Document Detail

The design and development of imidazothiazole-chalcone derivatives as potential anticancer drugs.
MedLine Citation:
PMID:  23317445     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: Imidazothiazole derivatives have long been therapeutically used for the treatment of various diseases. In recent years, the imidazothiazole and chalcone moieties have emerged as important pharmacophores in the development of antitumor agents. Imidazothiazole-chalcone conjugates can be accessed by covalently binding these two powerful pharamacophore units. These conjugates are known to exhibit a wide range of biological properties, including anticancer, antimicrobial, anti-inflammatory and immunosuppressive activities. Their promising biological profile and easy synthetic accessibility have triggered investigations directed at the design and development of new imidazothiazole-chalcone conjugate derivatives as potential chemotherapeutics.
AREAS COVERED: The present review focuses on recent reports of the syntheses and anticancer properties of various imidazothiazoles, chalcones and imidazothiazole-linked chalcone conjugates. Furthermore, the authors discuss the structure-activity relationships (SAR) of imidazothiazoles and chalcones and their conjugates as new antitumor agents, as well as in vitro and in vivo evaluation, clinical use and their future therapeutic applications.
EXPERT OPINION: A large number of imidazothiazoles, chalcones and a new series of imidazothiazole-chalcone conjugates possess potent anticancer activity that could be further developed as drug candidates. Imidazothiazole-based conjugates could also display synergistic effect, and still there is a need to use the drug combinations permitting lower dose and development of new generation of drugs. Despite encouraging observed results for their response to tumors in clinical studies, full characterization of their toxicity is further required for their clinical usage as safe drugs for the treatment of cancer.
Ahmed Kamal; Methuku Kashi Reddy; Arutla Viswanath
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Publication Detail:
Type:  Journal Article; Review     Date:  2013-01-15
Journal Detail:
Title:  Expert opinion on drug discovery     Volume:  8     ISSN:  1746-045X     ISO Abbreviation:  Expert Opin Drug Discov     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-22     Completed Date:  2013-08-06     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  101295755     Medline TA:  Expert Opin Drug Discov     Country:  England    
Other Details:
Languages:  eng     Pagination:  289-304     Citation Subset:  IM    
CSIR - Indian Institute of Chemical Technology, Division of Organic Chemistry, Tarnaka, Hyderabad, India.
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MeSH Terms
Antineoplastic Agents / pharmacology*
Chalcone / analogs & derivatives*,  pharmacology*
Drug Design
Imidazoles / pharmacology*
Thiazoles / pharmacology*
Reg. No./Substance:
0/Antineoplastic Agents; 0/Imidazoles; 0/Thiazoles; 94-41-7/Chalcone

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