Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 23, Issue 10, 2023

Background: The side effects of ionising radiation include skin changes, dry mouth, hair loss, low blood count, and the mutagenic effect on normal cells when utilized in radiotherapy for cancer treatment. These radiations can cause damage to the cell membrane, lipids, proteins, and DNA and generate free radicals. Evidence reports stated that radiotherapy accounts for 17-19% of secondary malignancies, labelling this treatme Read More

Tumour relapse, chemotherapy resistance, and metastasis continue to be unsolved issues in cancer therapy. A recent approach has been to scrutinise drugs used in the clinic for other illnesses and modify their structure to increase selectivity to cancer cells. Chloroquine (CQ) and hydroxychloroquine (HCQ), known antimalarials, have successfully treated autoimmune and neoplastic diseases. CQ and HCQ, well-kno Read More

Background: Kaurane-type diterpenoids, obtained from various natural sources, have shown many biological activities, including anti-inflammatory and antitumor effects. Caracasine, an ent-kaurane diterpenoid isolated from the flowers of Croton micans, was shown to induce apoptosis in leukaemia cell lines. Objective: The present study aimed to ascertain the compound’s mechanism of cell death induction using two leuka Read More

Introduction: Tubulin polymerization inhibitors induce cancer cell death; therefore, they can be developed as chemotherapeutic agents. We hypothesized that hybrid compounds, including the trans-stilbene moiety contained in resveratrol and penta-1,4-dien-3-one contained in curcumin, could inhibit tubulin polymerization. Methods: Twenty-six hybrid stilbene and pentadienone compounds were designed and synthesized. T Read More

Indole and spiro-fused oxindole frameworks widely exist in a variety of natural bioactive products, pharmaceuticals, and drug candidates, featuring unique functions in the regulation of proliferation, infiltration, and metastasis of cancer cells. In recent years, significant progress in proteolysis targeting chimeric (PROTAC) technology that employs ubiquitin-proteasome system (UPS) to eliminate disease-associated proteins has b Read More

Lupeol (LP) and Mangiferin (MG) have beneficial effects on health. However, their pharmacokinetic properties can affect their bioavailability when administered orally. Therefore, their incorporation as a vehicle in a hybrid matrix of ZnO and PLGA could contribute to improving bioavailability. Methods: This study aimed to develop this matrix and evaluate the optical and bioactive properties obtained by the solvent emulsion and Read More

Background: Carbonic Anhydrases (CAs) are a family of metalloenzymes that catalyze the reversible interconversion of CO2 and water to bicarbonate and proton. CA isoforms I, II, IX, and XII are considered physiologically and pharmacologically relevant. Objective: The objective of this study is to synthesize potent and selective tumor-associated CA IX and XII inhibitors. Methods: A library of 17 coumarin derivatives clubb Read More

Objective: We reported herein the synthesis of novel arylazo derivatives 3a-e incorporating isoquinoline moiety. Methods: A coupling reaction of 2-(6,7-dimethoxy-3,4-dihydroisoquinolin-1-yl)acetonitrile 1 with diazotized heterocyclic amines 2 in ethanol in the presence of sodium acetate to give arylazo derivatives 3a-e. Results: Cytotoxic effect of five arylazo derivatives on breast carcinoma MCF7 and hepatocellular carcinoma He Read More

Background: Erianin is an active dibenzyl compound isolated from Dendrobium officinale and Dendrobium chrysotoxum and there are very few studies on molecular mechanisms and drug targets of erianin. In addition, there is no study investigating the anti-cancer effect of erianin on neuroblastoma cells. Objective: The aim of the study is to investigate the anticancer effect of erianin and the underlying mechanism of t Read More

Background: Nasopharyngeal carcinoma (NPC) is a malignant tumor of the nasopharynx. Objective: Here, we aimed to understand better the molecular basis for arctigenin (ARG)'s ability to promote NPC 5- 8F cell invasion. Methods: We tested the effects of several doses of ARG on 5-8F cells that had been cultured in vitro. We estimated the metabolic activity of cells by The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltet Read More

Aim: Human carbonic anhydrase (CA, EC 4.2.1.1) isoforms IX and XII are validated antitumor/ antimetastatic drug and tumor imaging targets with sulfonamide inhibitors and monoclonal antibodies in clinical development. Coumarins act as isoform-selective inhibitors of these isoforms over the cytosolic and mitochondrial ones. Methods: We report the synthesis and in vitro CA inhibitory evaluation of a large panel of coumarins in Read More