БОРИС СЕМЕНОВИЧ ЗІМЕНКОВСЬКИЙ

УДК 016:615.1(092)

У ювілейному виданні висвітлено основні віхи життя, наукової, науковопедагогічної та організаційної діяльності відомого українського науковця в галузі фармацевтичної, органічної і біоорганічної хімії, ректора Львівського
національного медичного університету імені Данила Галицького (1998–2023 рр.), академіка Національної Академії медичних наук України, доктора фармацевтичних наук, професора, заслуженого працівника Вищої школи України, лавреата Державної премії України в галузі науки і техніки, заслуженого професора ЛНМУ ім. Данила Галицького, почесного доктора Люблінського медичного університету, дійсного члена НТШ та низки
громадських академій.
Хронологічний покажчик друкованих праць, авторських свідоцтв та патентів знайомить з науковим доробком ученого.
Це видання стане важливим корисним ресурсом для науково-педагогічної спільноти, аспірантів, студентів, а також істориків, бібліографів та всіх, хто цікавиться історією львівської медичної і фармацевтичної науки та освіти.

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Effect of Bisphenol-Formaldehyde Resin on Physico-Mechanical Properties of Road Bitumen.

A bisphenol-formaldehyde resin was synthesized using the polycondensation method of bisphenol A with formaldehyde. Road bitumen has been modified with this resin. The possibility of its use as a road petroleum bitumen modifier has been established for different contents of the synthesized resin. It has been established that the introduction of synthesized bisphenol-formaldehyde resin into the composition of bitumen significantly increases its heat resistance. The synthesized resin and modified bitumens were characterized using IR spectroscopy. The change in the composition and properties of the bitumen modified with bisphenol-formaldehyde resin has been described. 

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Synthesis and biological activity of rhodanine-furan conjugates: A review.

Rhodanines are recognized as privileged heterocycles in medicinal chemistry. The main achievements include the development of drug-like molecules with numerous biological activities as well as approved drugs. The Furan nucleus is considered one of the promising heterocyclic cores in medicinal chemistry that showed numerous ranges of activity. The combination of several heterocycles in a one molecule commonly provides much more interest in the enhanced activity profile of its analogs than their parent separate constituents. Such conjugates are promising objects for modern medicinal chemistry. In this review paper recent advances in the synthesis and biological activities rhodanine-furan conjugates which its application in the different field of drug discovery.

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Synthesis, analysis adme-tox parameters and anti-cancer activity of n-(5-r-benzylthiazole-2-yl)-2-morpholin-4-yl-2-thioxoacetamides

Aim. Study of the synthesis, analysis of ADME - Tox parameters and anti-cancer activity of a series of N-(5-R-benzylthiazole-2-yl)-2-morpholin-4-yl-2-thioxoacetamides.
Methods. Organic synthesis, 1H NMR spectroscopy, analytical method, in silico ADME-Tox analysis and in vitro cytotoxicity assay.
Results. The series of new N-(5-R-benzylthiazole-2-yl)-2-morpholin-4-yl-2-thioxoacetamides was synthesized according to a convenient synthetic method. Their structures were confirmed by 1H NMR spectroscopy and microanalyses. Using the internet resources of SwissADME and pkCSM-pharmacokinetics, the ADME - Tox profiles of the synthesized compounds were calculated. It was determined that the substances were within the optimal limits of  bioavailability. All compounds meet the criteria of drug similarity according to the rules of Lipinski, Weber, Egan and Mugge. It is also determined that low toxicity is predicted for these substances. The synthesized compounds were tested in vitro for their antitumor activity according to the Developmental Therapeutic Program of the National Cancer Institute (NCI) (www.dtp.nci.nih.gov) against 60 cancer lines in the concentration of 10 μM. Human tumor
cell lines from nine different cancer types were used: leukemia, melanoma, lung, colon, CNS, ovarian, kidney, prostate an d breast cancer. Screening results showed that, in most cases, these compounds are of low activity. An exception is the renal cancer line UO-31, which was moderately sensitive to all synthesized compounds.
Conclusions. A series of 2-aminothiazole hybrids containing morpholine moiety was synthesized and studied in silico ADME-Tox profiles. The ADME-Tox profiles indicated good oral bioavailability and low toxicity. Synthesized compounds were tested in vitro for their anti-cancer activity. They showed moderate antiproliferative activity.
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Current trends of chemoinformatics and computer chemistry in drug design: A review.

A crucial direction in the progress of modern medical chemistry is the development and improvement of theoretical investigation methods of drugs mechanisms of action, predicting their activity, and virtual design of new drugs. This review describes the history of targeted search for biologically active compounds, current in silico approaches and tools used in the rational design of potential drugs, in particular the main computational strategies used in modern drug design are presented and outlines the main methodologies for implementing these strategies. 

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