Literature DB >> 19813465

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

Ashraf H Abadi1, Dalal A Abouel-Ella, Nermin S Ahmed, Bernard D Gary, Jose T Thaiparambil, Heather N Tinsley, Adam B Keeton, Gary A Piazza.   

Abstract

Two closely related series of novel beta-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.

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Year:  2009        PMID： 19813465      PMCID： PMC4980831          DOI： 10.1055/s-0031-1296417

Source DB:  PubMed          Journal:  Arzneimittelforschung        ISSN： 0004-4172


  12 in total

1.  Exisulind, a novel proapoptotic drug, inhibits rat urinary bladder tumorigenesis.

Authors:  G A Piazza; W J Thompson; R Pamukcu; H W Alila; C M Whitehead; L Liu; J R Fetter; W E Gresh; A J Klein-Szanto; D R Farnell; I Eto; C J Grubbs
Journal:  Cancer Res       Date:  2001-05-15       Impact factor: 12.701

Review 2.  The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.

Authors:  David T Manallack; Richard A Hughes; Philip E Thompson
Journal:  J Med Chem       Date:  2005-05-19       Impact factor: 7.446

3.  Expression of PDE11A in normal and malignant human tissues.

Authors:  Michael R D'Andrea; Yuhong Qiu; Donna Haynes-Johnson; Sheela Bhattacharjee; Patricia Kraft; Scott Lundeen
Journal:  J Histochem Cytochem       Date:  2005-07       Impact factor: 2.479

4.  Cyclic GMP mediates apoptosis induced by sulindac derivatives via activation of c-Jun NH2-terminal kinase 1.

Authors:  J W Soh; Y Mao; M G Kim; R Pamukcu; H Li; G A Piazza; W J Thompson; I B Weinstein
Journal:  Clin Cancer Res       Date:  2000-10       Impact factor: 12.531

Review 5.  The novel functions of cGMP-specific phosphodiesterase 5 and its inhibitors in carcinoma cells and pulmonary/cardiovascular vessels.

Authors:  Bing Zhu; Samuel J Strada
Journal:  Curr Top Med Chem       Date:  2007       Impact factor: 3.295

6.  High biochemical selectivity of tadalafil, sildenafil and vardenafil for human phosphodiesterase 5A1 (PDE5) over PDE11A4 suggests the absence of PDE11A4 cross-reaction in patients.

Authors:  J L Weeks; R Zoraghi; A Beasley; K R Sekhar; S H Francis; J D Corbin
Journal:  Int J Impot Res       Date:  2005 Jan-Feb       Impact factor: 2.896

Review 7.  Evaluating preference trials of oral phosphodiesterase 5 inhibitors for erectile dysfunction.

Authors:  John P Mulhall; Francesco Montorsi
Journal:  Eur Urol       Date:  2005-09-22       Impact factor: 20.096

Review 8.  beta-Catenin signaling: therapeutic strategies in oncology.

Authors:  Han Li; Rifat Pamukcu; W Joseph Thompson
Journal:  Cancer Biol Ther       Date:  2002 Nov-Dec       Impact factor: 4.742

9.  A fluorescence polarization assay for cyclic nucleotide phosphodiesterases.

Authors:  Wei Huang; Yan Zhang; J Richard Sportsman
Journal:  J Biomol Screen       Date:  2002-06

10.  Exisulind-induced apoptosis in a non-small cell lung cancer orthotopic lung tumor model augments docetaxel treatment and contributes to increased survival.

Authors:  Clark M Whitehead; Keith A Earle; John Fetter; Songmei Xu; Theresa Hartman; Daniel C Chan; Tom L M Zhao; Gary Piazza; Andres J P Klein-Szanto; Rifat Pamukcu; Hector Alila; Paul A Bunn; W Joseph Thompson
Journal:  Mol Cancer Ther       Date:  2003-05       Impact factor: 6.261
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  4 in total

1.  Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.

Authors:  Heba A Mohamed; Nancy M R Girgis; Rainer Wilcken; Matthias R Bauer; Heather N Tinsley; Bernard D Gary; Gary A Piazza; Frank M Boeckler; Ashraf H Abadi
Journal:  J Med Chem       Date:  2010-12-28       Impact factor: 7.446

2.  Novel Therapeutics: NSAIDs, Derivatives, and Phosphodiesterases.

Authors:  Heather N Tinsley; Gary A Piazza
Journal:  Curr Colorectal Cancer Rep       Date:  2012-12

3.  Sildenafil potentiates the antitumor activity of cisplatin by induction of apoptosis and inhibition of proliferation and angiogenesis.

Authors:  Mona Mohamed El-Naa; Mohamed Othman; Sheren Younes
Journal:  Drug Des Devel Ther       Date:  2016-11-16       Impact factor: 4.162

4.  Potential synergistic effect of phosphodiesterase inhibitors with chemotherapy in lung cancer.

Authors:  Kalliopi Domvri; Konstantinos Zarogoulidis; Nikolaos Zogas; Paul Zarogoulidis; Savvas Petanidis; Konstantinos Porpodis; Efrosini Kioseoglou; Wolfgang Hohenforst-Schmidt
Journal:  J Cancer       Date:  2017-10-09       Impact factor: 4.207
  4 in total

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