Most cited article - PubMed ID 26599982
Design, Synthesis and In Vitro Activity of Anticancer Styrylquinolines. The p53 Independent Mechanism of Action
The knowledge of interactions between different molecules is undoubtedly the driving force of all contemporary biomedical and biological sciences. Chemical biology/biological chemistry has become an important multidisciplinary bridge connecting the perspectives of chemistry and biology to the study of small molecules/peptidomimetics and their interactions in biological systems. Advances in structural biology research, in particular linking atomic structure to molecular properties and cellular context, are essential for the sophisticated design of new medicines that exhibit a high degree of druggability and very importantly, druglikeness. The authors of this contribution are outstanding scientists in the field who provided a brief overview of their work, which is arranged from in silico investigation through the characterization of interactions of compounds with biomolecules to bioactive materials.
A series of 116 small-molecule 1-hydroxynaphthalene-2-carboxanilides was designed based on the fragment-based approach and was synthesized according to the microwave-assisted protocol. The biological activity of all of the compounds was tested on human colon carcinoma cell lines including a deleted TP53 tumor suppressor gene. The mechanism of activity was studied according to the p53 status in the cell. Several compounds revealed a good to excellent activity that was similar to or better than the standard anticancer drugs. Some of these appeared to be more active against the p53 null cells than their wild-type counterparts. Intercalating the properties of these compounds could be responsible for their mechanism of action.
- MeSH
- Apoptosis drug effects MeSH
- DNA metabolism MeSH
- Doxorubicin pharmacology MeSH
- HCT116 Cells MeSH
- Intercalating Agents pharmacology MeSH
- Small Molecule Libraries chemistry pharmacology MeSH
- Humans MeSH
- Models, Molecular MeSH
- Tumor Suppressor Protein p53 metabolism MeSH
- Naphthols chemical synthesis chemistry pharmacology MeSH
- Cell Proliferation drug effects MeSH
- Antineoplastic Agents chemical synthesis chemistry pharmacology MeSH
- Drug Design * MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 1-naphthol MeSH Browser
- calf thymus DNA MeSH Browser
- DNA MeSH
- Doxorubicin MeSH
- Intercalating Agents MeSH
- Small Molecule Libraries MeSH
- Tumor Suppressor Protein p53 MeSH
- Naphthols MeSH
- Antineoplastic Agents MeSH
The 46th EuroCongress on Drug Synthesis and Analysis (ECDSA-2017) was arranged within the celebration of the 65th Anniversary of the Faculty of Pharmacy at Comenius University in Bratislava, Slovakia from 5-8 September 2017 to get together specialists in medicinal chemistry, organic synthesis, pharmaceutical analysis, screening of bioactive compounds, pharmacology and drug formulations; promote the exchange of scientific results, methods and ideas; and encourage cooperation between researchers from all over the world. The topic of the conference, "Drug Synthesis and Analysis," meant that the symposium welcomed all pharmacists and/or researchers (chemists, analysts, biologists) and students interested in scientific work dealing with investigations of biologically active compounds as potential drugs. The authors of this manuscript were plenary speakers and other participants of the symposium and members of their research teams. The following summary highlights the major points/topics of the meeting.
- Keywords
- chemical biology, drug design and development, medicinal chemistry, natural compounds, new small entities, organic synthesis, pharmaceutical analysis, therapeutic proteins,
- MeSH
- Pharmacists MeSH
- Chemistry, Pharmaceutical MeSH
- Quantitative Structure-Activity Relationship MeSH
- Humans MeSH
- Intersectoral Collaboration MeSH
- Drug Compounding * MeSH
- Research Personnel MeSH
- Check Tag
- Humans MeSH
- Publication type
- Congress MeSH
- Geographicals
- Slovakia MeSH
The Eighth Central European Conference "Chemistry towards Biology" was held in Brno, Czech Republic, on August 28-September 1, 2016 to bring together experts in biology, chemistry and design of bioactive compounds; promote the exchange of scientific results, methods and ideas; and encourage cooperation between researchers from all over the world. The topics of the conference covered "Chemistry towards Biology", meaning that the event welcomed chemists working on biology-related problems, biologists using chemical methods, and students and other researchers of the respective areas that fall within the common scope of chemistry and biology. The authors of this manuscript are plenary speakers and other participants of the symposium and members of their research teams. The following summary highlights the major points/topics of the meeting.
- Keywords
- ADME, drug delivery systems, biological chemistry, biomaterials, chemical biology, drug design, nanoparticles, natural compounds, proteins and nucleic acids, synthesis, targeting,
- MeSH
- Epigenesis, Genetic MeSH
- Chemistry, Pharmaceutical methods MeSH
- Drug Delivery Systems MeSH
- Proteins chemistry MeSH
- Drug Design MeSH
- Systems Biology MeSH
- Structure-Activity Relationship MeSH
- Publication type
- Congress MeSH
- Names of Substances
- Proteins MeSH
