scholarly journals Triple action Pt(iv) derivatives of cisplatin: a new class of potent anticancer agents that overcome resistance

2018 ◽  
Vol 9 (18) ◽  
pp. 4299-4307 ◽  
Author(s):  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Irene Solazzo ◽  
Valentina Gandin ◽  
Dan Gibson
Keyword(s):  
Cancer Cells ◽  
Anticancer Agents ◽  
Single Agent ◽  
Cellular Processes ◽  
New Class ◽  
Derivatives Of

A series of triple action Pt(iv) prodrugs was designed to test the hypothesis that multi-action compounds, where each bioactive moiety intervenes in several cellular processes, might be more effective than a single agent at killing cancer cells.

Synthesis, Cytotoxicity, Anti-migration and Anti-invasion Activity of Diphyllin Heterocyclic Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Weidong Shen ◽  
Haijiao Chen ◽  
Miaomiao Wu ◽  
Ting Zhang ◽  
Li Zhu ◽  
...  
Keyword(s):  
Atpase Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Migration And Invasion ◽  
Transwell Invasion Assay ◽  
Atpase Inhibitors ◽  
Scratch Wound ◽  
Heterocyclic Derivatives ◽  
Antiviral Activities ◽  
Derivatives Of

Background: Diphyllin, an arylnaphthalene lignan lactone, isolated from many traditional medicinal plants, has been reported to possess anticancer and antiviral activities. Natural diphyllin and its glycosides were identified as potent vacuolar H+ -ATPase (V-ATPase) inhibitors. Objective: The aim of this study was to design and synthesize a series of heterocyclic derivatives of diphyllin as novel anticancer agents. Methods: The targeted heterocyclic derivatives of diphyllin were synthesized from diphyllin employing etherification reaction and N-substitution reaction. Cytotoxicity of these compounds on four cancer cells was assessed by MTT assay. The inhibitory activity of V-ATPase of compound 3n was measured on MGC-803 cells. Anti-migration and anti-invasion abilities were assessed by transwell invasion assay and scratch wound assay. Results: Most of these derivatives displayed potent cytotoxicity on four cancer cells at submicromolar concentrations. The most potent derivative 3n has been shown to inhibited V-ATPase activity, migration and invasion abilities on MGC-803 cells at 0.75 mM. Conclusion: The collective results clearly indicate that heterocyclic derivatives of diphyllin inhibit the viability, V-ATPase activity, migration and invasion of the MGC803 cells. The current findings provide valuable insights for the future development of novel diphyllin derivatives as anticancer agents.

scholarly journals Identification of the First Inhibitor of the GBP1:PIM1 Interaction. Implications for the Development of a New Class of Anticancer Agents against Paclitaxel Resistant Cancer Cells

2014 ◽  
Vol 57 (19) ◽  
pp. 7916-7932 ◽  
Author(s):  
Mirko Andreoli ◽  
Marco Persico ◽  
Ajay Kumar ◽  
Nausicaa Orteca ◽  
Vineet Kumar ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Anticancer Agents ◽  
New Class

A mode of action study of cationic anthraquinone analogs: a new class of highly potent anticancer agents

MedChemComm ◽  
2015 ◽  
Vol 6 (11) ◽  
pp. 2012-2022 ◽  
Author(s):  
Jaya P. Shrestha ◽  
Yagya Prasad Subedi ◽  
Liaohai Chen ◽  
Cheng-Wei Tom Chang
Keyword(s):  
Cancer Cells ◽  
Anticancer Agents ◽  
Mode Of Action ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
New Class ◽  
Structure Activity ◽  
Sar Study

Previously, we reported the synthesis and structure–activity relationship (SAR) study of a series of novel 4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-3-ium salts, which had very potent anti-proliferative activities (low μM to nM GI50) against a broad range of cancer cells.

scholarly journals Pharmacotherapy of Hematologic Malignancies with Tipifarnib

2009 ◽  
Vol 1 ◽  
pp. CMT.S1097
Author(s):  
Ioannis Kotsianidis ◽  
Evangelia Nakou ◽  
Irene Bouchliou
Keyword(s):  
Anticancer Agents ◽  
Myeloid Leukemia ◽  
Single Agent ◽  
Specific Inhibitor ◽  
Hematologic Malignancies ◽  
Farnesyltransferase Inhibitors ◽  
Cellular Processes ◽  
Predictors Of Response ◽  
Inhibition Of Tumor Growth ◽  
Molecular Aberrations

The illumination of cellular processes in cancer has revolutionized oncology drug development leading to a shift from non-specific chemotherapy to the selective targeting of tumorigenic signal transduction pathways. Farnesyltransferase inhibitors (FTIs) target proteins needing prenylation for functioning, thus inhibiting a wide variety of molecular targets crucial for cell proliferation and survival. Tipifarnib (R115777, Zarnestra®), a potent and specific inhibitor of Farnesyltransferase, can attain strong inhibition of tumor growth in preclinical models. As a single agent, tipifarnib has demonstrated activity in several hematologic malignancies, namely acute myeloid leukemia, myelodysplastic syndrome, chronic myeloid leukemia and multiple myeloma. However, considering the complexity of the molecular aberrations implicated in the pathogenesis of hematologic neoplasms, it is rather unlikely that monotherapy with tipifarnib will serve as a stand-alone treatment approach. Indeed, improved results have been achieved by combining tipifarnib with other anticancer agents, whereas the first efforts for the identification of molecular predictors of response are reporting intriguing results. Ongoing trials are anticipated to define the exact role of tipifarnib in the treatment of hematologic malignancies.

