl and thiazolyl urea derivatives was synthesized, fully characterized and evaluated in vitro as anticancer agents. The chemistry involves a facile protocol for the preparation of urea derivatives 12–22 through the reaction of isocyanates (p‐tolylsulfonyl isocyanate, p‐tolyl isocyanate, benzoyl isocyanate and ethylisocyanate) 8–11 with the corresponding aminoisoxazoles and aminothiazoles 2, 3, 6 and 7. The cytotoxicity of the synthesized compounds 12–22 were evaluated using human lung adenocarcinoma cell line (A549), cervical cancer cell line (HeLa), and breast cancer cell line (MCF7). All novel compounds (except compounds 12, 17, and 18) were potential cytotoxic against lung cancer as it displayed IC50s less than the reference drug (5‐Fluro uracil (5FU)). All tested compounds (except 15 and 19) showed strong inhibition of breast cancer cell line even much better than the 5FU. The tested compounds were less cytotoxic against cervical cancer except compounds 16, 19, 20, and 21. The molecular docking studies of the synthesized compounds against the three different proteins Janus kinase 2 (JAK2), cyclin dependent kinase‐2 (CDK2), and B‐cell lymphoma‐2 (BCL2) that are major proteins involved in pathogenesis of cancer were discussed. The molecular‐docking analyses revealed that compounds 13, 14 and 20 were the best docked ligand compared to reference docked ligands against the tested targeted proteins. In conclusion, the urea derivatives 13 and 14 were the most promising compounds with lowest IC50s against the tested cancer cell lines, and they displayed the lowest binding energies, critical hydrogen bonds and hydrophobic interactions with the molecular targets compared to other tested compounds.

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Section: Introductionmentioning

confidence: 99%

Facile Synthesis, Structural Activity Relationship, Molecular Modeling and In Vitro Biological Evaluation of New Urea Derivatives with Incorporated Isoxazole and Thiazole Moieties as Anticancer Agents

2019

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“…Motivated by these findings and in conjunction with our ongoing research work on bis(heterocycles) as well as poly(heterocycles) , we report herein on the synthesis of novel bis(substituted pyrazole) derivatives starting from novel bis(ketene‐ N , S ‐acetals).…”

Section: Introductionmentioning

confidence: 92%

Novel Bis(2‐cyanoketene‐S,S‐/S,N‐acetals): Versatile Precursors for Novel Bis(aminopyrazole) Derivatives

Hebishy

Elgemeie

Elwahy

2019

Journal of Heterocyclic Chem

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A synthesis of novel bis(aminopyrazoles) by the reaction of hydrazine hydrate with the appropriate bis(2‐cyanoketene‐S,N‐acetals) was reported. The latter compounds were prepared by treatment of bis(cyanoacetamides) with phenyl isothiocyanate in KOH/EtOH and subsequent alkylation with methyl iodide. The utility of bis(2‐cyanoketene‐S,S‐acetals) as building blocks for novel bis(aminopyrazoles) was also investigated.

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“…Mohamed et al reported a novel synthesis of bis spiro‐cyclic 2‐oxindole derivatives of pyrimido[4,5‐ b ]quinolone tetraone derivatives 148 by the reaction of bis‐isatin 42 , dimidone 72 , and 6‐aminouracil 67 in acetic acid (Scheme ).…”

Section: Synthesis Of Fused Tricyclic Systemmentioning

confidence: 99%

Synthesis of heterocyclic compounds via Michael and Hantzsch reactions

Abdella

Abdelmoniem

Abdelhamid

et al. 2020

Journal of Heterocyclic Chem

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Heterocycles represent the largest diversity of organic compounds with signifcant chemical, biomedical, and industrial applications. They exist in numerous natural products, dyes, and as scaffolds in diverse drugs and related pharmaceutically active substances. Substantial attention has been paid to develop various elegant methods to synthesize heterocycles. Among different strategies, Michael and Hantzsch reactions are considered as effective approaches for construction of heterocycles and their corresponding fused derivatives. This review covers this area especially in the last 10 years. The heterocyclic systems reported in this review are classified according to the kind of the heterocyclic systems.

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DNA Fragmentation, Cell Cycle Arrest, and Docking Study of Novel Bis Spiro-cyclic 2-oxindole of Pyrimido[4,5-b]quinoline-4,6-dione Derivatives Against Breast Carcinoma

Cited by 49 publications

References 0 publications

Facile Synthesis, Structural Activity Relationship, Molecular Modeling and In Vitro Biological Evaluation of New Urea Derivatives with Incorporated Isoxazole and Thiazole Moieties as Anticancer Agents

Facile Synthesis, Structural Activity Relationship, Molecular Modeling and In Vitro Biological Evaluation of New Urea Derivatives with Incorporated Isoxazole and Thiazole Moieties as Anticancer Agents

Novel Bis(2‐cyanoketene‐S,S‐/S,N‐acetals): Versatile Precursors for Novel Bis(aminopyrazole) Derivatives

Synthesis of heterocyclic compounds via Michael and Hantzsch reactions

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