Synthesis of novel tadalafil analogues and their evaluation as phosphodiesterase inhibitors and anticancer agents

Ashraf H. Abadi, Dalal A. Abouel-Ella, Nermin S. Ahmed, Bernard D. Gary, Jose T. Thaiparambil, Heather N. Tinsley, Adam B. Keeton, Gary A. Piazza

Research output: Contribution to journalArticle

10 Scopus citations

Abstract

Two closely related series of novel β-carboline derivatives, electronically similar to tadalafil (CAS 171596-29-5), were synthesized and evaluated for their inhibitory effects upon phosphodiesterase 5 (PDE5) and phosphodiesterase 11 (PDE11) and their in vitro tumor cell growth inhibitory activity versus HT29 colorectal carcinoma cell line. Interestingly, some of the synthesized compounds showed growth inhibitory properties that appear to be associated with their ability to inhibit PDE5. Moreover, the PDE5 inhibition seems relevant to the stereochemical aspects of the compounds.

Original languageEnglish (US)
Pages (from-to)415-421
Number of pages7
JournalArzneimittel-Forschung/Drug Research
Volume59
Issue number8
DOIs
StatePublished - 2009

Keywords

  • Antitumor agents
  • CAS 171596-29-5
  • Tadalafil
  • β-Carboline derivatives, anticancer activity, phosphodiesterase 5 inhibition

ASJC Scopus subject areas

  • Drug Discovery

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