Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 22, Issue 2, 2022

Abstract: In conjunction with radio-chemotherapy, pulmonary resection is recommended for early-stage nonsmall- cell lung carcinoma but not for advanced-stage NSCLC patients having high-grade metastatic lesions. In these cases, the rapid Arc-Stereotactic body radiotherapy (Ra-SBRT) technique offers a therapeutic advantage by delivering focal irradiation to metastatic lung lesions and reduces the bystander toxicity to Read More

Abstract: Early diagnosis and accurate prognosis are significant important challenges against effective treatment of cancer and improving patient’s condition. Hitherto, many research works have tended to focus on the carcinoembryonic antigen (CEA) to detect cancers and estimate the survival rates of patients with multiple cancer types, including colorectal, breast, non-small cell lung, and pancreas cancer. Limited sensitivity an Read More

Abstract: Reactive Oxygen Species (ROS) refers to the highly reactive substances which contain oxygen radicals. Hypochlorous acid, peroxides, superoxide, singlet oxygen, alpha-oxygen, and hydroxyl radicals are the major examples of ROS. Generally, the reduction of oxygen (O2) in molecular form produces superoxide (•O2 −) anion. ROS are produced during a variety of biochemical reactions within the cell organell Read More

Background: Lung adenocarcinoma (LUAD) and squamous cell carcinoma (LUSC) are two major subtypes of Non-Small Cell Lung Cancer (NSCLC). Studies have shown that abnormal expression of glucose transport type 1 (GLUT1) in NSCLC patients has been associated with cancer progression, aggressiveness, and poor clinical outcome. However, the clinical effect of GLUT1 expression on LUAD and LUSC is unclear. Objective: Thi Read More

Background: The clinical outcomes of patients with Acute Myeloid Leukemia (AML) remain unsatisfactory. Therefore the development of more efficacious and better-tolerated therapy for AML is critical. We have previously reported anti-leukemic activity of synthetic halohydroxyl dimeric naphthoquinones (BiQ) and aziridinyl BiQ. Objective: This study aimed to improve the potency and bioavailability of BiQ compounds and i Read More

Background: SphK1 is a conserved lipid kinase, which can catalyze the formation of tumorpromoting factor sphingosine phosphate-1 (S1P). Objective: This study aimed to investigate the effect of SphK1 on the proliferation/migration of colon cancer cells and associated mechanisms. Methods: Transcription of the SphK1 gene in colon cancer cells was detected. Gene transcription of SphK1 was inhibited by transfecting Read More

Background: Cytochrome P450 1B1 (CYP1B1) is specifically expressed in a variety of tumors which makes it a promising imaging target of tumor. Objective: We aimed to design and synthesize CYP1B1 targeted chelators for the potential application in positron emission tomography (PET) imaging of tumor. Methods: 1,4,7-triazacyclononane-1,4-diiacetic acid (NODA) was connected to the CYP1B1 selective inhibitor we devel Read More

Background: This study aimed to determine the effect and mechanism of Celastrol inhibiting the proliferation and decreasing the drug resistance of cisplatin-resistant gastric cancer cells. Objective: The objective of this study was to explore the effect and mechanism of Celastrol on proliferation and drug resistance of human gastric cancer cisplatin-resistant cells SGC7901/DDP. Methods: The thiazole blue (MTT) method was used t Read More

Background: Metformin (MET) is a well-known anti-diabetic drug that also has anti-cancer effects. However, high therapeutic doses of MET on cancer cells and the low efficacy of combinatory therapeutic approaches limit its clinical application. Recent studies have shown that chrysin (CHR) can improve the pharmaceutical efficacy of MET by suppressing human telomerase reverse transcriptase (hTERT) and cyclin D1 gene ex Read More

Background: Triple-Negative Breast Cancer (TNBC) is a highly heterogeneous and invasive malignancy that is characterized by high recurrence and mortality rates as well as extremely poor prognosis. Objective: The objective of this study is to analyze T cells and Macrophages in the tumor microenvironment with the aim of identifying targets with therapeutic potential. Methods: Single-cell sequencing data of TNBC patients f Read More

Background: In the current era, the development of molecular techniques involves nano techniques, and the synthesis of nanoparticles is considered the preferred field in nanotechnology. Objective: The aim of the present work is to analyze the anticancer activity of the thymoquinone conjugated ZnO nanoparticles and understand its mechanism of action in triple-negative breast cancer cell lines MDA-MB-231. Methods: Read More

Background: EGFR (Epidermal Growth Factor Receptor) and CDK2 (Cyclin Dependent Kinase 2) are important targets in the treatment of many solid tumors and different ligands of these receptors share many common structural features. Objective: The study involved the synthesis of benzamide-substituted chalcones and determination of their antiproliferative activity as well as a preliminary evaluation of EGFR and CDK2 inhibitor Read More

Background: The lead compounds from the series of 2, 4-disubstituted quinoline-3-carboxylic acid derivatives were selected for the in-silico mechanistic study. The compounds were found selective and potent for the cancer cell. Moreover, the relevant ADME in-silico data also support the safety of lead. Objective: The objective of the study is to correlate the interaction of DNA and quinoline derivative, which was reported w Read More

Aim: The present study aims to identify the anticancer effect of novel 1H-indole-2,3-dione 3- thiosemicarbazone derivatives. These compounds could be promising anticancer agents in leukemia treatment. Background: Conventional chemotherapeutic agents accumulate in both normal and tumor cells due to nonspecificity. For effective cancer treatment, new drugs need to be developed to make chemotherapeutics selective Read More

Aim: The study aimed to determine the cytotoxic and apoptotic effect of propofol on glioma cells. Background: Propofol [2,6-diisopropylphenol] is a commonly used intravenous anesthetic. Propofol is known to have a mechanism of action on the PI3K-AKT pathway. Objective: This study aimed to evaluate the effect of propofol on the proliferation and apoptosis of human glioma cells, as well as to investigate changes in expression l Read More

Background: Marine actinomycetes are among indispensable sources of natural bioactive compounds with unique antimicrobial and anti-cancer activities. Objective: Herein, it was aimed to elucidate the bioactive potential of a marine-derived Streptomyces ovatisporus S4702T, isolated previously. Methods: Streptomyces ovatisporus S4702T was cultured in N-Z Amine broth, and extraction was carried out using different Read More

Background: Chemotherapeutics have been commonly used in cancer treatment. Objective: In this study, the effects of Cisplatin, 5-fluorouracil, Irinotecan, and Gemcitabine have been evaluated on two-dimensional (2D) (sensitive and resistance) cell lines and three dimensional (3D) spheroid structure of MDA-MB- 231. The 2D cell culture lacks a natural tissue-like structural so, using 3D cell culture has an important role in the d Read More

Background: Grade IV gliomas are classified as glioblastoma (GBM), which is the most malignant brain cancer type. Various genetic and epigenetic mechanisms play a role in the initiation and progression of GBM. MicroRNAs (miRNAs) are small, non-coding RNA molecules that belong to the main epigenetic regulatory RNA class that plays different roles in either physiological or pathological conditions, including GBM pathogenesis r Read More

Background: Hydroxytyrosol is one of the phenolic compounds of olive oil and can induce anticancer effects on colorectal cancer cells. Objective: The aim of the present study was to evaluate the free hydroxytyrosol and nano-capsulated hydroxytyrosol effects on the cell cycle arrest in HT-29 colorectal cancer cell line. Methods: The nano-capsulated hydroxytyrosol was synthesized in poly lactide-co-glycolide-co-polyacrylic acid Read More