8-Methly-4-(3-diethylaminopropylamino) pyrimido [4′,5′;4,5] thieno (2,3–b) quinoline (MDPTQ), a quinoline derivate that causes ROS-mediated apoptosis in leukemia cell lines

P, Sudheer Shenoy; Vasania, Viraf S.; Gopal, M.; Mehta, Ashish

doi:10.1016/j.taap.2007.04.005

Cited by 25 publications

(11 citation statements)

References 27 publications

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“…It has been reported that the members of the spiroquinazolinone family are cytotoxic to several types of cancer cells (Shenoy et al, 2007;Sharma et al, 2004).…”

Section: Discussionmentioning

confidence: 99%

Spiroquinazolinone-induced cytotoxicity and apoptosis in K562 human leukemia cells: alteration in expression levels of Bcl-2 and Bax

et al. 2015

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-Spiroquinazolinone compounds have been considered as a new series of potent apoptosis-inducing agents. In this study, anti-proliferative and apoptotic effects of the derivatives from the spiroquinazolinone family were investigated in the human chronic myeloid leukemia K562 cells. The K562 cells were treated with various concentrations of the spiroquinazolinone (10-300 μM) for 3 days and cell viability was determined by MTT growth inhibition assay. 4t-QTC was more active among these compounds with IC50 of 50 ± 3.6 μM and was selected for further studies. Apoptosis, as the mechanism of cell death was investigated morphologically by acridine orange/ethidium bromide (AO/EtBr) double staining, cell surface expression assay of phosphatidyl serine by Annexin V/PI technique, as well as the formation of DNA ladder. The K562 cells underwent apoptosis upon a single dose (at IC50 value) of the 4t-QTC compound, and over-expressed caspase-3 expression by more than 1.7-fold, following a 72 hr treatment. Furthermore, RT-PCR and Western blot analysis revealed that treatment of the K562 cells with 4t-QTC down-regulates and up-regulates the expression of Bcl-2 (anti-apoptotic) and Bax (pro-apoptotic), respectively. Based on the present data, it seems that these compounds from the spiroquinazolinone family are good candidates for further evaluation as an effective chemotherapeutic family acting through induction of apoptosis in chronic myeloid leukemia.

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“…It has been reported that the members of the spiroquinazolinone family are cytotoxic to several types of cancer cells (Shenoy et al, 2007;Sharma et al, 2004).…”

Section: Discussionmentioning

confidence: 99%

Spiroquinazolinone-induced cytotoxicity and apoptosis in K562 human leukemia cells: alteration in expression levels of Bcl-2 and Bax

et al. 2015

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“…The structural elucidation of the compound was determined by IR and 1 H NMR. The parameters were as follows: BPTQ: C 17 BPTQ (81 µM) was incubated with various concentrations of C. perfringens DNA, calf thymus DNA, and poly[d(G-C)] DNA in 50 mM Tris-HCl (pH 7.4), 15 mM NaCl, 1 mM EDTA. The absorbance and fluorescence emission spectrum of BPTQ on addition of each DNA aliquot was recorded with Spekol spectrophotometer (Analytic Jena, Germany) and F-2000 fluorescence spectrophotometer (Hitachi, Japan), respectively.…”

Section: Synthesis Of Bptqmentioning

confidence: 99%

“…Mitochondrial membrane potential was measured using fluorescent potentiometric dye JC-1 as described previously [17]. MOLT-4 cells were treated with BPTQ (5 μM) for different time intervals and then washed and labeled for 45 min with 10 μM JC-1 at 37 °C.…”

Section: Mitochondrial Membrane Potential Measurementmentioning

confidence: 99%

“…Quinolines and their derivatives are among such interesting class of molecules, as they have been reported to possess a broad spectrum of biological activities such as antimalarial, antimicrobial [15], and antineoplastic activity [16]. These considerations prompted us to explore a new series of planar heterocyclic quinoline derivatives, pyrimido[4′,5′:4,5] thieno(2,3-b)quinolines as new cytotoxic anticancer molecules [17,18].…”

Section: Introductionmentioning

confidence: 99%

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DNA intercalative 4-butylaminopyrimido[4′,5′:4,5]thieno(2,3-b)quinoline induces cell cycle arrest and apoptosis in leukemia cells

RohitKumar

Asha

Raghavan

et al. 2015

Cancer Chemother Pharmacol

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“…18 Quinoline derivatives are also known as P-glycoprotein inhibitors, 19 topoisomerase I/II inhibitors, 20,21 PDGF receptor tyrosine kinase inhibitors, 22 and PI3-kinase-related kinases (PIKKs) inhibitors. 23 Some of these quinolines induce cell cycle arrest, 18,20 generation of reactive oxygen species (ROS), 24 disruption of mitochondrial membrane potential, 25 DNA single-strand breaks, 18 activation of caspases, 25 and interact with DNA. 20,21 Based on the above-mentioned effects of quinolines, a new series of substituted nitrogen atomcontaining heterocyclic compounds was prepared.…”

Section: Introductionmentioning

confidence: 99%

4‐Amino‐3‐acetylquinoline‐induced apoptosis of murine L1210 leukemia cells involves ROS‐mitochondrial‐mediated death signaling and activation of p38 MAPK

Jantová

Repicky

Letašiová

et al. 2008

Cell Biochemistry & Function

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Quinolines are known to be multitarget agents with a broad spectrum of biological activity. In a previous study, we showed that newly prepared 4-amino-3-acetylquinoline (AAQ) possesses strong anticancer activities. In this study, we investigated whether AAQ has cytotoxicity in murine L1210 leukemia cells. Results from cell proliferation assays showed that AAQ caused significant decrease in cell number in a dose-dependent manner. The cell death induced by AAQ appeared to involve apoptosis, based on evidence from apoptotic DNA fragmentation, flow cytometry, fluorescence microscopy, and Western blot analyses. We found that AAQ-treated cells had activated p38 MAPK and that apoptosis was processed through a reactive oxygen species (ROS)-dependent mitochondrial pathway. In summary, our results suggest that AAQ can induce apoptosis, at least in part, through the activation of the p38 MAPK pathway in L1210 leukemia cells.

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8-Methly-4-(3-diethylaminopropylamino) pyrimido [4′,5′;4,5] thieno (2,3–b) quinoline (MDPTQ), a quinoline derivate that causes ROS-mediated apoptosis in leukemia cell lines

Cited by 25 publications

References 27 publications

Spiroquinazolinone-induced cytotoxicity and apoptosis in K562 human leukemia cells: alteration in expression levels of Bcl-2 and Bax

Spiroquinazolinone-induced cytotoxicity and apoptosis in K562 human leukemia cells: alteration in expression levels of Bcl-2 and Bax

DNA intercalative 4-butylaminopyrimido[4′,5′:4,5]thieno(2,3-b)quinoline induces cell cycle arrest and apoptosis in leukemia cells

4‐Amino‐3‐acetylquinoline‐induced apoptosis of murine L1210 leukemia cells involves ROS‐mitochondrial‐mediated death signaling and activation of p38 MAPK

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