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Indolyl-α-keto-1,3,4-oxadiazoles: Synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerization.
Tantak, Mukund P; Malik, Monika; Klingler, Linus; Olson, Zachary; Kumar, Anil; Sadana, Rachna; Kumar, Dalip.
Afiliación
  • Tantak MP; Department: Department of Chemistry Birla Institute of Technology and Science, Pilani 333 031, India.
  • Malik M; Department: Department of Chemistry Birla Institute of Technology and Science, Pilani 333 031, India.
  • Klingler L; Department: Department of Natural Sciences, University of Houston - Downtown, Houston, TX 77002, USA.
  • Olson Z; Department: Department of Natural Sciences, University of Houston - Downtown, Houston, TX 77002, USA.
  • Kumar A; Department: Department of Chemistry Birla Institute of Technology and Science, Pilani 333 031, India.
  • Sadana R; Department: Department of Natural Sciences, University of Houston - Downtown, Houston, TX 77002, USA. Electronic address: sadanar@uhd.edu.
  • Kumar D; Department: Department of Chemistry Birla Institute of Technology and Science, Pilani 333 031, India. Electronic address: dalipk@pilani.bits-pilani.ac.in.
Bioorg Med Chem Lett ; 37: 127842, 2021 04 01.
Article en En | MEDLINE | ID: mdl-33556575
A series of novel indolyl-α-keto-1,3,4-oxadiazole derivatives have been synthesized by employing molecular iodine-mediated oxidative cyclization of acylhydrazones. In vitro anti cell proliferation activity of these derivatives against various cancer cells lines such as human lymphoblast (U937), leukemia (Jurkat & SB) and human breast (BT474) was investigated. Among the synthesized indolyl-α-keto-1,3,4-oxadiazoles 19a-p, only one compound (19e) exhibited significant antiproliferative activity against a panel of cell lines. The compound 19e with 3,4,5-trimethoxyphenyl motif, endowed strong cytotoxicity against U937, Jurkat, BT474 and SB cancer cells with IC50 values of 7.1, 3.1, 4.1, and 0.8 µM, respectively. Molecular docking studies suggested a potential binding mode for 19e in the colchicine binding site of tubulin. When tested for in vitro tubulin polymerizaton, 19e inhibited tubulin polymezations (IC50 = 10.66 µM) and induced apoptosis through caspase 3/7 activation. Further, the derivative 19e did not cause necrosis when measured using lactate dehydrogenase assay.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxadiazoles / Tubulina (Proteína) / Moduladores de Tubulina / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxadiazoles / Tubulina (Proteína) / Moduladores de Tubulina / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: India Pais de publicación: Reino Unido