1,4,5,6,7,8-Hexahydroquinolines and 5,6,7,8-tetrahydronaphthalenes: A new class of antitumor agents targeting the colchicine binding site of tubulin

Shaheen, Mennatallah A.; El-Emam, Ali A.; El‐Gohary, Nadia S.

doi:10.1016/j.bioorg.2020.103831

Cited by 6 publications

(2 citation statements)

References 64 publications

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“…Numerous studies demonstrate that tubulin polymerization inhibitors are capable of inducing cellular apoptosis [35,36]. To evaluate the mode of cell death induced by 19h, Annexin-V/PI assay was used.…”

Section: Apoptosis Quantification In Mcf-7 Cellsmentioning

confidence: 99%

Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity

et al. 2020

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A novel series of quinoline derivatives of combretastatin A-4 incorporating rigid hydrazone and a cyclic oxadiazole linkers were synthesized and have demonstrated potent tubulin polymerization inhibitory properties. Many of these novel derivatives have shown significant antiproliferative activities in the submicromolar range. The most potent compound, 19h, demonstrated superior IC50 values ranging from 0.02 to 0.04 µM against four cancer cell lines while maintaining low cytotoxicity in MCF-10A non-cancer cells, thereby suggesting 19h’s selectivity towards proliferating cancer cells. In addition to tubulin polymerization inhibition, 19h caused cell cycle arrest in MCF-7 cells at the G2/M phase and induced apoptosis. Collectively, these findings indicate that 19h holds potential for further investigation as a potent chemotherapeutic agent targeting tubulin.

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Section: Apoptosis Quantification In Mcf-7 Cellsmentioning

confidence: 99%

Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity

et al. 2020

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“…The known phenothiazine and anthracene compounds like C5-PTZ, C5-PTZA, and ANTCN were synthesized using reported procedures. 15,16 C5-PTZCN, C5-PTZDCA, and ANTDCA are the compounds that were newly synthesized. Their structures were veried by FT-IR, LCMS (Liquid Chromatography Mass Spectrometry)/HRMS (High-Resolution Mass Spectrometry), and 1 H and 13 C NMR data (see ESI; pages (3)(4)(5)(6) and Fig. (S11-S16) †).…”

Section: Methodsmentioning

confidence: 99%

Binding interactions and FRET between bovine serum albumin and various phenothiazine-/anthracene-based dyes: a structure–property relationship

et al. 2021

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Design, Synthesis and Molecular Docking of Chalcone Derivatives as Potential Anticancer Agents

2021

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Twenty derivatives of chalcones were synthesized and their anticancer activities were estimated against both breast and liver cancer besides two human normal cell lines. Out of our candidates, there were five compounds 3 b, 3 d, 3 h, 7 and 10 b that revealed a broad superlative antitumor activity against both HepG2 and MCF7 cell lines. Surprisingly, 3 h showed the most powerful anticancer activity (GI 50 = 5.43 � 0.170 μM for MCF7 and GI 50 = 1.80 � 0.50 μM for HepG2) and displayed the most effective inhibition activity on tubulin with IC 50 = 4.51 � 0.13 μM. 3 h exerted low toxicity toward both normal human, Hs371.T and AML12, cell lines. 3 h revealed arrest of cell cycle at G2/M and induced apoptosis compared to control cells. Docking study of all newly derivatives was achieved to decide the preeminent binding mode. Generally, the outcome of the docking study showed that 3 h had better binding mode.

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1,4,5,6,7,8-Hexahydroquinolines and 5,6,7,8-tetrahydronaphthalenes: A new class of antitumor agents targeting the colchicine binding site of tubulin

Cited by 6 publications

References 64 publications

Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity

Potent Quinoline-Containing Combretastatin A-4 Analogues: Design, Synthesis, Antiproliferative, and Anti-Tubulin Activity

Binding interactions and FRET between bovine serum albumin and various phenothiazine-/anthracene-based dyes: a structure–property relationship

Design, Synthesis and Molecular Docking of Chalcone Derivatives as Potential Anticancer Agents

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