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

doi:10.1055/s-0031-1296417

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 journal › Article › peer-review

12 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 language	English (US)
Pages (from-to)	415-421
Number of pages	7
Journal	Arzneimittel-Forschung/Drug Research
Volume	59
Issue number	8
DOIs	https://doi.org/10.1055/s-0031-1296417
State	Published - 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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10.1055/s-0031-1296417

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title = "Synthesis of novel tadalafil analogues and their evaluation as phosphodiesterase inhibitors and anticancer agents",

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.",

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

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language = "English (US)",

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T1 - Synthesis of novel tadalafil analogues and their evaluation as phosphodiesterase inhibitors and anticancer agents

AU - Abadi, Ashraf H.

AU - Abouel-Ella, Dalal A.

AU - Ahmed, Nermin S.

AU - Gary, Bernard D.

AU - Thaiparambil, Jose T.

AU - Tinsley, Heather N.

AU - Keeton, Adam B.

AU - Piazza, Gary A.

PY - 2009

Y1 - 2009

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AB - 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.

KW - Antitumor agents

KW - CAS 171596-29-5

KW - Tadalafil

KW - β-Carboline derivatives, anticancer activity, phosphodiesterase 5 inhibition

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

Abstract

Keywords

ASJC Scopus subject areas

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