N-Glycoside of Indolo[2,3-]pyrrolo[3,4-]carbazole LCS1269 Exerts Anti-Glioblastoma Effects by G2 Cell Cycle Arrest and CDK1 Activity Modulation: Molecular Docking Studies, Biological Investigations, and ADMET Prediction.

Indolo[2,3-]pyrrolo[3,4-]carbazole scaffold is successfully used as an efficient structural motif for the design and development of different antitumor agents. In this study, we investigated the anti-glioblastoma therapeutic potential of glycosylated indolocarbazole analog LCS1269 utilizing in vitro, in vivo, and in silico approaches. Cell viability was estimated by an MTT assay.

Open surgery: Still a great option to treat patients with post-traumatic arteriovenous fistulas: A case report.

Background: In the modern era of endovascular surgery percutaneous interventions are being widely used to treat a number of vascular disorders including arteriovenous fistulas (AVF). Still, patients with hostile anatomy or complicated cases such as large post-traumatic AVFs may be successfully treated using conventional vascular surgery.

Case Summary: This paper presents state-of-the-art treatment options in subjects with post-traumatic AVFs and a case-report of a successful open surgical approach in a patient with a 25 year old history of a post-traumatic AVF between the common femoral artery and common femoral vein.

Modified Technogenic Asphaltenes as Enhancers of the Thermal Conductivity of Paraffin.

The low thermal conductivity of paraffin and other organic phase change materials limits their use in thermal energy storage devices. The introduction of components with a high thermal conductivity such as graphene into these materials leads to an increase in their thermal conductivity. In this work, we studied the use of inexpensive carbon fillers containing a polycyclic aromatic core, due to them having a structural similarity with graphene, to increase the thermal conductivity of paraffin.

Tailoring of Dissimilar Friction Stir Lap Welding of Aluminum and Titanium.

An approach was proposed to optimize dissimilar friction stir lap welding of aluminum and titanium alloys. The basic concept of the new technique included (i) the plunging of the welding tool solely into the aluminum part (i.e.

A novel glycosylated indolocarbazole derivative LCS1269 effectively inhibits growth of human cancer cells in vitro and in vivo through driving of both apoptosis and senescence by inducing of DNA damage and modulating of AKT/mTOR/S6K and ERK pathways.

In recent decades, indolocarbazole glycosides containing sugar moieties have attracted attention due to their diverse anti-tumor activities. In the present study, a series of new indolo [2,3-a]pyrrolo [3,4-c]carbazole derivatives were synthesized for the first time. First of all, we have shown that compound 6e (LCS1269) had the most pronounced effect on inhibiting tumor growth in the transferable solid and non-solid murine tumors as compared with other synthesized indolocarbazole derivatives.

Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.

Prostate cancer is the second most common type of cancer among men. Its main method of treatment is chemotherapy, which has a wide range of side effects. One of the solutions to this challenge is targeted delivery to prostate cancer cells.

PSMA-targeted small-molecule docetaxel conjugate: Synthesis and preclinical evaluation.

Prostate cancer is one of the most commonly diagnosed men's cancers and remains one of the leading causes of cancer death. The development of approaches to the treatment of this oncological disease is an ongoing process. In this work, we have carried out the selection of ligands for the creation of conjugates based on the drug docetaxel and synthesized a series of three docetaxel conjugates.