Small-molecule anticancer agents kill cancer cells by harnessing reactive oxygen species in an iron-dependent manner

2018 ◽  
Vol 16 (9) ◽  
pp. 1465-1479 ◽  
Author(s):  
Sara R. Fedorka ◽  
Kevin So ◽  
Ayad A. Al-Hamashi ◽  
Ibtissam Gad ◽  
Ronit Shah ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Cancer Cells ◽  
Cell Lines ◽  
Small Molecule ◽  
Anticancer Agents ◽  
Reactive Oxygen ◽  
Dependent Manner ◽  
Oxygen Species ◽  
Open Chain ◽  
New Class

In the course of generating a library of open-chain epothilones, we discovered a new class of small molecule anticancer agents that has no effect on tubulin but instead kills selected cancer cell lines by harnessing reactive oxygen species in an iron-dependent manner.

scholarly journals Cyano- and Ketone-Containing Selenoesters as Multi-Target Compounds against Resistant Cancers

Cancers ◽  
2021 ◽  
Vol 13 (18) ◽  
pp. 4563
Author(s):  
Nikoletta Szemerédi ◽  
Simona Dobiasová ◽  
Noemi Salardón-Jiménez ◽  
Annamária Kincses ◽  
Márta Nové ◽  
...  
Keyword(s):  
Wound Healing ◽  
Atpase Activity ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Biological Assessment ◽  
One Pot ◽  
Potential Applications ◽  
Induced Apoptosis ◽  
Derivatives Of ◽  
Target Activity

Fifteen selenocompounds, comprising of eight ketone-containing selenoesters (K1–K8, also known as oxoselenoesters) and seven cyano-containing selenoesters (N1–N7, known also as cyanoselenoesters), have been designed, synthesized, and evaluated as novel anticancer agents. These compounds are derivatives of previously reported active selenoesters and were prepared following a three-step one-pot synthetic route. The following evaluations were performed in their biological assessment: cytotoxicity determination, selectivity towards cancer cells in respect to non-cancer cells, checkerboard combination assay, ABCB1 inhibition and inhibition of ABCB1 ATPase activity, apoptosis induction, and wound healing assay. As key results, all the compounds showed cytotoxicity against cancer cells at low micromolar concentrations, with cyanoselenoesters being strongly selective. All of the oxoselenoesters, except K4, were potent ABCB1 inhibitors, and two of them, namely K5 and K6, enhanced the activity of doxorubicin in a synergistic manner. The majority of these ketone derivatives modulated the ATPase activity, showed wound healing activity, and induced apoptosis, with K3 being the most potent, with a potency close to that of the reference compound. To summarize, these novel derivatives have promising multi-target activity, and are worthy to be studied more in-depth in future works to gain a greater understanding of their potential applications against cancer.

Glycolysis Inhibition as a Strategy for Hepatocellular Carcinoma Treatment?

2018 ◽  
Vol 19 (1) ◽  
pp. 26-40 ◽  
Author(s):  
A.P. Alves ◽  
A.C. Mamede ◽  
M.G. Alves ◽  
P.F. Oliveira ◽  
S.M. Rocha ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Glucose Transporter ◽  
Public Health Problem ◽  
High Morbidity ◽  
Curative Intent ◽  
Malignant Liver Tumor ◽  
Glucose Transporter 1 ◽  
Inhibition Of Glycolysis

Hepatocellular carcinoma (HCC) is the most frequently detected primary malignant liver tumor, representing a worldwide public health problem due to its high morbidity and mortality rates. The HCC is commonly detected in advanced stage, precluding the use of treatments with curative intent. For this reason, it is crucial to find effective therapies for HCC. Cancer cells have a high dependence of glycolysis for ATP production, especially under hypoxic environment. Such dependence provides a reliable possible strategy to specifically target cancer cells based on the inhibition of glycolysis. HCC, such as other cancer types, presents a clinically well-known upregulation of several glycolytic key enzymes and proteins, including glucose transporters particularly glucose transporter 1 (GLUT1). Such enzymes and proteins constitute potential targets for therapy. Indeed, for some of these targets, several inhibitors were already reported, such as 2-Deoxyglucose, Imatinib or Flavonoids. Although the inhibition of glycolysis presents a great potential for an anticancer therapy, the development of glycolytic inhibitors as a new class of anticancer agents needs to be more explored. Herein, we propose to summarize, discuss and present an overview on the different approaches to inhibit the glycolytic metabolism in cancer cells, which may be very effective in the treatment of HCC.

Targeting Membrane Receptors of Ovarian Cancer Cells for Therapy

2019 ◽  
Vol 19 (6) ◽  
pp. 449-467
Author(s):  
Zhiquan Liang ◽  
Ziwen Lu ◽  
Yafei Zhang ◽  
Dongsheng Shang ◽  
Ruyan Li ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cancer Cells ◽  
Receptor Binding ◽  
Cytoreductive Surgery ◽  
Therapeutic Strategies ◽  
Membrane Receptors ◽  
Ovarian Cancer Cells ◽  
Advanced Stage ◽  
Targeted Therapeutics ◽  
Cellular Processes

Ovarian cancer is a leading cause of death worldwide from gynecological malignancies, mainly because there are few early symptoms and the disease is generally diagnosed at an advanced stage. In addition, despite the effectiveness of cytoreductive surgery for ovarian cancer and the high response rates to chemotherapy, survival has improved little over the last 20 years. The management of patients with ovarian cancer also remains similar despite studies showing striking differences and heterogeneity among different subtypes. It is therefore clear that novel targeted therapeutics are urgently needed to improve clinical outcomes for ovarian cancer. To that end, several membrane receptors associated with pivotal cellular processes and often aberrantly overexpressed in ovarian cancer cells have emerged as potential targets for receptor-mediated therapeutic strategies including specific agents and multifunctional delivery systems based on ligand-receptor binding. This review focuses on the profiles and potentials of such strategies proposed for ovarian cancer treatment and imaging.

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