Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 22, Issue 13, 2022

The growth of nanotechnology has revolutionized the diagnosis and treatment of diseases with high precision and effectiveness. Nanoparticles (NPs) represent a major point of attention in the scientific field, with an increasing number of studies revealing promising results. The unique physicochemical properties, biocompatibility, and highly developed chemical properties of gold nanoparticles (AuNPs) have promoted br Read More

Background: A high yielding green protocol has been developed and delineated for the synthesis of 3,3- di(indolyl)indolin-2-ones, potentially bioactive compounds, involving one pot aqueous medium condensation of isatin with indole in the presence of VOSO4. The synthesized compounds were screened for their carbonic anhydrase inhibitory activity against human (h) isoforms hCA I, hCA II, hCA IX, and hCA XII. These non- Read More

Glioblastoma, an aggressive brain cancer, demonstrates the least life expectancy among all brain cancers. Because of the regulation of diverse signaling pathways in cancers, the chemotherapeutic approaches used to suppress their multiplication and spread are restricted. Sensitivity towards chemotherapeutic agents has been developed because of the pathological and drug-evading abilities of these diverse mechanis Read More

Background: Disease-modifying therapy in cancer can be defined as long-term treatment that has a beneficial outcome on the course of cancer, affecting the underlying pathophysiology of cancer. The anticancer potential of polyphenols is widely studied. However, there is a significant gap between experimental data obtained in vitro and in vitro and the current role of polyphenols in cancer therapy. Objective: In this article, Read More

Microbial L-asparaginase is the most effective first-line therapy used in the treatment protocols of paediatric and adult leukemia. Leukemic cells’ auxotrophy for L-asparagine is exploited as a therapeutic strategy to mediate cell death through metabolic blockade of L-asparagine using L-asparaginase. Escherichia coli and Erwinia chrysanthemi serve as the major enzyme deriving sources accepted in clinical practice, and t Read More

Background: Colon cancer is one of the most important causes of death in the entire world. New pharmacological strategies are always needed, especially in resistant variants of this pathology. We have previously reported that drugs such as menadione (MEN), D, L-buthionine-S,R-sulfoximine or calcitriol, used in combination, enhanced cell sensibility of breast and colon tumour models, due to their ability to modify the oxidativ Read More

Background: Despite the dynamic development of medicine, globally cancer diseases remain the second leading cause of death. Therefore, there is a strong necessity to improve chemotherapy regimens and search for new anticancer agents. Pyridocarbazoles are compounds with confirmed antitumor properties based on multimodal mechanisms, i.e. DNA intercalation and topoisomerase II-DNA complex inhibition. One of the Read More

Background: Coumarin is a functional compound with a pronounced wide range of biological activities and has recently been shown to have anticancer effects on various human cancer cells. Cisplatin is widely used in treating many cancers, but its effectiveness is limited due to acquired resistance and dose-related side effects. Objective: This study aimed to reveal the chemosensitizing ability of novel synthesized coumari Read More

Background: Isatin (1H-indole-2,3-dione) and its derivatives have been utilized in a variety of biological activities. Anticancer compounds were the most extensively highlighted and explored among the range of beneficial properties. Objective: Herein, we report the targeting effect of halogenated isatin derivatives on cancer cell mitochondria and their antiproliferative mechanism. Methods: A series of novel 5-halo-Isati Read More

Aim: This study aimed to investigate the anticancer effect and the underlying mechanisms of organoantimony (III) fluoride on MDA-MB-231 human breast cancer cells. Methods: Five cancer and one normal cell line were treated with an organoantimony (III) compound 6-cyclohexyl-12- fluoro-5,6,7,12-tetrahydrodibenzo[c,f][1,5]azastibocine (denoted as C4). The cell viability was detected by MTT assay. Induction of cell death w Read More

Background: Lung cancer is one of the leading causes of cancer-related deaths worldwide. Platycodin D (PD), a major pharmacological constituent from the Chinese medicinal herb named Platycodonis Radix, has shown potent anti-tumor activity. Also, it is reported that PD could inhibit cellular growth in the non-small-cell lung carcinoma (NSCLC) A549 cell line. However, the underlying mechanism is not fully clarified. Methods: C Read More

Background: Poly (ADP-ribose) polymerase (PARP) plays a key role in DNA damage repair. A novel compound (E)-N'-(2,3-dibromo-4,5-dihydroxyphenyl)-N-(phenylcarbamothioyl)formimidamide (DDPF-20) with excellent PARP inhibitory activity was synthesized. Objective: In this study, we aimed to clarify the mechanism of the novel PARP inhibitor DDPF-20 against lung cancer by inducing DNA damage and inhibiting angi Read More

Background: The demand for millet-based diets has increased significantly in recent years due to their beneficial effects on human health. Foxtail Millet (Setaria italica (L.) P. Beauv, previously known as Panicum italicum L., referred as FTM in this manuscript) seeds have been not only used as astringent and diuretic agents, but they are also used to treat dyspepsia and rheumatism. Recent studies have shown that solvent extra Read More

Background: Aberrant expression of cell adhesion molecules and matrix metalloproteinase (MMPs) plays a pivotal role in tumor biological processes, including progression and metastasis of cancer cells. Targeting these processes and acquiring a detailed understanding of their underlying molecular mechanism are an essential step in cancer treatment. Dexamethasone (Dex) is a type of synthetic corticosteroid h Read More