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Author: search.filters.author.Chotsaeng, NawasitSubject: search.filters.subject.SAR

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    Synthesis and Cytotoxicity Evaluation of Novel C-3 Aminocarbamate Pregnenolone Derivatives
    (2025-03-06)
    Charoenying, Patchanee
    ;
    Chotsaeng, Nawasit
    Cancer is one of the leading causes of death worldwide. There are many ongoing studies in the search for new treatments or drugs to combat cancer. Similarly, in this research, twelve 3-aminocarbamate pregnenolones (2a–2l) were designed, synthesized, and evaluated for their cytotoxicity against five cancer cell lines: Human hepatocellular carcinoma (HepG2), Human colon adenocarcinoma (HT-29), Human oral cavity carcinoma (KB), Human breast adenocarcinoma (MCF-7), Murine leukemia (P388), and one normal cell line, African green monkey kidney fibroblast (Vero), using the MTT assay. Notably, 3-aminobenzylcarbamate pregnenolone (2b), 3-diaminoheptylcarbamate pregnenolone (2f), and 3-diaminopropanolcarbamate derivative (2i) were the most potent against these cancer cell lines. Specifically, for P388 cell lines, these compounds were more potent than the positive control drug, vinblastine sulfate salt. Results from the SAR study demonstrated that the length of the alkyl chain of diaminocarbamate derivatives was crucial for their anticancer properties. These findings will be useful in the future research and development of anticancer drugs.
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    Synthesis and Anti-Plant Pathogenic Fungal Activity of Flavokawain-Derived Flavones and Related Flavones Against Rhizoctonia solani
    (2024-01-03)
    Onnom, Panuwat
    ;
    Chotpatiwetchkul, Warot
    ;
    Meesin, Jatuporn
    ;
    Thapanapongworakul, Pilunthana
    ;
    Kittiwongwattana, Chokchai
    Flavones are organic compounds in the flavonoid family that have a diverse range of biological functions. In this research, many flavones with various substituents were designed and synthesized from flavokawains A, B, and C, and their chalcone derivatives via an iodinecatalyzed oxidative cyclization process. All synthetic flavones were investigated for antifungal activities against Rhizoctonia solani, a plant pathogenic fungus. At 400 µg, most of the substances did not inhibit the tested species and R. solani growth was inhibited by only obromoflavone (40) by 74.88±0.91%. This indicated that the detrimental effect of flavones depends on the type and position of substituent, with the ortho bromo group showing the most promise. The molecular docking study on the succinate dehydrogenase (SDH) enzyme revealed that the bromophenyl moiety (ring B) is a key molecular substructure of the flavone fungicide. The findings of this study will be used to develop novel plant pathogenic fungicides.
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    Design, Synthesis, and Structure-Activity Relationship (SAR) Studies of Ketone-Isobenzofuranone Hybrid Herbicides
    (2023-02-01)
    Chotsaeng, Nawasit
    Thirty-five ketone-isobenzofuranone hybrids (1–35) were designed, synthesized, and evaluated for their herbicidal activity against Chinese amaranth (Amaranthus tricolor) and barnyard grass (Echinochloa crus-galli). The structure-activity relationship (SAR) results revealed that the position and type of substituent were crucial for activity. The o-substituted derivatives outperformed the m- and p-substituted derivatives. Compounds with strong electron-donating groups (OH, OMe) had low activity, while those with heterocycles (N-methylpyrrole, furan, and thiophene) had a moderate herbicidal effect. Compounds with a weak electron-donating group (Me) and weak, moderate, and strong electron-withdrawing groups (F, Cl, Br, and NO<inf>2</inf>) showed promising herbicidal activity. Among these, the o-F substituted compound (20) was the most effective against Chinese amaranth, and the o-Cl substituted compound (23) was the most potent against barnyard grass. This is the first time the herbicidal potential of ketone-isobenzofuranone hybrids has been studied. The discovery of current chemical clues would be beneficial for the development of novel herbicides.