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Anticancer Agents Med Chem 2022 May 19. Epub 2022 May 19.

Institute of Immunology, Faculty of Medicine, Central University of Venezuela, 50109, Los Chaguaramos 1050-A, Caracas, Venezuela.

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. Read More

Anticancer Agents Med Chem 2022 May 19. Epub 2022 May 19.

Department of Dermatology, the First Affiliated Hospital of Chongqing Medical University, Chongqing 400010, China.

Background: Melanoma is a highly invasive and metastatic malignant tumor originating from melanocytes and is associated with a poor prognosis. Surgical resection and chemotherapy are currently the main therapeutic options for malignant melanoma; however, their efficacy is poor, highlighting the need for the development of new, safe, and effective drugs for the treatment of this cancer.

Objective: To investigate the effects of alantolactone (ALT) on the proliferative, migratory, invasive, and apoptotic ability of malignant melanoma cells and explore its potential anticancer mechanism. Read More

Anticancer Agents Med Chem 2022 May 19. Epub 2022 May 19.

School of Pharmacy, Fudan University, Lane 826, Zhangheng Road, Shanghai 201203, PR China.

Aim: The main aim of the this study was to improve the solubility, reduce side effect and increase the therapeutic efficacy of CSL by using functionalized graphene oxide as carrier, to fulfill chemo-photothermal therapy.

Background: Celastrol (CSL), which is extracted from the traditional Chinese medicinal plant Tripterygiumwilfordii, has been reported significant antitumor activity in vitro and in vivo cancer models. However, disadvantages with regard to solubility, short plasma half-life and toxicity hinder its use in pharmaceutical application. Read More

Anticancer Agents Med Chem 2022 Apr 21. Epub 2022 Apr 21.

Department of Natural Products, National Institute of Pharmaceutical Education & Research (NIPER), S.A.S Nagar, Mohali-160062, Punjab, India.

Flavonoids, a class of polyphenolic secondary metabolites, are present in fruits, vegetable beverages such as wine and tea abundantly. Flavonoids exhibit a diverse array of pharmacological activities, including anticancer activity, and are toxic to cancer cells but not harmful to healthy cells. Besides, humans and animals cannot synthesize flavonoids, which leads to a dramatic increase in the consumption of plant flavonoids. Read More

Anticancer Agents Med Chem 2022 Apr 21. Epub 2022 Apr 21.

Department of Oncology, Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, China.

Background: Tanshinone IIA (Tan IIA) exerts a significant inhibitory effect on various tumor cells since it induces cell apoptosis and affects the proliferation, differentiation, metastasis and invasion of tumor cells. However, the mechanism underlying the antitumor activity of Tan IIA has not been totally elucidated.

Objective: This study aimed to uncover the role of Tan IIA in colorectal cancer (CRC) and its potential mechanism of action. Read More

Anticancer Agents Med Chem 2022 Apr 21. Epub 2022 Apr 21.

The Third Clinical Medicine College, Nanjing University of Chinese Medicine, Nanjing 210029, Jiangsu Province, China.

Background: Gastric cancer is a common global cancer disease. So far, the best choice for diagnosis and treatment of gastric cancer includes surgical resection, chemotherapy, and other targeted drug therapies, however, the overall survival rate of gastric cancer patients is still very low. Hypoxic microenvironment facilitates tumor cells to develop tolerance to chemotherapy and radiotherapy, and promotes the early invasion and metastasis of various tumors. Read More

Anticancer Agents Med Chem 2022 Apr 21. Epub 2022 Apr 21.

Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi - 221005, Uttar Pradesh, India.

Glioblastoma multiforme (GBM) is among the most critical and aggressive carcinomas of CNS, characterised by poor prognosis, low survival rate and difficult clinical correlations. Current treatment opportunities have proved to be insufficient due to high chemoresistance, and relapse of the disease with enhanced malignancy. Molecular diagnostics and epigenetic profiling of GBM have discovered several signaling pathways and cellular mediators which play key roles in triggering GBM phenotypic manifestations via somatic and genetic aberrations and recruitment of GBM stem-like cells (GSCs). Read More

Anticancer Agents Med Chem 2022 Apr 21. Epub 2022 Apr 21.

