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Article
Preparation of 155Tb-labeled short somatostatin analog
The complex of the short somatostatin analog, DOTA—Phe—D-Trp—Lys—Thr—OMe (DOTA is 1,4,7,10-tetrraazacyclododecane-1,4,7,10-tetraacetic acid), with the theragnostic 155Tb radionuclide was obtained for the first ti...
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Article
Synthesis of precursors for obtaining targeted radiopharmaceuticals based on short peptides, analogs of the hormone somatostatin
New precursors with various linkers for the construction of targeted radiopharmaceuticals based on a pharmacophore fragment of the hormone somatostatin, tetrapeptide H-Phe-d-Trp-Lys-Thr-OH, were synthesized. The ...
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Article
Comparison of the Reactivities of Tyrosine–Proline-Based Dipeptides toward Acylation with Nitrophenyl Benzoates
The reactivities of the L-Tyr–L-Pro dipeptide and its analog with a hydroxymethyl group instead of carboxy group in the proline moiety were compared by studying the kinetics of their acylation with d...
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Article
Reactivity of Tyrosyl–Proline toward Benzoylation in Aqueous 1,4-Dioxane
The kinetics of the reaction of L-tyrosyl-L-proline (Tyr–Pro) with di- and trinitrophenyl benzoates in aqueous 1,4-dioxane (40 wt % of water) were studied in the temperature range 298–313 K. The reaction rate ...
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Article
Effect of Derivatives of Hydroxamic Acids on Vasculogenic Mimicry
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 studi...
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Article
Reactions of CH acids with the Michael acceptors in the presence of potassium carbonate
New 2-cyclohexenone derivatives were synthesized via the Michael reaction in the presence of potassium carbonate. These derivatives containing the acetyl substituent in position 6 are of special interest due to t...
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Article
Synthesis and Antitumor Activity of Conjugates Based on the Phe-D-Trp-Lys-Thr Peptide Fragment of Somatostatin
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...
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Article
Synthesis and properties of 1,2-dihydro-4(3H)-quinazolinones
We modified the preparative-scale method for the synthesis of 2-aryl 1,2-dihydro-4(3H)-quinazolinone derivatives obtained in high yields by the reaction of new and commercially available aromatic aldehydes with a...
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Article
Pentapeptide analogs of somatostatin containing a thiazolidine fragment: synthesis and cytotoxic activity
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 teste...
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Article
Synthesis and cytotoxic activity of Boc-protected pentapeptide amide analogs of somatostatin
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 com...
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Article
Potassium carbonate as a base for generation of carbanions from CH-acids in organic synthesis
A reaction of CH-acids with electrophilic agent (Michael acceptors, alkyl and allyl halides, dihaloalkanes and -alkenes, etc.) in the presence of potassium carbonate constitutes a convenient method for the elonga...
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Article
Synthetic Peptide Analogs of Somatostatin: Trends in the Synthesis of and Prospects in the Search for New Anticancer Drugs
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 ...
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Article
Alkylation of NH-, OH-, and SH-acids in the presence of potassium carbonate
An easily scalable, economocal, and more safe method for the preparation of 3-chloromethyl-4-methoxybenzaldehyde was developed. The latter was subjected to reactions with NH-, OH-, and SH-acids in the presence...
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Article
Reaction of CH-acids with Michael acceptors in the presence of potassium carbonate. Syntheses of 6-acetyl- and 3,5-dialkylcyclohex-2-enones
The reaction of acetylacetone with α,β-enones in the presence of potassium carbonate affords 6-acetylcyclohex-2-enones. The assembly of two acetoacetate and one alkanal molecules gives 3,5-dialkylcyclohex-2-en...
