scholarly journals Synthesis and biological evaluation of indazole derivatives as anti-cancer agents

RSC Advances ◽  
2021 ◽  
Vol 11 (26) ◽  
pp. 15675-15687
Author(s):  
Wei Wei ◽  
Zhihao Liu ◽  
Xiuli Wu ◽  
Cailing Gan ◽  
Xingping Su ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Breast Cancer Cell Line ◽  
Cell Apoptosis ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Migration And Invasion ◽  
Anti Cancer ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

One of the synthesized indazole derivatives, 2f, displayed inhibitory activities against proliferation, migration and invasion of breast cancer cell line 4T1, with the potential of inducing cell apoptosis, and suppressing tumor growth in vivo.

scholarly journals In vitro antineoplastic activity in triple-negative breast cancer cell line and in vivo

2014 ◽  
Vol 8 (Suppl 4) ◽  
pp. P22
Author(s):  
Klesia Madeira ◽  
Murilo Cerri ◽  
Renata Daltoé ◽  
Alice Herlinger ◽  
João Filho ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Triple Negative Breast Cancer ◽  
Breast Cancer Cell Line ◽  
Triple Negative ◽  
Cancer Cell Line

scholarly journals Synthesis and Biological Evaluation of Genistein-IR783 Conjugate: Cancer Cell Targeted Delivery in MCF-7 for Superior Anti-Cancer Therapy

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4120 ◽  
Author(s):  
Yang Guan ◽  
Yi Zhang ◽  
Juan Zou ◽  
Li-Ping Huang ◽  
Mahendra D. Chordia ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Therapy ◽  
Natural Product ◽  
Cancer Cell ◽  
Biological Evaluation ◽  
Cyanine Dye ◽  
Therapeutic Window ◽  
Anti Cancer ◽  
Mcf 7

The flavonoid-based natural product genistein is a biologically active compound possessing promising anti-oxidant and anti-cancer properties. Poor pharmacokinetics along with low potency limit however the therapeutic application of genistein in cancer therapy. In order to overcome those limitations and to expand its therapeutic window of efficacy, we sought to covalently attach genistein with a heptamethine cyanine dye—IR 783—for cancer cell targeting and enhanced delivery to tumors. Herein we report the synthesis, a selective detailed characterization and preliminary in vitro/in vivo biological evaluation of genistein-IR 783 conjugate 4. The conjugate 4 displayed improved potency against human breast cancer MCF-7 cells (10.4 ± 1.0 μM) as compared with the parent genistein (24.8 ± 0.5 μM) or IR 783 (25.7 ± 0.7 μM) and exhibited selective high uptake in MCF-7 as against the normal mammary gland MCF-10A cells in various assays. In the cell viability assay, conjugate 4 exhibited over threefold lower potency against MCF-10A cells (32.1 ± 1.1 μM) suggesting that the anti-cancer profile of parent genistein is significantly improved upon conjugation with the dye IR783. Furthermore, the genistein-IR783 conjugate 4 was shown to be especially accumulated in MCF-7 cancer cells by fluorescent intensity measurements and inverted fluorescence microscopy in fixed cells as well as in live cells with time via live cell confocal fluorescence imaging. The mechanism-based uptake inhibition of conjugate 4 was observed with OATPs inhibitor BSP and in part with amiloride, as a macropinocytosis inhibitor. For the first time we have shown amiloride inhibited uptake of cyanine dye by about ~40%. Finally, genistein-IR 783 conjugate 4 was shown to be localized in MCF-7 tumor xenografts of mice breast cancer model via in vivo near infrared fluorescence (NIRF) imaging. In conclusion, conjugation of genistein with cyanine dye IR783 indeed improved its pharmacological profile by cancer cell selective uptake and targeting and therefore warrants further investigations as a new anti-cancer therapeutics derived from natural product genistein.

Silibinin Inhibit Cell Migration through Downregulation of RAC1 Gene Expression in Highly Metastatic Breast Cancer Cell Line

Drug Research ◽  
2020 ◽  
Vol 70 (10) ◽  
pp. 478-483
Author(s):  
Hamed Esmaeil Lashgarian ◽  
Vahid Adamii ◽  
Vajihe Ghorbanzadeh ◽  
Leila Chodari ◽  
Fayze Kamali ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Tumor Cells ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Breast Cancer Cell Line ◽  
Cancer Cell Line ◽  
Migration And Invasion ◽  
And Migration ◽  
Proliferation And Migration

Abstract Background Triple negative breast cancer is the most invasive breast cancer subtype and possesses poor prognosis and survival. Rho GTPase famil, especially Rac1 participates in a number of signaling events in cells with crucial roles in malignancy, migration and invasion of tumor cells. Silibinin, a flavonoid antioxidant from milk thistle has attracted attention in the recent decades for chemoprevention and chemotherapy of tumor cells. In this study, the effect of silibinin on the migration capacity of MDA-MB-231 cells, a highly metastatic human breast cancer cell line was investigated by evaluation of Rac1 expression. Method MTT wound healing and transwell assays were performed to evaluate the effects of silibinin on proliferation and migration of MDA-MB-231 cells. In addition, the influence of the silibinin on the expression of Rac1mRNAs was assessed by RT-PCR. Results Results indicated significant dose-dependent inhibitory effect of silibinin on proliferation and migration of MDA-MB-231 cells. It significantly inhibited the expression of Rac1 mRNA. Conclusion In conclusion, the results demonstrate that the silibinin can be used as an experimental therapeutic for the management of TNBC metastatic cancer.

scholarly journals Reduced in vivo lung metastasis of a breast cancer cell line after treatment with Herceptin mAb conjugated to chemotherapeutic drugs

Oncogene ◽  
2012 ◽  
Vol 32 (20) ◽  
pp. 2527-2533 ◽  
Author(s):  
A Galan Garcia ◽  
H Nedev ◽  
K Bijian ◽  
J Su ◽  
M A Alaoui-Jamali ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Lung Metastasis ◽  
Breast Cancer Cell Line ◽  
Cancer Cell Line ◽  
Chemotherapeutic Drugs

scholarly journals Synthesis and biological evaluation of (E)-4-(3-arylvinyl-1H-indazol-6-yl)pyrimidin-2-amine derivatives as PLK4 inhibitors for the treatment of breast cancer

RSC Advances ◽  
2017 ◽  
Vol 7 (44) ◽  
pp. 27737-27746 ◽  
Author(s):  
Zhihao Liu ◽  
Qian Lei ◽  
Wei Wei ◽  
Lu Xiong ◽  
Yaojie Shi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Biological Evaluation ◽  
Amine Derivative ◽  
Synthesis And Biological Evaluation ◽  
Cancer Activity

SAR explorations identified (E)-4-(3-arylvinyl-1H-indazol-6-yl)pyrimidin-2-amine derivative14ias a potential PLK4 inhibitor with significant anti-breast cancer activityin vitroandin vivo.

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