Conju-probe, San Diego, CA, USA.

Anticancer Agents Med Chem 2022 May 17. Epub 2022 May 17.

Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

Background: Xenografts of various human cancers in nude mice provide a helpful model in cancer research. This study aimed to develop a xenograft mouse model of MCF-7 breast cancer using injectable estradiol valerate.

Methods: Thirty healthy female C57 nu/nu mice were engrafted with three protocols to establish an MCF-7 tumor. Read More

Anticancer Agents Med Chem 2022 May 9. Epub 2022 May 9.

Faculty of Medicine, Near East University, Nicosia 99138.

Background: Triple-negative breast cancer is challenging to treat due to its heterogeneity and lack of therapeutic targets. Hence, systemic chemotherapy is still the mainstay in TNBC treatment. Unfortunately, patients commonly develop chemo-resistance. Read More

Anticancer Agents Med Chem 2022 May 9. Epub 2022 May 9.

Shanghai Municipal Hospital of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai.

Background And Purpose: Osteosarcoma is the commonly seen type of primary malignant bone tumors in children and adolescents. Partial patients with osteosarcoma cannot tolerate the side effects of chemotherapy drugs. Hence, it is urgent to find anti-osteosarcoma drugs with low side effects. Read More

Anticancer Agents Med Chem 2022 May 9. Epub 2022 May 9.

División de Inmunología, Centro de Investigación Biomédica de Occidente (CIBO)-Instituto Mexicano del Seguro Social (IMSS), Sierra Mojada No. 800, Col. Independencia, 44340, Guadalajara, Jalisco, Mexico.

Cervical Cancer (CC) is one of the most prevalent cancer-related pathologies in the female population. It is considered the second leading cause of cancer-related deaths in developing countries. The most important etiological factor for the development of CC is the persistent infection with high-risk human papillomavirus. Read More

Anticancer Agents Med Chem 2022 May 9. Epub 2022 May 9.

State Key Laboratory of Southwestern Chinese Medicine Resources, Hospital of Chengdu University of Traditional Chinese Medicine, School of Pharmacy and College of Medical Technology, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

Indole and spiro-fused oxoindole 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 of proteolysis targeting chimeric (PROTAC) technology that employs ubiquitin-proteasome system (UPS) to eliminate disease-associated proteins has been witnessed, thus opening a promising avenue to the discovery of new indole-related drugs. In this review, we focus on summarizing the achievements on small molecule PROTACs that involve indole/spiro-fused oxoindole scaffolds in the part of ligands of the protein of interest (POI). Read More

Anticancer Agents Med Chem 2022 May 9. Epub 2022 May 9.

Department of Hepatobiliary and Pancreatic Surgery, First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325000, China.

Objective: This study aimed to determine the effects of berbamine on pancreatic cancer as well as the underlying mechanisms.

Methods: The pancreatic cancer cells were treated with different concentrations of berbamine and then subjected to cell viability assay, colony formation assay, cell cycle analysis, and apoptosis detection. Western blotting and immunofluorescence analysis were performed to investigate the mechanisms underlying biological effects of berbamine on the pancreatic cancer cells. Read More

Anticancer Agents Med Chem 2022 May 16. Epub 2022 May 16.

School of Pharmacy, University of Nottingham Malaysia, Jalan Broga, Semenyih - 43500, Selangor, Malayisa.

Ocimum sanctum is a sacred herb of India and is commonly known as 'Tulsi' or 'Holy Basil' in regional languages of the country. Various parts of O. sanctum are recognised to have remarkable therapeutic efficacy, and are therefore used in Indian traditional medicine system, Ayurveda. Read More

Anticancer Agents Med Chem 2022 May 13. Epub 2022 May 13.

Department of Gynecologic Oncology, Shandong Cancer Hospital and Institute, Shandong First Medical University and Shandong Academy of Medical Sciences, Jinan, Shandong, China.

