title: Effect of new hybrids based on 5,16-pregnadiene scaffold linked to an anti-inflammatory drug on the growth of a human astrocytoma cell line (U373).
abstract: In spite of the fact that anaplastic astrocytoma is an uncommon disease, very often the pathology of this disease is associated with lethal effects due to the late diagnosis and unspecific treatments. This paper reports the synthesis and the biological effect on the growth of U373 cell line (human anaplastic astrocytoma) of new hybrid compounds based on 5,16-pregnadiene scaffold linked to an anti-inflammatory drug (6a-e). Moreover, we also determined the cell growth effect of five non-steroidal anti-inflammatory drugs (naproxen, ibuprofen, ketoprofen, indomethacin and sulindac) as well as the free steroidal alcohol 5. The results from this study indicated that sulindac as well as compound 5 decreased the number of U373 cells at different concentrations. However, when an anti-inflammatory drug was bound to the steroidal structure (5), the resulting compounds (6a-e) showed an enhanced biological effect with exception of hybrid 6c. Furthermore, derivative 6e (sulindac hybrid) did not allow cell growth during six days of experiment at a concentration of 10 μM. The overall data indicated that these molecules showed an anti-proliferative activity on anaplastic astrocytoma cell line.
authors: Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, D.F. 04510, Mexico. Electronic address: mariana6618@hotmail.com.
authors: Mariana
authors: M
authors: Garrido
authors: Departamento de Medicina Genómica y Toxicología Ambiental, Instituto de Investigaciones Biomédicas, Universidad Nacional Autónoma de México, D.F. 04510, Mexico.
authors: Aliesha
authors: A
authors: González-Arenas
authors: Facultad de Química, Departamento de Biología, Universidad Nacional Autónoma de México, Mexico.
authors: Ignacio
authors: I
authors: Camacho-Arroyo
authors: Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana-Xochimilco, México, D.F., Mexico.
authors: Marisa
authors: M
authors: Cabeza
authors: Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, D.F. 04510, Mexico.
authors: Belén
authors: B
authors: Alcaraz
authors: Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, D.F. 04510, Mexico.
authors: Eugene
authors: E
authors: Bratoeff
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018929:Cell Culture Techniques; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D011245:Pregnadienes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013467:Sulindac / Q000737:chemistry*; D013997:Time Factors
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D011245:Pregnadienes; D013467:Sulindac
keywords: Anaplastic astrocytoma; Anti-inflammatory drugs; Hybrids; Pregnadiene derivatives