As potential HDAC inhibitors, new derivatives of 1,2-dihydroquinazolin-4-one in combination with alkyl hydroxamic acid have been proposed. The latter were obtained by the interaction of an alkyl hydroxyamide derivative of anthranilamide with various aldehydes by boiling in ethanol with yields of 73-99% and were characterized by H-1-NMR and ESI-MS spectra..ytotoxic properties of target compounds were also studied by the MTT test on cell lines of human tumors (MCF-7, A549, PC-3, and HCT-116). Based on the SAR results, the resulting products can potentially be used as a new candidate drug for a promising anti-cancer strategy.

Pentapeptide analogs of somatostatin containing an (R)-1,3-thiazolidine fragment (Thz) of the general formula X-Thz-Phe-D-Trp-Lys(Y)-Thr-Z were synthesized for the first time. The synthesized compounds were tested for cytotoxic activity against three cancer cell lines (MCF-7, PC3, and HCT-116) and against human embryo fibroblasts.

An effective four-step synthesis of the tripeptide H-Pyr-His-Trp-OH that is used to produce synthetic gonadoliberin agonists was developed. The synthesis was carried out without adding and removing protecting groups and could produce the target compound with >98% purity.

New Boc-protected pentapeptide amides of the general formula Boc-Cys(Boc)-Phe-d-Trp-Lys(Boc)-Thr-NHR, which are analogs of the natural hormone somatostatin, were synthesized. The cytotoxic activity of the new compounds was evaluated against the cancer cell lines MCF-7, PC 3, and HCT-116 by the MTT test, and some of these compounds were found to exhibit activity at micromolar concentrations.

preparative method for a one-step synthesis of amino acid amides was developed using dimethyldichlorosilane. This method produces amides with yields ranging from 45% to 89% and purity greater than 95%. Neither racemization nor inversion of the configuration of the asymmetrical center in the starting α-amino acid occurs during the reaction.

A preparative method for a one-step synthesis of amino acid amides was developed using dimethyldichlorosilane. This method produces amides with yields ranging from 45% to 89% and purity greater than 95%. Neither racemization nor inversion of the configuration of the asymmetrical center in the starting α-amino acid occurs during the reaction.

A new improved liquid-phase method of preparation of the 7-8 fragment of octreotide and its derivatives was developed. This method allows to prepare target dipeptide with a purity of more than 95 %, is easily scalable and provides regeneration of the HOBt.

An unusual five-step synthesis of H-beta-Ala-Pro-DabNHBz diacetate (a muscular nicotinic acetylcholine receptor antagonist) has been delineated through Hofmann-type rearrangement as a final step to build the target skeleton. The synthesis has been carried out using a protecting group free strategy and employed readily available reagents as the starting materials. (C) 2014 Elsevier Ltd. All rights reserved.

A method for preparing leuprorelin acetate – a synthetic agonist of natural gonadotropin-releasing hormone - was developed, using liquid-phase peptide synthesis. The new method yields target peptide with a main substance content of > 99% on a semi-industrial scale.

A new process for the preparation of octreotide (synthetic analog of natural hormone somatostatine) has been developed based on the 4+2+2 strategy using liquid-phase peptide synthesis. The proposed method is easy to implement and ensures large-scale synthesis of the target peptide with up to 56.4% yield.

A method was developed for the production of octreotide – a synthetic analog of the natural hormone somatostatin - by liquid-phase peptide synthesis using the 4 + 2 + 2 strategy. The new method is easily scalable and produces the target peptide with a yield of 56.4%.

A three-step alternative synthesis of lenalidomide was developed. The proposed route produced the desired product in 59.8% yield and 99.6% purity.

A new effective liquid-phase method for preparation of triptorelin (agonist of gonadotropin-releasing hormone) was developed. This method based on buserelin production and allows the collaborative process of producing two products using the same peptide blocks.

A three-step alternative synthesis of lenalidomide has been developed. This route compares favorably to the previously developed synthetic process and ensures obtaining of a highly pure product (99.6%) with improved overall yield (59.8%).

Effective and large scale method for preparation H-Phe-D-Trp-Lys(e-Boc)-Thr-OMe key tetrapeptide intermediate for somatostatine analogs synthesis was developed.