Background: Glutamine is one of the primary nutrients utilized by cancer cells for energy production and biosynthesis. Hence, interfering with glutamine metabolism may impose anti-tumor effects.

Objective: In this study, we assessed the anti-tumorigenic effects of glutaminase-1 enzyme (GLS1) inhibition in endometrial cancer in vitro and in vivo. Read More

Anticancer Agents Med Chem 2022 May 13. Epub 2022 May 13.

Department of Pharmaceutics, Swamy Vivekananda College of Pharmacy, Elayampalayam, Namakkal, Tamilnadu 637205, India.

Background: Cervical cancer is one of the leading causes of female death, with a mortality rate of over 200,000 per year in developing countries. . Despite a decrease in cervical cancer occurrences in developed countries over the last decade, the frequency of the disease in developing nations continues to climb at an alarming rate, particularly when it is linked to the human papillomavirus (HPV). Read More

Anticancer Agents Med Chem 2022 May 13. Epub 2022 May 13.

Leibniz Institut für analytische Wissenschaften - ISAS e.V. Bunsen-Kirchhoff-Str.1144139 Dortmund, Germany.

Background Incidence rates and prevalence of cancer are substantially high globally. New safe therapeutic drugs are endorsed to overcome high toxicity and poor safety profile of clinical anticancer agents. Objectives As antineoplastic Vosaroxin is a commercial fluoroquinolone (FQ); we hypothesize that superlative antiproliferation activity of lipophilic FQs/TFQs series correlate to their acidic groups and C8-C7 ethylene diamine Chelation Bridge along with bulky dual halogenations. Read More

Anticancer Agents Med Chem 2022 May 13. Epub 2022 May 13.

Pamukkale University, Faculty of Medicine, Department of Physiology, Denizli, Turkey.

Background: Src family tyrosine kinases play a potential role in Bcr-Abl induced leukemogenesis. Src kinase inhibitors are reported as selective inhibitors of chronic myeloid leukemia.

Objective: Since there is an inhibitive effect of Src kinase inhibitors on chronic myeloid leukemia, indole derivatives (C-1, C-2, C-3) previously found as potent inhibitors of Src kinase were tested against chronic myeloid leukemia in this study. Read More

Anticancer Agents Med Chem 2022 May 11. Epub 2022 May 11.

Center of Biotechnology and Microbiology, Abdual Wali Khan University Mardan.

Schiff bases and their transition metal complexes play an important role in the field of medicine, in particular in the treatment of cancer. Since the discovery of the cisplatin anticancer activity, great efforts have focused on the rational design of metal-based anticancer drugs that can be potentially used for the treatment of cancer. However, drug resistance and significant side effects greatly limit its clinical application. Read More

Anticancer Agents Med Chem 2022 May 11. Epub 2022 May 11.

Pharmaceutical Chemistry Division, Chandigarh College of Pharmacy, Landran, Punjab-140301, India.

Cancer involves the uncontrolled division of cells resulting in abnormal cell growth due to various gene mutations and is considered the second major cause of death. Due to drug resistance to current anticancer drugs, cancer incidence is rising, and seeking effective treatment is a major concern. Natural products are prospective to yield unique molecules, as nature is a leading source of various drug molecules due to plenty of pharmacologically active molecules. Read More

Anticancer Agents Med Chem 2022 ;22(9):1826-1836

Department of Pharmaceutical Sciences, School of Pharmacy, University of Jordan, Amman 11942, Jordan.

Background: Lung cancer remains the leading cause of cancer-related deaths worldwide. Hence, novel therapeutic approaches targeting crucial pathways are needed to improve its treatment. Previous studies have verified the involvement of the estrogen pathway, mediated through estrogen receptor β (ERβ), in the development and progression of lung carcinogenesis. Read More

Anticancer Agents Med Chem 2022 May 1. Epub 2022 May 1.

Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Ghudda, Bathinda, India.

Collagen is the most important structural protein and also a main component of extra-cellular matrix (ECM). It plays a role in tumor progression. Collagen can be regulated by altering it's biosynthesis pathway through various signaling pathways, receptors and genes. Read More

Anticancer Agents Med Chem 2022 May 1. Epub 2022 May 1.

