Delving into the Latest Updates on N.D. Zelinsky Institute of Organic Chemistry with Synapse

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This study focused on the synthesis of secosteroids with good antiproliferative properties against hormone-dependent breast cancer. A straightforward and efficient method for synthesizing secosteroid - 1,3,4-oxadiazole hybrids was developed starting from 13α-hydroxy-3-methoxy-13,17-secoestra-1,3,5(10)-trien-17-oic acid hydrazide. The cyclization of hydrazide moiety with CS₂ into 1,3,4-oxadiazole-2(3H)-thione fragment followed by sulfur alkylation resulted in the formation of various secosteroid - 2-mercapto-1,3,4-oxadiazole hybrids. These novel compounds were evaluated for their antiproliferative activity against the hormone-dependent human breast cancer cell line MCF-7. Among the synthesized hybrids, compounds 3i, 3o, and 3q displayed notable antiproliferative effects, with IC₅₀ values ranging from 6.5 to 8.9 µM, comparable to the reference drug cisplatin. Furthermore, compound 3i showed minimal toxicity toward non-cancerous hFB-hTERT fibroblasts, indicating high selectivity. Compounds 3o and 3q exhibited antiestrogenic activity. Additionally, their effects on PARP and Bcl-2 suggest a pro-apoptotic mechanism of action. These findings highlight the potential of secosteroidal hybrids as promising candidates for the development of new anti-breast cancer agents targeting ERα and apoptosis pathways.

01 Jun 2025·Carbohydrate Research

Structure of O-polysaccharide from the Azospirillum himalayense ptl-3T lipopolysaccharide

Article

Author: Sigida, Elena N ; Zdorovenko, Evelina L ; Fedonenko, Yulia P ; Konnova, Svetlana A ; Dmitrenok, Andrey S

Lipopolysaccharide was extracted with hot aqueous phenol from cells of Azospirillum himalayense ptl-3^T, a diazotrophic Gram-negative bacterium isolated from Himalayan valley soil, India. The O-polysaccharide (OPS) was released by mild acid hydrolysis of the lipopolysaccharide and was structurally characterized by chemical analyses and by 1D and 2D NMR spectroscopy. The following structure of the OPS trisaccharide repeating unit was established. →3)-α-l-Fucp-(1→3)-α-l-Fucp-(1→3)-α-d-Rhap4NAc-(1→.

01 Jun 2025·Journal of Hazardous Materials

Integrated toxicity assessment of complex chemical mixtures in catalytic reactions

Article

Author: Ananikov, Valentine P ; Kolesnikov, Andrey E ; Egorova, Ksenia S

Catalytic cross-coupling reactions, such as the Mizoroki-Heck reaction, play a crucial role in synthetic chemistry but pose significant environmental and health risks due to the toxicity of reaction components and their mixtures. In this study, we conducted a comprehensive cytotoxicity assessment of individual substances and complex reaction mixtures at different stages of the Mizoroki-Heck reaction. We demonstrate that the cytotoxicity of these mixtures often deviates from predictions on the basis of individual components due to synergistic and antagonistic interactions, with chlorobenzene-containing mixtures mostly exhibiting the lowest toxicity. Furthermore, our findings suggest that noncovalent interactions, including halogen bonding and π-stacking, significantly influence cytotoxicity. Notably, incomplete conversion of the reactants leads to an increase in mixture toxicity, emphasizing the importance of optimizing the reaction conditions. This study underscores the necessity of revising current chemical safety assessment strategies to account for complex molecular interactions in catalytic reactions.

100 Deals associated with N.D. Zelinsky Institute of Organic Chemistry

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Pipeline

Pipeline Snapshot as of 28 Jun 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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