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Full-Text Articles in Heterocyclic Compounds

Design And In Silico Modeling Of Heterocyclic-Based Xanthone Derivatives As Potential Anticancer Agents Through Tyrosine Kinase Inhibition, Yehezkiel Steven Kurniawan, Ervan Yudha, Nela Fatmasari, Radite Yogaswara, Harno Dwi Pranowo, Eti Nurwening Sholikhah, Jumina Jumina Mar 2026

Design And In Silico Modeling Of Heterocyclic-Based Xanthone Derivatives As Potential Anticancer Agents Through Tyrosine Kinase Inhibition, Yehezkiel Steven Kurniawan, Ervan Yudha, Nela Fatmasari, Radite Yogaswara, Harno Dwi Pranowo, Eti Nurwening Sholikhah, Jumina Jumina

Makara Journal of Science

Cancer is one of the deadliest diseases nowadays, and tyrosine kinase receptors play crucial roles in cancer cell survival, differentiation, proliferation, and migration. This study designed and developed a new inhibitor from heterocyclic-based xanthone derivatives to target two tyrosine kinase receptors, epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor (PDGFR), through in silico screening. Eighteen heterocyclic-based xanthones were evaluated through molecular docking for both receptors. All heterocyclic-based xanthones gave the root mean square deviation (RMSD) value lower than 2.00 Å. Xanthone with isobenzothiazole substituent (iBzThio) was found as the most potent inhibitor with binding energies of -10.60 and …


Dz-Bau2021-14n As Novel Pyrazolopyridine Nanocrystals: Appraisal Of Anticancer Activity Against Hct-116 And Ht-29 Colorectal Cancer Cell Lines, Zahra Kassem, Soumaiah Abou Staiteieh, Jamal Nasr, Amina Mneimneh, Ali Youssef, Nadine Darwiche, Doaa Issa, Raghida Bou Merhi, Mohammed Mehanna Oct 2021

Dz-Bau2021-14n As Novel Pyrazolopyridine Nanocrystals: Appraisal Of Anticancer Activity Against Hct-116 And Ht-29 Colorectal Cancer Cell Lines, Zahra Kassem, Soumaiah Abou Staiteieh, Jamal Nasr, Amina Mneimneh, Ali Youssef, Nadine Darwiche, Doaa Issa, Raghida Bou Merhi, Mohammed Mehanna

BAU Journal - Health and Wellbeing

Mentioning DZ-BAU2021-14 (C19H17N5O2,347.370 g/mol) developed in BAU Labs, its promising preliminary antitumor effect nominated it to be selected as a lead antiproliferative compound against colorectal cancer cell lines owing to its proved Cyclin Dependent Kinase 2 (CDK2) inhibition (Kassem et al., 2021). Solving many problems restricting traditional cancer therapy, nanotechnology is offering safety margins and targeted delivery of poorly soluble drug. The potential effect of this compound was combined with the advantages of nanotechnology, precisely nanocrystals to achieve better antiproliferative and hopeful less cytotoxic patterns. The nanocrystals DZ-BAU2021-14N were …


Preparation Of Meta-Nitrobenzoylhydrazone Ferrocenoylacetone And Synthesis On Its Basis, Zilola Abduraxmonovna Sulaymonova, Bako Bafayevich Umarov Doctor Chemical Science, Professor Aug 2021

Preparation Of Meta-Nitrobenzoylhydrazone Ferrocenoylacetone And Synthesis On Its Basis, Zilola Abduraxmonovna Sulaymonova, Bako Bafayevich Umarov Doctor Chemical Science, Professor

Chemical Technology, Control and Management

β-diketone-ferrocenoylacetone was obtained by Claisen condensation. Meta-nitrobenzoylhydrazone of ferrocenoylacetone (H2L) was synthesized by the interaction of meta-nitrobenzoic acid hydrazide with ferrocenoylacetone. On its basis, complexes with copper(II) and nickel(II) ions were synthesized. The obtained compounds were characterized by the methods of elemental analysis, IR-, 1H NMR andelectronic spectroscopy. The research results showed that H2L in solution exists in the form of a tautomeric mixture: hydrazone, α-hydroxyazine, and cyclic 5-hydroxypyrazoline forms. According to the results of IR and 1H NMR spectra, the complexes were assigned a planar-square structure, and in them the doubly deprotonated …


Synthesis Of 1-(4-Ethoxy-3-Methoxybenzyl)-1,10-Phenanthrolin-1-Ium Bromide And Its Evaluation As Antiplasmodium Through Heme Polymerization Inhibitory Activity (Hpia) Assay, Dhina Fitriastuti, Viny Alfiyah, Mustofa Mustofa, Jumina Jumina, Muhammad Idham Darussalam Mardjan Mar 2021

Synthesis Of 1-(4-Ethoxy-3-Methoxybenzyl)-1,10-Phenanthrolin-1-Ium Bromide And Its Evaluation As Antiplasmodium Through Heme Polymerization Inhibitory Activity (Hpia) Assay, Dhina Fitriastuti, Viny Alfiyah, Mustofa Mustofa, Jumina Jumina, Muhammad Idham Darussalam Mardjan

Makara Journal of Science

This study describes the development of N-benzyl-1,10-phenantrolinium salt as an antiplasmodium agent. The salt, that is, 1-(4-ethoxy-3-methoxybenzyl)-1,10-phenanthrolin-1-ium bromide, was prepared using vanillin as the starting material in four simple synthetic steps. First, the alkylation of vanillin using diethyl sulfate produced 4-ethoxy-3-methoxybenzaldehyde in 79% yield. Second, the reduction of the protected vanillin by NaBH4 through the grinding method allowed us to obtain 4-ethoxy-3-methoxybenzyl alcohol in 96% yield. Next, the bromination of the benzyl alcohol under solvent-free condition led to the formation of the corresponding benzyl bromide, which in turn underwent bimolecular nucleophilic substitution with 1,10-phenanthroline to produce the desired …