Literature DB >> 19719240

Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.

Dario Giardinà1, Daniele Martarelli, Gianni Sagratini, Piero Angeli, Dario Ballinari, Ugo Gulini, Carlo Melchiorre, Elena Poggesi, Pierluigi Pompei.   

Abstract

Doxazosin analogues 1-3 and 1a were synthesized and investigated at alpha1-adrenoceptors and PC-3, DU-145, and LNCaP human prostate cancer cells. Compound 1 (cyclodoxazosin) was a potent alpha(1B)-adrenoceptor antagonist displaying antiproliferative activity higher than that of doxazosin in cancer cells in vitro and in vivo, respectively. Because of its antitumor efficacy at low concentrations, lower apoptotic activity in NHDF vs tumor cells, and antiangiogenetic effect, 1 showed a better therapeutic profile relative to doxazosin.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19719240     DOI： 10.1021/jm8016046

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  6 in total

Review 1.  Advances in the design and synthesis of prazosin derivatives over the last ten years.

Authors:  Andreas Desiniotis; Natasha Kyprianou
Journal:  Expert Opin Ther Targets       Date:  2011-12-13       Impact factor: 6.902

2.  Chiral analogues of (+)-cyclazosin as potent α1B-adrenoceptor selective antagonist.

Authors:  Gianni Sagratini; Michela Buccioni; Gabriella Marucci; Elena Poggesi; Matthew Skorski; Stefano Costanzi; Dario Giardinà
Journal:  Bioorg Med Chem       Date:  2018-05-17       Impact factor: 3.641

Review 3.  Therapeutic value of quinazoline-based compounds in prostate cancer.

Authors:  Johnathan Bilbro; Matthew Mart; Natasha Kyprianou
Journal:  Anticancer Res       Date:  2013-11       Impact factor: 2.480

4.  Expression of heat shock protein 27 in prostate cancer cell lines according to the extent of malignancy and doxazosin treatment.

Authors:  Seung Wook Lee; Jeong Woo Lee; Jae Hoon Chung; Jung Ki Jo
Journal:  World J Mens Health       Date:  2013-12-24       Impact factor: 5.400

5.  Efficient Synthesis of Novel 1,3,4-Oxadiazoles Bearing a 4-N,N-Dimethylaminoquinazoline Scaffold via Palladium-Catalyzed Suzuki Cross-Coupling Reactions.

Authors:  Barbara Wołek; Mateusz Werłos; Magdalena Komander; Agnieszka Kudelko
Journal:  Molecules       Date:  2020-11-05       Impact factor: 4.411

Review 6.  Age-related changes in the innervation of the prostate gland: implications for prostate cancer initiation and progression.

Authors:  Carl W White; Jin Han Xie; Sabatino Ventura
Journal:  Organogenesis       Date:  2013-05-14       Impact factor: 2.500
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.