indirubin/breast neoplasms

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[The cytotoxicity of indirubin derivative PHII-7 against human breast cancer MCF-7 cells and its mechanisms].

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OBJECTIVE To observe the cytotoxicity of indirubin derivative PHII-7 against human breast cancer MCF-7 cells and to study its primary mechanisms. METHODS The proliferation of MCF-7 cells was detected using MTT colorimetry. Annexin V/PI double staining was applied to detect the apoptosis rate of

A novel indirubin derivative PHII-7 potentiates adriamycin cytotoxicity via inhibiting P-glycoprotein expression in human breast cancer MCF-7/ADR cells.

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Multidrug resistance (MDR) is a major impediment to the effective chemotherapy of many human malignancies, and novel MDR reversal agents are desirable for combination therapy to reduce MDR, enhance anti-tumor activity and reduce side effects. Overexpression of P-glycoprotein (P-gp) is the most

Transient induction of cytochromes P450 1A1 and 1B1 in MCF-7 human breast cancer cells by indirubin.

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The aryl hydrocarbon receptor (AhR), when activated by exogenous ligands such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), regulates expression of several phase I and phase II enzymes and is also involved in the regulation of cell proliferation. Several studies suggest that endogenous AhR

Induction of discrete apoptotic pathways by bromo-substituted indirubin derivatives in invasive breast cancer cells.

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Indirubin derivatives gained interest in recent years for their anticancer and antimetastatic properties. The objective of the present study was to evaluate and compare the anticancer properties of the two novel bromo-substituted derivatives 6-bromoindirubin-3'-oxime (6BIO) and

Chemical characterization and biological activity data for a novel indirubin derivative, LDD-1819.

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This article contains chemical characterization and biological activity data for a novel indirubin derivative, termed LDD-1819. The detailed synthesis procedure and associated NMR data are presented. The concentration-dependent inhibition data of two biological targets, glycogen synthase kinase-3

Proliferative and androgenic effects of indirubin derivatives in LNCaP human prostate cancer cells at sub-apoptotic concentrations.

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Certain indirubin derivatives are potent cyclin-dependent kinase (CDK) and glycogen synthase kinase (GSK-3β) inhibitors and may be effective against various cancers. We evaluated the effects of aloisine A, alsterpaullone, aminopurvalanol, indirubin-3'-oxime, 6-Br-indirubin-3'-oxime, kenpaullone,

Indirubin derivative 6BIO suppresses metastasis.

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While metastasis is the chief cause of cancer mortality, there nonetheless remains a lack of antimetastatic therapies that are clinically available. In this study, we present the indirubin derivative 6-bromo-indirubin-3'-oxime (6BIO) as a promising antimetastatic agent. 6BIO strongly reduced

The pleiotropic profile of the indirubin derivative 6BIO overcomes TRAIL resistance in cancer.

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TRAIL (TNFα-related apoptosis-inducing factor) has been promoted as a promising anti-cancer agent. Unfortunately many tumor cells develop resistance towards TRAIL due to numerous defects in apoptotic signaling. To handle this problem combination therapy with compounds affecting as many different

Synthesis of indirubin-N'-glycosides and their anti-proliferative activity against human cancer cell lines.

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The first indirubin-N'-glycosides were prepared based on reactions of isatin-N'-glycosides with indoxyls. The products show a significant anti-proliferative activity against various human cancer cell lines. Good results were observed for an indirubin-N'-mannoside which was shown to have medium to

A novel role of the aryl hydrocarbon receptor (AhR) in centrosome amplification - implications for chemoprevention.

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BACKGROUND Centrosome aberrations can cause genomic instability and correlate with malignant progression in common human malignancies such as breast and prostate cancer. Deregulation of cyclin/cyclin-dependent kinase 2 (CDK2) activity has previously been shown to be critically involved in centrosome

Design, synthesis and biological evaluation of novel indolin-2-ones as potent anticancer compounds.

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The indolin-2-one core is a privileged structure for antitumor agents, especially kinase inhibitors. Twenty-three novel indolin-2-ones were designed by molecular dissection of the anticancer drug indirubin. Seventeen of them exhibited significant inhibition against the tested cell lines, and two of

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