Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 19, Issue 11, 2019

Background: Cancer is a multi-factorial disease including alterations in the cell signalling pathways. Currently, several drugs are in use to treat cancer but such drugs show negative side effects on normal cells and cause severe toxicity. Methods: The current research is mainly focused on medicinal plants with potential therapeutic efficacy in the treatment of cancer without any adverse effects on normal cells. In this regar Read More

Introduction: Amidst the numerous effective therapeutic options available for the treatment of Diffuse Large B-cell Lymphoma (DLBCL), about 30-40% of patients treated with first-line chemoimmunotherapy still experience a relapse or refractory DLBCL. This has necessitated a continuous search for new therapeutic agents to augment the existing therapeutic arsenal. Methods: The dawn of Computer-Aided Drug Design (CA Read More

Objective: Many experiments have revealed the anti-tumor activity of spiro-quinazolinone derivatives on different cell types. Exposing KG1-a cells to N-(4- tert- butyl- 4'- oxo- 1'H- spiro [cyclohexane- 1, 2'- quinazoline]- 3'(4'H)- yl)- 4- methyl benzenesulfonamide (4t-CHQ), as an active sub-component of spiroquinazolinone benzenesulfonamides, the experiment investigated the possible mechanisms that manifest the role of Read More

Background: 9-anilinoacridines are acting as DNA-intercalating agents which plays an important role as antitumor drugs, due to their anti-proliferative properties. Some anticancer agents contain 9- anilinoacridines such as amsacrine (m-AMSA), and nitracrine (Ledakrine) have been already developed. Methods: In this study, novel 9-anilinoacridines substituted with thiazines 4a-r were designed, synthesized, characteri Read More

Background: Gastric Cancer (GC) is a frequently common malignancy. Recent studies have reported Rab1A as an activator of mTORC1, and the mTOR1 pathway is involved in regulating Gli1 expression in several cancers. Only a few studies have been performed to explore the relationship between Rab1A and p-S6K/Gli1in GC. Methods: Immunohistochemistry (IHC) was performed to explore the association of Rab1A/p-S6K/G Read More

Background: Pyrazolo[3,4-d]pyrimidine scaffold was reported to possess potent cytotoxic and CDK2 inhibitory activity as analogue of roscovitine. Objective: To design and synthesize novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidine derivatives as bioisosters of roscovitine with potential cytotoxic and CDK2 inhibitory activity. Methods: A series of novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidines were designed and synthe Read More

Background: Peptide-based agents are used in molecular imaging due to their unique properties, such as rapid clearance from the circulation, high affinity and target selectivity. Many of the radiolabeled peptides have been clinically experienced with diagnostic accuracy. The aim of this study was to investigate in vivo biological behavior of [99mTc(CO)3(H2O)3]+ radiolabeled glycylglycine (GlyGly). Methods: Glycylglycine was ra Read More

Background: Parallel to the safety of liver resections, new chemotherapy drugs have emerged for the control of liver metastases. However, there is unclear evidence about the combination of intensive BVZ-therapy and extended resections. The main aim was to analyse the impact of Bevacizumab (BVZ) in terms of liver safety and tolerability in two experimental models: a basal-toxicity situation and after major hepate Read More

Background and Purpose: Patrinia villosa Juss is an important Chinese herbal medicine widely used for thousands of years, but few reports on the ingredients of the herb have been presented. In this study, we aim to isolate the bioactive compound from the plant. Material and Methods: The air-dried leaves of P. villosa (15kg) were extracted three times with 70% EtOH under reflux. The condensed extract was suspended in H2O a Read More

Background: Mitomycin C (MMC) is an anti-cancer drug used for the treatment of breast cancer with limited therapeutic index, extreme gastric adverse effects and bone marrow suppression. The purpose of the present study was the preparation of a dual-targeted delivery system of MMC for targeting CD44 and LHRH overexpressed receptors of breast cancer. Methods: MMC loaded LHRH targeted chonderosome was prep Read More

Background: Vitamin D (VD) deficiency affects individuals of different ages in many countries. VD deficiency may be related to several diseases, including cancer. Objective: This study aimed to review the relationship between VD deficiency and cancer. Methods: We describe the proteins involved in cancer pathogenesis and how those proteins can be influenced by VD deficiency. We also investigated a relationship between Read More