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Synthesis and Bioevaluation of Quaternary Centered 3-hydroxy-3 (alkynyl)indolin-2-one Derivatives as Potential Cytotoxic Agents and Akt Kinase Inhibitors.
Prathima, P Sai; Bikshapathi, R; Poornachandra, Y; Himabindu, V; Kumar, G Jagadeesh; Jagadeesh, N; Kumar, C Ganesh; Rao, V Jayathirtha.
Afiliación
  • Prathima PS; Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology (IICT), Uppal Road, Tarnaka, Hyderabad, 500 607, India.
  • Bikshapathi R; Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology (IICT), Uppal Road, Tarnaka, Hyderabad, 500 607, India.
  • Poornachandra Y; Medicinal Chemistry and Pharmacology Division, (IICT), Hyderabad, India.
  • Himabindu V; Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology (IICT), Uppal Road, Tarnaka, Hyderabad, 500 607, India.
  • Kumar GJ; Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology (IICT), Uppal Road, Tarnaka, Hyderabad, 500 607, India.
  • Jagadeesh N; X-ray Crystallography Division(IICT), Hyderabad, India.
  • Kumar CG; Medicinal Chemistry and Pharmacology Division, (IICT), Hyderabad, India.
  • Rao VJ; Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology (IICT), Uppal Road, Tarnaka, Hyderabad, 500 607, India.
Anticancer Agents Med Chem ; 17(14): 1963-1970, 2018 Feb 07.
Article en En | MEDLINE | ID: mdl-28403775
BACKGROUND: Alkynes are fundamental building blocks in synthetic chemistry with high pharmaceutical applications. Among the bioactive acetylenic molecules, propargylic alcohol is most important as almost all the marketed drugs contains quaternary centered propargylic alcohol functionality. OBJECTIVE: In this study we have synthesised and evaluated 3-hydroxy-3-ethynylindolin-2-one derivatives for in vitro cytotoxic activity. METHOD: An expeditious method for direct alkynylation of isatins (ketones) has been developed using tetrabutylammonium fluoride (TBAF) as a catalyst in THF solvent at room temperature under metal-free conditions. Furthermore, this method is an economically viable process that also compliments green aspects like being a ligand/metal free process under ambient conditions. This reaction tolerated a wide range of substrates with good to excellent yields (80-94%). RESULTS: The results showed that the synthesized compounds (4m, 4n and 4p) has the ability to inhibit Akt kinase activity with IC50 values ranging from 7.7 to 9.8 µM. CONCLUSION: All the 3-hydroxy-3-ethynylindolin-2-one derivatives were subjected for in vitro cytotoxic activity on five different cancer cell lines. Further, the synthesized compounds (4m, 4n and 4p) were evaluated for their ability to inhibit Akt kinase activity and exhibited good inhibition with IC50 values ranging from 7.7 to 9.8 µM..
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Citotoxinas / Inhibidores de Proteínas Quinasas / Proteínas Proto-Oncogénicas c-akt / Indoles / Antineoplásicos Límite: Humans Idioma: En Revista: Anticancer Agents Med Chem Asunto de la revista: ANTINEOPLASICOS / QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: India Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Citotoxinas / Inhibidores de Proteínas Quinasas / Proteínas Proto-Oncogénicas c-akt / Indoles / Antineoplásicos Límite: Humans Idioma: En Revista: Anticancer Agents Med Chem Asunto de la revista: ANTINEOPLASICOS / QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: India Pais de publicación: Países Bajos