Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 21, Issue 17, 2021

Background: Tumors are still among the major challenges to human health. Tumor-targeted therapy is an effective way to treat tumors based on precise medical models. Sialic acid (SA) is overexpressed on the surface of tumor cells, and Phenyl Boric Acid (PBA) can specifically bind to SA. However, studies on the use of PBA in tumor-targeted therapy are few. Objective: To summarize and analyze the characteristics and infl Read More

Background: The antimetabolite, 5-Fluorouracil (5-FU), is the only chemotherapeutic drug to significantly improve 12-month survival rates of patients with Colorectal Cancer (CRC). However, resistance to 5-FU is a major obstacle to effective treatment. The mechanism of 5-FU resistance has been discovered but is not fully known. Nuclear factor-erythroid 2-related factor 2 (Nrf2), a master regulator of cellular defense agai Read More

MiRNAs that are characterized by small non-coding RNAs orchestrate the expression of important genes involved in cancer cell development processes, including apoptosis, proliferation, angiogenesis, metastasis, and drug resistance at the post-transcriptional level. Dysregulation of miR-9 in various cancers has been reported. Recently, miR-9 has been considered as a key miRNA in various malignancies. However, its import Read More

Hypoxia pathway and aberrant miRNA expression profile play crucial roles in the development of various cancers. Recent studies have emphasized that there are many collaborations in this cases because both of them are involved in cancer cell processes, including differentiation, metastasis, and cell proliferation and signaling pathways. Further studies have elucidated that miRNAs affect the hypoxia route, and more interestin Read More

The resistance to therapy of cancer cells is a challenge for achieving an appropriate therapeutic outcome. Cancer (stem) cells possess several mechanisms for increasing their survival following exposure to toxic agents such as chemotherapy drugs, radiation, as well as immunotherapy. Evidences show that apoptosis plays a key role in the response of cancer (stem) cells and their multi-drug resistance. Modulation of both Read More

Background: Prostate cancer is the most common visceral neoplasia in men and frequently presents chemotherapy resistance. In this context, lemongrass (Cymbopogon citratus (D.C.) Stapf) has been studied since it presents many important biological activities, such as anticancer. Objective: We investigated the antitumor effect of lemongrass and in chemotherapy activity using prostate cancer cells line (DU-145). M Read More

Background: Coumarin structures were widely employed in anti-cancer drug design. Herein we focused on the modifications of C4 and C6 positions on coumarin scaffold to get novel anti-cancer agents. Objective: The objective of the current work was the synthesis and biological evaluation of a series of 4, 6-coumarin derivatives to get novel anticancer agents. Methods: Thirty-seven coumarin derivatives were designed and synth Read More

Background: The Androgen Receptor (AR) signaling functionis a critical driving force for the progression of Prostate Cancer (PCa) to bring about anti-prostate cancer agents, and AR has been proved to be an effective therapeutic target even for Castration-Resistant Prostate Cancer (CRPC). Objective: In order to discover novel anti-prostate cancer agents, we performed structural modifications based on the lead compounds Read More

Background: Pyrvinium Pamoate (PP) is an old drug approved by the FDA for the treatment of pinworm infections. Recently, it has been introduced as an anti-tumor agent, however, low aqueous solubility severely limits its potential effects. In this study, we developed a liposomal formulation of pyrvinium pamoate to investigate its in vitro cytotoxicity and in vivo efficacy against melanoma cells. Materials & Methods: As drug carri Read More

Background: In previous studies, we provided evidence suggesting the involvement of γ-synuclein in growth, invasion, and metastasis of colon cancer cells in vitro and in vivo. Among γ-synuclein downstream genes, the microtubule-associated protein 1 Light Chain 3 (LC3), an autophagy gene, was screened by gene expression profile chip analysis. Objective: We planned to investigate the functional effects of γ-synuclein o Read More

Background: Thiazolidine-4-one is a promising class of heterocyclic compounds with interesting pharmacological and biological activities, such as anticancer and antibacterial. Therefore, many researchers have synthesized thiazolidine-4-ones and evaluated their biological potential for developing new drugs. Objective: In this study, two novel thiazolidine-4-one derivatives (T1 and T2) were synthesized and evaluated for t Read More

Background: The benzimidazole and their derivatives have rich biological relevance with respect to available natural amino acids and their role in protein folding and quaternary conformations. Thus the ligand trizbenzim and their Cu(II) and Zn(II) metal complexes were prepared to induce G-quadruplex conformation even under no-salt conditions with remarkable anticancer activities. Methods: The ligand N,N',N''-Tris-(1H-benz Read More

Background: We previously synthesized two DNA intercalative Pyrimido[4’,5’:4,5]thieno(2,3-b) quinolines (PTQ), 9-hydroxy-4-(3-diethylaminopropylamino)pyrimido[4’,5’:4,5]thieno(2,3-b) quinolines (Hydroxy- DPTQ) and 8-methoxy-4-(3-diethylaminopropylamino) pyrimido[4’,5’:4,5]thieno(2,3-b) quinolines (Methoxy-DPTQ), and reported their cytotoxicity against cancer cell lines. Methods: In the pre Read More

Background: Recent advances in nanotechnology have led to the use of nanomaterials in the diagnosis of cancer by imaging techniques. Objective: This study aimed to synthesize fluorescein-conjugated gold nanoparticles and study the parameters affecting the loading of fluorescein on synthesized coated gold nanoparticles with the ability to be used in medical diagnostic methods. Methods: The synthesized gold nanopar Read More

Background: Recently, products of Multi-Component Reactions (MCR’s) acquired special attention due to their wide range of pharmacological activities especially therapeutic activities. In the market it was found that many pharmacological drugs containing the pyran and pyridine nucleus that were produced through MCR’s were found. Objective: This work aims to synthesize target molecules not only possess anti-tumour a Read More

Minor changes are required in the Funding information and the acknowledgement for the article entitled “Organosulphur Compounds Induce Apoptosis and Cell Cycle Arrest in Cervical Cancer Cells via Downregulation of HPV E6 and E7 Oncogenes” in “Anti-Cancer Agents in Medicinal Chemistry, 2021, Vol. 21, No. 3, pp. 393-405.” The correct Funding information and Acknowledgement is given below: FUNDING: This pro Read More