A5076047738- Estrogen and related hormone effects
- Pharmacogenetics and Drug Metabolism
- Hormonal Regulation and Hypertension
- Steroid Chemistry and Biochemistry
- Prostate Cancer Treatment and Research
- Cancer therapeutics and mechanisms
- Hormonal and reproductive studies
- 14-3-3 protein interactions
- Computational Drug Discovery Methods
- Organic Chemistry Cycloaddition Reactions
- Click Chemistry and Applications
- Synthesis and Biological Evaluation
- Protein Degradation and Inhibitors
- Radiopharmaceutical Chemistry and Applications
- Cancer, Lipids, and Metabolism
- Cancer Treatment and Pharmacology
- Chemical Synthesis and Analysis
- Inflammatory mediators and NSAID effects
- Histone Deacetylase Inhibitors Research
- Drug Transport and Resistance Mechanisms
Institute of Biomedical Chemistry
2017-2024
Institute of Physiologically Active Compounds
2021
Russian Academy of Sciences
2018
This review deals with studies of researches novel CYP17A1 steroidal inhibitors and relative compounds published over the last ten years. The contains six chapters in which targets well-known inhibirors (abiraterone galeterone), anti-cancer anti-proliferative activities them major metabolites new synthetic analogs, addition another nitrogen-containing androstane pregnane derivatives are considered. In 354 structures steroid efficiency data Analysis literature allows us to consider as...
Derivatives of 3β-hydroxyandrost-5,16-diene and 3β-hydroxyandrost-5-ene containing 2-oxazoline, 2-benzoxazole, 2-benzimidazole substituents at C-17 position were synthesized. Docking the synthesized compounds into active site human CYP17A1 predicted their high affinity for enzyme. Of 6 new compounds, 5 suppressed proliferation prostate carcinoma cells LNCaP PC-3, activity oxazoline benzimidazole derivatives androsta-5,16-diene significantly exceeded known anticancer agents abiraterone galeterone.
Abstract Steroid derivatives modified with nitrogen containing heterocycles attract attention as anticancer agents for prostate cancer treatment. In this study we have developed a simple and convenient procedure preparation of 17(20)‐21‐norpregnene androst‐16‐ene 2’‐oxazolinyl 2’‐benzoxazolyl derivatives, based on the reaction an appropriately steroidal carboxylic acid 1,2‐amino alcohols or o‐aminophenol. Using method conducted synthesis series new steroid hybrids differing either in...
The review is dedicated to results of investigations steroid conjugates published predominantly over the past decade. It consists three parts in which data concerning biological activity with known drugs, dimers, and some natural compounds, their fragments related derivatives analogs, are discussed. structures 231 anti-cancer properties presented.
Background: The goal of this study was to evaluate the anticancer and testosteroneinhibitory effects 2‘-[(E) androst-5-en-17-ylidene]methyl-4‘,5‘-dihydro-1‘,3‘-oxazole-3β-oleate (Alsevirone-NF). Materials Methods: PC-3, DU-145, LnCap 22rv1 prostate cancer cell lines were used for MTT assay. subcutaneous xenografts in Balb/c nude mice vivo efficacy experiments. Testosterone level determined after repeated administration Abiraterone 20, 100 or 200 mg/kg vs Alsevirone-NF 5, 25 50 daily 14 days....
The aim of this study was to explore the mechanisms action alsevirone in prostate cancer (PC) vitro and vivo: CYP17A1 inhibition, cytotoxic, apoptotic, antitumor effects comparison with abiraterone. CYP17A1-inhibitory activity investigated rat testicular microsomes using high-performance liquid chromatography. Testosterone levels were evaluated enzyme-linked immunoassay. IC50 values calculated for PC3, DU-145, LNCaP, 22Rv1 cells MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium...
BACKGROUND: Prostate cancer is the most frequently diagnosed type of in men developed countries. It dependent upon androgens and could be effectively combated by androgen deprivation therapy. Reduction synthesis can accomplished through inhibition enzyme 17α-hydroxylase/17.20-lyase (CYP17A1), which catalyzes two sequential reactions production androgens. Steroid derivatives modified with nitrogen-containing heterocycles attract attention as antineoplastic agents for prostate treatment due to...