Department of Hepatobiliary and Pancreatic Surgery, The Second Affiliated Hospital of Kunming Medical University, Kunming, Yunnan 650101, China.

Objective: To investigate the therapeutic potential of Berbamine-loaded lipid nanoparticles (BBM-NPs) in pancreatic cancer.

Methods: Dopamine polymerization-polylactide-TPGS nanoparticles were synthesized to prepare BBM-NPs, and the change of particle size of BBM-NPs was measured. Cell Counting Kit-8 (CCK8) assay, plate cloning experiment and apoptosis analysis were performed to evaluate the cytotoxicity of BBM-NPs against the pancreatic cancer cells (PANC-1 and AsPC-1). Read More

Anticancer Agents Med Chem 2022 May 1. Epub 2022 May 1.

Department of Medicinal Chemistry and Biology, International Humanitarian University, 25A, Fontanskaya road, Odessa, 65009, Ukraine.

Over the past 55 years of research, various experimental methods have been developed for the total synthesis of the anticancer camptothecin, a potent antitumor antibiotic, and its numerous active derivatives. The discoveries made in the study of the synthetic pathways of the camptothecin heterocyclic core have contributed significantly to the theory and strategy of directed organic synthesis aimed at finding effective anticancer drugs. The synthetic medicinal chemistry of camptothecin, the development of structures of anticancer camptothecin analogues and the mechanism of their activity in inhibiting the growth of different types of lung, ovarian, breast, pancreas and stomach cancers are analyzed. Read More

Anticancer Agents Med Chem 2022 May 1. Epub 2022 May 1.

School of Food and Biological Engineering, Hefei University of Technology, Hefei 230601, China.

Background: GRPR is over-expressed in cancer cells and is a potential drug target for the treatment of cancer. PD176252, as the most representative non-peptide inhibitor of GRPR, can inhibit the growth of cancer cells, but its low selectivity to cancer cells and normal cells limits its further application.

Objective: The aim of this study was to design and synthesize novel GRPR inhibitor with stronger anti-cancer activity and higher affinity with GRPR than the lead compound PD176252. Read More

Anticancer Agents Med Chem 2022 Apr 26. Epub 2022 Apr 26.

Eskişehir Technical University, Faculty of Science, Department of Biology, Turkey.

Introduction: Ovarian cancer is the deadliest gynecological malignancy, usually not detected until the late stages. In vitro cell culture is a method used to study the behavior of cells in a controlled environment. Turmeric has attracted the attention of scientists due to its anticancer potential. Read More

Anticancer Agents Med Chem 2022 Apr 26. Epub 2022 Apr 26.

Eskişehir Technical University, Faculty of Science, Department of Biology.

Introduction: Ovarian cancer is the deadliest gynecological malignancy. The aim of this study is to examine the anticancer effects of L-Citrulline in HeLa cell culture.

Materials-methods: HeLa cells were cultured in complete Eagle's Minimum Essential Medium. Read More

Anticancer Agents Med Chem 2022 Apr 26. Epub 2022 Apr 26.

Trakya University, School of Medicine, Turkey.

Background: Abiraterone acetate (AA) is a selective inhibitor of CYP17 α-hydroxylase which is crucial for androgen biosynthesis. Apigenin (Api) is a natural plant-derived flavonoid with potent antiproliferative and anti-migration effects.

Objectives: We aimed to investigate the possible role of Api in combination with the androgen receptor inhibitor AA in the treatment of androgen-sensitive human prostate cancer LNCaP cells. Read More

Anticancer Agents Med Chem 2022 Apr 26. Epub 2022 Apr 26.

Department of Pharmaceutical Sciences, School of Pharmacy, University of Jordan, Amman 11942, Jordan.

Background: Lung tumors express high levels of aromatase enzyme compared to surrounding normal tissue. Inhibition of aromatase has emerged as a recent therapeutic approach for the treatment of breast cancer. However, the role of aromatase inhibition in lung cancer treatment requires further investigation. Read More