Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives

Nagarsenkar, Atulya; Guntuku, Lalita; Guggilapu, Sravanthi Devi; Bai, Kai-Kai; Srinivasulu, Gannoju; Naidu, V.G.M.; Babu, Bathini Nagendra

doi:10.1016/j.ejmech.2016.09.009

Cited by 71 publications

(19 citation statements)

References 40 publications

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“…Cytotoxic compounds mainly exert their effects by intervening with cell cycle progression, inhibiting cellular proliferation, and thus, inducing cell death. [ 16–18 ] The subG1 phase of the cell cycle represents the cells that are hypodiploid and undergoing apoptosis. [ 19,20 ] NCI‐H460 cells treated with compound PP‐31d at different concentrations were subjected to cell cycle analysis after propidium iodide (PI) staining to observe the percentage of cells undergoing apoptosis and their distribution in different phases of the cell cycle.…”

Section: Resultsmentioning

confidence: 99%

Novel pyrazolo[3,4‐d]pyrimidine derivatives inhibit human cancer cell proliferation and induce apoptosis by ROS generation

Gaonkar

Savanur

Nadaf

et al. 2020

Archiv der Pharmazie

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The paucity of effective anticancer drugs for successful treatment is a major concern, indicating the strong need for novel therapeutic compounds. In the quest of new molecules, the present study aimed to explore the potential of pyrazolo[3,4‐d]pyrimidine derivatives as antiproliferative agents. In vitro anticancer screening of selected compounds was done by the National Cancer Institute's Developmental Therapeutics Programme against a panel of 60 cancer cell lines. The lead compound PP‐31d considerably inhibited the growth of cancer cells, such as NCI‐H460 (non‐small‐cell lung cancer), OVCAR‐4 (ovarian cancer), 786‐0 (renal cancer), A549 (non‐small‐cell lung cancer), and ACHN (renal cancer), showing strong anticancer potential, among other derivatives. Kinetic studies of PP‐31d on NCI‐H460 cells revealed a dose‐dependent effect with an IC50 of 2 µM. The observed inhibition by PP‐31d is attributed to the generation of reactive oxygen species and the subsequent induction of cellular apoptosis, as evidenced by the increase in the hypodiploid (subG1) population, the early apoptotic cell population, and caspase‐3/7 activity, the loss of the mitochondrial membrane potential, and the degradation of nuclear DNA. Collectively, our results demonstrated that pyrazolo[3,4‐d]pyrimidine derivatives inhibit cancer cell proliferation by inducing apoptosis and, thus, have the potential to be further explored for anticancer properties.

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Section: Resultsmentioning

confidence: 99%

Novel pyrazolo[3,4‐d]pyrimidine derivatives inhibit human cancer cell proliferation and induce apoptosis by ROS generation

Gaonkar

Savanur

Nadaf

et al. 2020

Archiv der Pharmazie

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“…To determine the percentage of cells undergoing apoptosis or necrosis by compound 4g which showed the most cytotoxic effect, annexin V‐FITC/propidium iodide (PI) staining assay was performed in PC3 and MCF‐7 cancer cells according to the reported processes . This assay assists the detection of live cells (Q4), early apoptotic cells (Q3), late apoptotic cells (Q2), and necrotic cells (Q1).…”

Section: Resultsmentioning

confidence: 99%

“…After 24 hr of treatment, cells from the supernatant and adherent monolayer cells were harvested by trypsinization and washed with PBS at 3,000 rpm. Then, the cells were treated with Annexin V‐assay kit (FITC Annexin V Apoptosis Detection Kit; BD Pharmingen™) according to the manufacturer's instruction and finally, FACS was done by a flow cytometer (Becton Dickinson).…”

Section: Methodsmentioning

confidence: 99%

Synthesis and biological evaluation of novel benzo[c]acridine‐diones as potential anticancer agents and tubulin polymerization inhibitors

Behbahani

Tabeshpour

Mirzaei

et al. 2019

Archiv der Pharmazie

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A new series of novel benzo[c]acridine-diones possessing pharmacophoric elements of antitubulins with central dihydropyridine bridge were designed and synthesized as potential anticancer agents and tubulin polymerization inhibitors. The cytotoxic activity of the synthesized compounds was evaluated against eight cancer cell lines including MCF-7, A2780, HeLa, HepG2, DU145, A549, PC3, and LNCAP cancer cells and normal cells (HUVEC) through 3-[4,5-dimethylthiazol-2yl]-2,5-diphenyl tetrazolium bromide (MTT) assay, wherein β-lapachone and combretastatin A-4 were used as positive controls. Some of our compounds (4c and 4g) showed significant cytotoxic activity on cancer cells with IC 50 values in the range of 5.23-24.32 μM. None of the synthesized compounds showed significant cytotoxicity on normal HUVEC cells. Among all investigated derivatives, compound 4g showed promising greater antiproliferative activity against all tested cancer cells with the highest sensitivity observed for the PC3 cell line. Results from the flow cytometry analysis of PC3 and MCF-7 cancer cells treated with 4g showed an induced cell-cycle arrest at G2/M, and therefore induced apoptosis which occurred at low concentration of test compound, whereas annexin V-FITC/propidium iodide staining assay in the aforementioned cancer cell lines treated with 4g showed that 4g can cause necrosis in PC3 and MCF-7 cancer cells at higher concentration. Compound 4g proved to be an inhibitor of tubulin polymerization in a mode similar to that of colchicine and in a dose-dependent manner. Molecular docking studies of 4g into the colchicine-binding site of tubulin exhibited a possible mode of interaction between this compound and tubulin.

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“…This indicates universal interruption in the cellular redox system, which is a hallmark of apoptosis. 29) The NH analogue 3a induced only a slight increase in ROS parameters indicating a possible different cytotoxic mechanism than 3e. Nonetheless, we found strong evidence for apoptotic cell death upon treatment of HCT116 cells by both compounds.…”

Section: Fig 7 Effects Of 3a and 3e On The Cellular Expression And mentioning

confidence: 95%

Design, Synthesis and Antiproliferative Activities of Oxidative Stress Inducers Based on 2-Styryl-3,5-dihydro-4<i>H</i>-imidazol-4-one Scaffold

Omar

Abdelghany

Abdel-Bakky

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives

Cited by 71 publications

References 40 publications

Novel pyrazolo[3,4‐d]pyrimidine derivatives inhibit human cancer cell proliferation and induce apoptosis by ROS generation

Novel pyrazolo[3,4‐d]pyrimidine derivatives inhibit human cancer cell proliferation and induce apoptosis by ROS generation

Synthesis and biological evaluation of novel benzo[c]acridine‐diones as potential anticancer agents and tubulin polymerization inhibitors

Design, Synthesis and Antiproliferative Activities of Oxidative Stress Inducers Based on 2-Styryl-3,5-dihydro-4<i>H</i>-imidazol-4-one Scaffold

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