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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Defant, Andrea Mancini, Ines Tomazzolli, Rossella Balzarini, Jan |
| Description | Country affiliation: Italy Author Affiliation: Defant A ( Dipartimento di Fisica, Università degli studi di Trento, Povo, Trento, Italy.) |
| Abstract | In search for more effective drugs against HIV infection acting as non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of new molecules with hybrid structures based on the natural product (+)-calanolide A and the synthetic molecule -APA, known as potent and selective inhibitors of this enzyme, were selected by docking calculations. A convergent synthetic strategy gave 21 compounds with a 2H-pyran-2-one structural unit and bearing isosteric modifications, which were tested against HIV-infected CEM cell cultures. Only compound 6 (4-((2-(1H-indol-3-yl)ethyl)amino)-6-methyl-2H-pyran-2-one) displayed inhibitory activity (EC50 : 25-50 µM). However, it was associated with a relatively high cytostatic effect on human T lymphocyte (CEM) cell cultures, not easily predictable, neither by the chemical structure nor by the computational approach. Although this drug design has failed in selecting a novel scaffold for NNRTIs, the results have driven the interest towards new potential antitumor molecules showing activity against L1210 murine leukemia and HeLa cervix carcinoma cells, among which compound 21 (6-methyl-4-((2-(naphthalen-1-yl)ethyl)sulfonyl)-2H-pyran-2-one) was the most effective (IC50 : 0.95 and 2.9 µM, respectively). |
| File Format | HTM / HTML |
| ISSN | 03656233 |
| Issue Number | 1 |
| Volume Number | 348 |
| e-ISSN | 15214184 |
| Journal | Archiv der Pharmazie |
| Language | English |
| Publisher | Wiley-VCH Verlag |
| Publisher Date | 2015-01-01 |
| Publisher Place | Germany |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology Anti-hiv Agents Chemical Synthesis Pharmacology Drug Design Hiv Reverse Transcriptase Antagonists & Inhibitors Hiv-1 Drug Effects Pyrans Reverse Transcriptase Inhibitors Animals Antineoplastic Agents Cell Proliferation Dose-response Relationship, Drug Genetics Metabolism Enzymology Hela Cells Humans Inhibitory Concentration 50 Mice Molecular Docking Simulation Molecular Structure Structure-activity Relationship Transfection Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Drug Discovery Pharmaceutical Science |
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