Anti-Cancer Agents in Medicinal Chemistry
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Sắp xếp:
Recent Development in Indole Derivatives as Anticancer Agent: A Mechanistic Approach
Background:
Cancer accounts for several deaths each year. There are multiple FDA approved drugs for cancer treatments. Due to the severe side effects and multiple drug resistance, the current drug therapies become ineffective. So, the newer moieties with fewer toxic effects are necessary for the development.
Objective:
The mechanism of indole derivatives as anti-cancer agents with their major target is explored in detail
in this article.
Methods:
Recent advances and mechanism of indole derivatives as anti-cancer agents are reviewed. This review suggests a detailed explanation of multiple mechanisms of action of various indole derivatives: cell cycle arrest, aromatase inhibitor estrogen receptor regulator, tubulin inhibitor, a tyrosine kinase inhibitor, topoisomerase inhibitors, NFkB/PI3/Akt/mTOR pathway inhibitors, through which these derivatives have shown promising anti-cancer potential.
Results:
A full literature review showed that the indole derivatives are associated with the properties of inducing apoptosis, aromatase inhibition, regulation of estrogen receptor and inhibition of tyrosine kinase, tubulin assembly, NFkB/PI3/Akt/mTOR pathway, and HDACs. These derivatives have shown significant activity against cancer cell lines.
Conclusion:
Indole derivatives seem to be important in cancer via acting through various mechanisms. This review has shown that the indole derivatives can further be explored for the betterment of cancer treatment, and to discover the hidden potential of indole derivatives.
Anti-Cancer Agents in Medicinal Chemistry - Tập 21 Số 14 - Trang 1802-1824 - 2021
Antidepressant Desipramine Leads to C6 Glioma Cell Autophagy: Implication for the Adjuvant Therapy of Cancer
Anti-Cancer Agents in Medicinal Chemistry - Tập 13 Số 2 - Trang 254-260 - 2013
Synthesis and Antiproliferative Effects of 5,6-Disubstituted Pyridazin-3(2H)-ones Designed as Conformationally Constrained Combretastatin A-4 Analogues
Anti-Cancer Agents in Medicinal Chemistry - Tập 13 Số 7 - Trang 1133-1140 - 2013
TPEN Exerts Antitumor Efficacy in Murine Mammary Adenocarcinoma Through an H2O2 Signaling Mechanism Dependent on Caspase-3
Background:
Breast cancer is the second most common cancer worldwide. N, N, N’, N’-Tetrakis
(2-pyridylmethyl)-ethylenediamine (TPEN) is a lipid-soluble zinc metal chelator that induces apoptosis in
cancer cells through oxidative stress (OS). However, the effectiveness and the mechanisms involved in TPENinduced
cell death in mammary adenocarcinoma cells in vitro and in vivo are still unclear.
Objective:
This study aimed to evaluate the cytotoxic effect of TPEN in mouse embryonic fibroblasts (MEFs, as
normal control cells) and mammary adenocarcinoma cancer cells (TS/A cells) in vitro and in a mammary tumor
model in vivo.
Methods:
Cells were treated with TPEN (0-3 µM), and changes in nuclear chromatin and DNA, mitochondrial
membrane potential (ΔΨm), and intracellular reactive oxygen species (ROS) levels were determined by both
fluorescence microscopy and flow cytometry. Cell proliferation and the cell cycle were also analyzed. Cellular
markers of apoptosis were evaluated by Western blot. Finally, the effect of TPEN in a mammary adenocarcinoma
tumor model in vivo was determined by immunohistological analyses.
Results:
TPEN induced apoptosis in TS/A cells in a dose-dependent manner, increasing nuclear chromatin condensation,
DNA fragmentation, cell cycle arrest and ΔΨm loss. Additionally, TPEN increased dichlorofluorescein
fluorescence (DCF+) intensity, indicative of ROS production; increased DJ-1-Cys106-sulfonate expression,
a marker of intracellular H2O2 stress; induced p53 and PUMA upregulation; and activated caspase-3.
Moreover, TPEN induced mammary cancer cell elimination and tumor size reduction in vivo 48 h after treatment
through an OS-induced apoptotic mechanism.
Conclusion:
TPEN selectively induces apoptosis in TS/A cells through an H2O2-mediated signaling pathway.
Our findings support the use of TPEN as a potential treatment for breast cancer.
Anti-Cancer Agents in Medicinal Chemistry - Tập 18 Số 11 - Trang 1617-1628 - 2019
Urea Derivatives as Anticancer Agents
Within the past ten years, a huge volume of research on the synthesis, structure-activity relationships (SAR), and anticancer activities of the urea derivatives was reported. Many aromatic urea derivatives such as N-phenyl-N-(2-chloroethyl)ureas (CEUs) and benzoylureas (BUs) show good anticancer activity, and these compounds have mainly been proved to be tubulin ligands that inhibit the polymerization of tubulin. Heterocyclic urea derivatives play an important role in anticancer agents because of their good inhibitory activity against receptor tyrosine kinases (RTKs), raf kinases, protein tyrosine kinases (PTKs), and NADH oxidase, which play critical roles in many aspects of tumorigenesis. Thiourea derivatives are also of wide interest because of their diverse anticancer activity against various leukemias and solid tumors. In this review, the anticancer activity of the urea derivatives mentioned above is summarized in detail. It is hoped that increasing knowledge of the SAR and cellular processes underlying the antitumor-activity of urea derivatives will be beneficial to the rational design of new generation of urea anticancer drugs.
Anti-Cancer Agents in Medicinal Chemistry - Tập 9 Số 4 - Trang 471-480 - 2009
Can We Effectively Degrade Microcystins? - Implications on Human Health
Anti-Cancer Agents in Medicinal Chemistry - Tập 11 Số 1 - Trang 19-37 - 2011
The Warburg Effect and the Hallmarks of Cancer
Anti-Cancer Agents in Medicinal Chemistry - Tập 17 Số 2 - Trang 164-170 - 2017
Tumor Initiation in Human Malignant Melanoma and Potential Cancer Therapies
Cancer stem cells (CSCs), also known as tumor-initiating cells, have been identified in several human malignancies, including human malignant melanoma. The frequency of malignant melanoma-initiating cells (MMICs), which are identified by their expression of ATP-binding cassette (ABC) family member ABCB5, correlates with disease progression in human patients. Furthermore, targeted MMIC ablation through ABCB5 inhibits tumor initiation and growth in preclinical xenotransplantation models, pointing to potential therapeutic promise of the CSC concept. Recent advances also show that CSCs can exert pro-angiogenic roles in tumor growth and serve immunomodulatory functions related to the evasion of host anti-tumor immunity. Thus, MMICs might initiate and sustain tumorigenic growth not only as a result of CSC-intrinsic self-renewal, differentiation and proliferative capacity, but also based on pro-tumorigenic interactions with the host environment.
Anti-Cancer Agents in Medicinal Chemistry - Tập 10 Số 2 - Trang 131-136 - 2010
Vitamin D and Cancer Mortality: Systematic Review of Prospective Epidemiological Studies
Anti-Cancer Agents in Medicinal Chemistry - Tập 13 Số 1 - Trang 107-117 - 2013
Discovery of Novel <i>N</i>-alkyl 4-anilinofuro[2,3-<i>b</i>]quinoline Derivatives (CIL-102 Derivatives) Against Castration-resistant Human Prostate Cancers
Anti-Cancer Agents in Medicinal Chemistry - Tập 15 Số 4 - Trang 493-500 - 2015
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