Synthesis and anticancer activity of open-resorcinarene conjugates

  • Bioorg Med Chem Lett. 2020 Jul 15;30(14):127275. doi: 10.1016/j.bmcl.2020.127275.
Luis Daniel Pedro-Hernández  1 ,  Carlos Hernández-Montalbán  1 ,  Elena Martínez-Klimova  2 ,  Teresa Ramírez-Ápan  1 ,  Marcos Martínez-García  3
Affiliations
  • 1. Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, Circuito Exterior, Coyoacán, C.P 04510 México, D.F., Mexico.
  • 2. Facultad de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, Circuito Interior, Coyoacán, C.P 04510 México, D.F., Mexico.
  • 3. Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, Circuito Exterior, Coyoacán, C.P 04510 México, D.F., Mexico. Electronic address: [email protected].
PMID: 32527536 DOI: 10.1016/j.bmcl.2020.127275
Abstract

The first example of conjugation of open-resorcinarenes with chlorambucil, ibuprofen, naproxen and indomethacin are presented. The cytotoxic properties of the obtained conjugates were tested against the Cancer cell lines U-251, PC-3, K-562, HCT-15, MCF-7 and SKLU-1. It was found that the conjugate with chlorambucil, naproxen or indomethacin (having 8 moieties) was toxic towards Cancer cell lines U-251 and K-562, with no activity against non-cancerous COS-7 cells. The conjugates with naproxen and indomethacin showed high selectivity towards U-251 tumor cells.

Keywords
Anticancer activity; Chlorambucil; Dendrimers; Nonsteroidal anti-inflammatory drugs; Open-resorcinarene.