Synthesis and anticancer evaluation of novel triazole linked N-(pyrimidin-2-yl)benzo[d]thiazol-2-amine derivatives as inhibitors of cell survival proteins and inducers of apoptosis in MCF-7 breast cancer cells

Kumbhare, Ravindra M.; Dadmal, Tulshiram L.; Ramaiah, M. Janaki; Kishore, Kaushal; Valli, S.N.C.V.L. Pushpa; Tiwari, Shalbha; Appalanaidu, K.; Rao, Yuanfang; Bhadra, Manika Pal

doi:10.1016/j.bmcl.2014.11.083

Cited by 48 publications

(15 citation statements)

References 63 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This shrinkage may be due to the inhibitory effect of the phytoconstituents and/or functional groups and/or active compounds present in the lyophilized pure fruit juice powder of C. limon. The above work finds support from similar observations on the effect of cladribine [82], Antrodia camphorata [19], selenium and vitamin E [83], zoledronic acid [84], doxorubicin [85], metronidazole [86], gemcitabine [87], fruit peel extracts [81], triazole linked N-(pyrimidin-2-yl) banzol [d] thaizol-2-amine [5] on MCF-7 cells.…”

Section: Ft-ir Spectral Analysissupporting

confidence: 79%

“…Cancer remains a major public health burden in developed as well as developing countries [1][2][3][4]. Cancer as a second cause of death after heart disease in the world has posed a great challenge to the field of medicine and immunology [5]. WHO has predicted that the number of new cases of cancer may increase up to 15 million in the year 2020 [6].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Phytochemical Profiling and Anti-cancer Study of Lyophilized Pure Fruit Juice of Citrus Limon (L.) Osbeck against Human Breast Cancer (MCF-7) Cell Line

A.¹,

Sivakumari²,

Ashok³

et al. 2017

JAMB

View full text Add to dashboard Cite

Abstract. The present study aims at the phytochemical profiling of lyophilized pure fruit juice powder of Citrus limon and demonstrates its efficacy as an antitumor agent against human breast cancer cell line (MCF-7). The cytotoxicity was evaluated using the changes in cell morphology, cell viability, and DNA fragmentation, the percentage of cell viability was determined by MTT assay. Our results showed that lyophilized pure fruit juice powder of Citrus limon inhibited the proliferation of human breast cancer cell line MCF-7 with an IC50 98.16 μg/ml at 48 h incubation, it was shown to promote apoptosis as seen as DNA fragmentation using ladder assay. These results suggest that lyophilized pure fruit juice powder of Citrus limon has antiproliferative effect against MCF-7 cell by suppressing its growth.

show abstract

Section: Ft-ir Spectral Analysissupporting

confidence: 79%

Section: Introductionmentioning

confidence: 99%

Phytochemical Profiling and Anti-cancer Study of Lyophilized Pure Fruit Juice of Citrus Limon (L.) Osbeck against Human Breast Cancer (MCF-7) Cell Line

A.¹,

Sivakumari²,

Ashok³

et al. 2017

JAMB

View full text Add to dashboard Cite

show abstract

“…As MEK and NF-κB inhibitors may also exert their effects on other tissues such as bones, joints, gastrointestinal system, liver, and muscles care should be taken when prescribing these drugs in combination with therapeutic targets with the aim of enhancing anti-tumor activity [42,[50][51][52][53]. Anyhow, results obtained from this experimental model support the use of adjuvant drugs for the improvement of LC treatment as it is the case in other cancer types.…”

Section: Study Limitationsmentioning

confidence: 71%

Pharmacological Approaches in an Experimental Model of Non-Small Cell Lung Cancer: Effects on Tumor Biology

Mateu-Jiménez¹,

Fermoselle²,

Rojo³

et al. 2016

CPD

View full text Add to dashboard Cite

Lung cancer (LC) remains the leading cause of cancer mortality worldwide, and non-small cell LC (NSCLC) represents 80% of all LC. Oxidative stress and inflammation, autophagy, ubiquitin-proteasome system, nuclear factor (NF)-κB, and mitogen activated protein kinases (MAPK) participate in LC pathophysiology. Currently available treatment for LC is limited and in vivo models are lacking. We hypothesized that antioxidants and NF-κB, MAPK, and proteasome inhibitors may exert an antitumoral response through attenuation of several key biological mechanisms that promote tumorigenesis and cancer cell growth. Body and tumor weights, oxidative stress, antioxidants, inflammation, NF-κB p65 expression, fibulins, apoptosis, autophagy, tumor and stroma histology were evaluated in the subcutaneous tumor of LC (LP07 adenocarcinoma) BALB/c mice, with and without concomitant treatment with NF-κB (sulfasalazine), MEK (U0126), and proteasome (bortezomib) inhibitors, and N-acetyl cysteine (NAC). Compared to LC control mice, in subcutanous tumors, the four pharmacological agents reduced oxidative stress markers and tumor proliferation (ki-67).Inflammation and NF-κB p65 expression were attenuated by NF-κB and MAPK inhibitors, and the latter also enhanced apoptotic markers. Catalase was induced by the three inhibitors, while bortezomib also promoted superoxide dismutase expression. NF-κB and MEK inhibitors significantly reduced tumor burden through several biological mechanisms that favored tumor degradation and attenuated tumor proliferation. These two pharmacological agents may enhance the anti-tumor activity of selectively targeted therapeutic strategies for LC. Proteasomal inhibition using bortezomib rather promotes tumor degradation, while treatment with antioxidants cannot be recommended. This experimental model supports the use of adjuvant drugs for the improvement of LC treatment.Word count: 250

show abstract

“…Among the compounds tested, promising compounds 42-45 (Table 3), under the concentration of 3 mM, 3.2 mM, 2.52 mM, 2.12 mM, respectively, caused most remarkable cytotoxicity against MCF-7 BC cells, by inducing apoptosis and affecting the expression of key proteins such as ERK1/2, NF-B and survivin that cause abnormal cell proliferation and up-regulate the activity of caspase-9. 53 One compound, 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6carbonitrile (46) induced growth arrest of most tumor cell lines, including a panel of BC cell lines, with GI 50 values ranging from 0.025 to 2 mM, as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-Related Kinase 5 (ARK5) ( Table 3). 54 Halogenated thieno[3,2-d]pyrimidines (47 and 48) with IC 50 value of 9 mM and 5.9 mM respectively are both toxic to the TNBC cell model MDA-MB-231 at low-micromolar concentrations, but that only for compound 47 can selectively triggers mitotic arrest ( Table 3).…”

Section: The Pyrimidine Functional Groupmentioning

confidence: 99%

Current research on anti-breast cancer synthetic compounds

et al. 2018

View full text Add to dashboard Cite

show abstract

Synthesis and anticancer evaluation of novel triazole linked N-(pyrimidin-2-yl)benzo[d]thiazol-2-amine derivatives as inhibitors of cell survival proteins and inducers of apoptosis in MCF-7 breast cancer cells

Cited by 48 publications

References 63 publications

Phytochemical Profiling and Anti-cancer Study of Lyophilized Pure Fruit Juice of Citrus Limon (L.) Osbeck against Human Breast Cancer (MCF-7) Cell Line

Phytochemical Profiling and Anti-cancer Study of Lyophilized Pure Fruit Juice of Citrus Limon (L.) Osbeck against Human Breast Cancer (MCF-7) Cell Line

Pharmacological Approaches in an Experimental Model of Non-Small Cell Lung Cancer: Effects on Tumor Biology

Current research on anti-breast cancer synthetic compounds

Contact Info

Product

Resources

About