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Research Journal of Pharmacy and Technology
Year : 2019, Volume : 12, Issue : 11
First page : ( 5427) Last page : ( 5432)
Print ISSN : 0974-3618. Online ISSN : 0974-360X.
Article DOI : 10.5958/0974-360X.2019.00941.7

Design and Synthesis of Novel Molecular Scaffolds of Bicaultamide derivatives for the treatment of Prostate Cell Cancer

Lanka Subrahmanyam1, Lakinani Vaikuntarao1, Kanaparthi Sagar Rao1, Kakani Siva Rama Rao2

1Department of Chemistry, GITAM Institute of Science, GITAM University, Visakhapatnam, India

2North East Frontier Technical University, Arunachal Pradesh

Corresponding Author E-mail: tvkpnr1985@gmail.com

Online published on 9 April, 2020.

Abstract

Prostate cancer is a major cause of male death worldwide and the identification of new efficient treatments is constantly needed. Different non-steroidal androgen receptor antagonists are approved also in the case of castration-resistant cancer forms. Using a rational approach and molecular modelling studies to modify the structure of antiandrogen drug bicalutamide, a new series of phenylsulfonyl-benzamide derivatives was designed and synthesised. Their antiproliferative activities were evaluated in four different human prostate cancer cell lines and several new compounds showed significantly improved IC50 values in the low μM range. The cytotoxicity profile was also evaluated for the novel structures in the HEK293 cell line.

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Keywords

Gemcitabine, RP-HPLC, Validation, LOD, LOQ, Robustness.

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