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.

Vasculogenic mimicry, the formation of vascular channels lined with tumor cells of a highly malignant phenotype, is currently considered as an additional system of blood supply of the tumor. Experimental studies in vivo have repeatedly demonstrated that vascular channels form in the areas of a tumor with a low density of blood vessels. It is supposed that the formation of a network of these channels inside the tumor maintains homeostasis and prevents early necrosis within it. In this work, bifunctional compounds based on a combination of quinazoline and hydroxamic acid in one molecule were examined for the ability to inhibit the migration of tumor cells and vasculogenic mimicry.

New somatostatin analogs containing the fragments of adamantane, coumarin, tetrahydrocarbazole, and palmitic acid of the general formula R-Phe-D-Trp-Lys(Boc)-Thr-OMe have been synthesized. The structure of the conjugates combines a peptide fragment, which has affinity for somatostatin receptors (sstr), and a nonpeptide fragment, which potentially possesses antitumor activity. Presumably, the compounds synthesized are the agonists of sstr. The amide bond between the peptide and nonpeptide fragments has been formed using the carbodiimide method and the method of activated esters. The structures of the conjugates have been confirmed by mass spectrometry (ESI + ) and 1 H NMR spectroscopy. The antitumor activity of the conjugates has been examined by the MTT test on human lung adenocarcinoma (A549), human prostate adenocarcinoma (PC3), human colon cancer (HCT-116), human breast cancer (MCF7), and acute human T‑cell leukemia (Jurkat) cell lines. Compounds selectively inhibiting the growth of A549 cells have been identified.

A kilogram-scale synthesis of fingolimod drug substance was developed using a 30-L pilot setup. The target product was obtained by a four-step procedure in 99.8% purity and 47% overall yield.

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.

A four-step synthesis of abiraterone acetate in good yield was developed. The synthesis employed Suzuki cross-coupling in the key step and produced the target compound in 99.8% 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.

The native hormone somatostatin plays an important role in vivo by acting on multiple targets via a family of five receptors to produce a broad spectrum of biological effects. Some peptide analogs of this enzyme are widely used in clinical practice. However, their clinical efficacy is limited because of some disadvantages. In this respect, the search for new drugs of this type is a critical task. In this review, we have summarized trends in the synthesis and biological effects of peptide somatostatin analogs since 1978 and future prospects for the development of these anticancer drugs.

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 method for using an F complex for pilot-scale production of Z-Phe-D-Trp-Lys(ε-Boc)OH – a protected tripeptide used in making synthetic analogs of somatostatin is described. This method involves regeneration of pentafluorophenol and allows the target compound to be prepared with a main substance content of ~99%.

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.