Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 22, Issue 5, 2022

Background: Lurbinectedin was approved on June 15, 2020 by the Food and Drug Administration with the brand name ZEPZELCA as the first systematic approved therapy for patients having Small Cell Lung Cancer (SCLC). Objectives: In this review, an attempt is made to summarize different aspects of Lurbinectedin, including the pathophysiology, chemistry, chemical synthesis, mechanism of action, adverse reaction Read More

Background: The platinum (II) complexes as anticancer agents have been well explored for the development of novel analogs. Yet, none of them achieved clinical importance in oncology. At present, anticancer compounds containing platinum (II) complexes have been employed in the treatment of colorectal, lung, and genitourinary tumors. Among the platinum-based anticancer drugs, Cisplatin (cis-diamine dichloroplati Read More

Background: Cancer is a global threat to humans and a leading cause of death worldwide. Cancer treatment includes, among other things, the use of chemotherapeutic agents, compounds that are vital for treating and preventing cancer. However, chemotherapeutic agents produce oxidative stress along with other side effects that would affect the human body. Objective: The aim of the study was to reduce the oxidative stress Read More

Background: Demethylzeylasteral (ZST93), a pharmacologically active triterpenoid monomer extracted from Tripterygium wilfordii Hook F (TWHF), has been reported to exert antineoplastic effects in several cancer cell types. However, the anti-tumour effects of ZST93 in human colorectal cancer (CRC) cells are unknown. Objective: The aim of the present study was to evaluate the antitumor effects of ZST93 on cell cycle arr Read More

Background: Gastric Cancer (GC) accounts for high mortality, which seriously threatens people’s health. This study set out to probe into the effect and mechanism of miR-27b-3p on invasion and migration of GC. Methods: The miRNA sequence data of GC was acquired from The Cancer Genome Atlas (TCGA) database. The Differential Expression of miRNAs (DEMis) was acquired through R packages “edgeR” and “limma.” TargetSc Read More

Background: Circular RNAs (circRNAs) play an essential role in developing tumors, but their role in Non- Small Cell Lung Cancer (NSCLC) is unclear. Thus, the present study explored the possible molecular mechanism of circRNAs in NSCLC. Methods: Three circular RNA (circRNA) microarray datasets were downloaded from the Gene Expression Omnibus (GEO) database. Differential expressions of circRNAs (DECs) were identifi Read More

Background: Xanthatin is a plant-derived bioactive sesquiterpene lactone from the Xanthium strumarium L., and it has been used as a traditional Chinese medicine. Recently, many studies have reported that xanthatin has anticancer activity. However, a comprehensive understanding of the mechanism underlying the antitumor effects of xanthatin is still lacking. Objective: To systematically and comprehensively identify the un Read More

Background and Objective: Beauvericin (BEA), a cyclic hexadepsipeptide mycotoxin, is a potent inhibitor of the acyl-CoA: cholesterol acyltransferase enzyme 1 (ACAT1), involved in multiple tumor-correlated pathways. However, the binding mechanisms between BEA and ACAT1 were not elucidated. Methods: BEA was purified from a mangrove entophytic Fusarium sp. KL11. Single-crystal X-ray diffraction was use Read More

Background: Conventional treatment resistance remains a significant problem in cancer care. Cancer stem cells might play a major role in treatment resistance, and as a result, basic stem cell pathways are instrumental in cancer. Sonic Hedgehog signaling has not been widely studied in oral cancer, and being one of the major cancer stem cell pathways, targeting it with natural compounds could open many opportunities Read More

Background: Histone deacetylases (HDACs) are the enzymes that catalyze the removal of the acetyl group from lysine residues and regulate several biological processes. Suberoylanilide hydroxamic acid (SAHA) is a notable HDAC inhibitor that exhibited remarkable anti-proliferative efficiency by alleviating gene regulation against solid and hematologic cancers. Aim: The aim of this study was to develop new chemoth Read More

Background: According to the global cancer report 2019, the burden of cancer will exceed more than 18 million, becoming one of the major causes of global mortality rate. There is a pressing need to establish novel drug candidates for cancer treatment, though many anticancer agents are available in the market owing to their adverse effects. In recent years, quinazoline and its derivatives have been considered as a novel cl Read More

Background: Cancer disease is a serious concern globally. Global cancer occurrence is steadily increasing every year. There is always a persistent need to develop new anticancer drugs with reduced side effects or that act synergistically with the existing chemotherapeutics. Objective: Benzoxazoles are fused bicyclic nitrogen and oxygen-containing heterocyclic compounds and are considered biologically privileged scaff Read More

Background: Tyrosine Kinase Inhibitors (TKIs) can be used to inhibit cancer cell proliferation by targeting the vascular endothelial growth factor receptor (VEGFR) family. SAR131675 is a highly selective receptor tyrosine kinase inhibitor to VEGFR3 that reveals the inhibitory effect on proliferation in human lymphatic endothelial cells. However, the molecular mechanisms underlying this process are generally unclear. O Read More

Background: Using a combination of chemotherapeutic agents with novel drug delivery platforms to enhance the anticancer efficacy of the drug and minimizing the side effects, is imperative to lung cancer treatments. Objective: The aim of the present study was to develop, characterize, and optimize porous poly (D, L-lactic-co-glycolic acid) (PLGA) microparticles for simultaneous delivery of docetaxel (DTX) and celecoxib (CXB Read More

Background: Target treatment using site-specific nanosystems is a hot topic for treating several diseases, especially cancer. Objective: The study was set out to develop site-specific liposomes using ConcanavalinA (ConA) to target β- lapachone(β-lap) to human breast cancer cells. Methods: Liposomes were prepared and characterized according to diameter size, zeta potential, ConA conjugation(%) and β-lap encapsulation ef Read More

Background: Pyrimidine-5-carbonitrile has a broad spectrum of biological activities such as antiviral, antioxidant, and anticancer activities. Among similar compounds, monastrol is the most prominent cell-permeant inhibitor of mitosis; therefore, we investigated the new Pyrimidine-5-carbonitrile as a cytotoxic agent for the p53 pathway. Objective: Several new benzyloxyphenyl pyrimidine-5-carbonitrile derivatives were designed, s Read More

Background: Gold nanorods (GNRs) are very promising agents with multiple applications in medicine and biology. However, the cytotoxic effects of GNRs have not been fully explored. Objective: Therefore, the main objective of this study was to determine the selective cytotoxic effect of GNRs towards several human tumor cell lines. Methods: To address this issue, three sizes of GNRs (10-nm, 25-nm, and 50-nm) were tested ag Read More

Background: The lack of specificity, severe side effects, and development of drug resistance have largely limited the use of platinum-based compounds in cancer treatment. Therefore, copper complexes have emerged as potential alternatives to platinum-based compounds. Objective: Ternary copper (II) complex incorporated with 1-10-phenanthroline and L-tyrosine was investigated for its anti-cancer effects in HT-29 co Read More

Background: Cancer is one of the most overwhelming diseases nowadays. It is considered the second cause of death after cardiovascular diseases. Due to the diversity of its types, stages and genetic origin, there is no available drug to treat all cancers. Serious side effects and resistance of existing drugs are other problems in the struggle against cancer. In such quest, fluoroquinolones (FQs) promising as antiproliferative co Read More