title: Recent advances on structural modifications of benzothiazoles and their conjugate systems as potential chemotherapeutics.
abstract: BACKGROUND
  Benzothiazole scaffold comprises a bicyclic ring system and is known to exhibit a wide range of biological properties including antimicrobial and anticancer activities. Benzothiazole derivatives have long been therapeutically used for the treatment of various diseases. However, in recent years, 2-arylbenzothiazoles have emerged as an important pharmacophore in the development of antitumor agents. The promising biological profile and synthetic accessibility have been attractive in the design and development of new benzothiazoles and their conjugate systems as potential chemotherapeutics.
  
  
  METHODS
  This review mainly focuses on the structural modifications of benzothiazole scaffold, development of various series of benzothiazoles and their conjugates as new antitumor agents. Furthermore, heterocyclic derivatives bearing benzothiazole moiety and their in vitro as well as in vivo screening, structure-activity relationships (SAR), mechanism, pharmacokinetics, clinical use and their future therapeutic applications are discussed here.
  
  
  CONCLUSIONS
  A large number of benzothiazole derivatives discussed here possess potent anticancer activity and can be further developed as drug candidates. Benzothiazole 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 results that have been observed for their response to tumor in clinical studies, full characterization of their toxicity is further required for their clinical usage as safe drugs for the treatment of cancer. We believe that this review gives a better understanding and scope for future drug design and development of benzothiazole-based compounds to implicate their use in cancer chemotherapy.
authors.affiliation: Indian Institute of Chemical Technology, Division of Organic Chemistry, Tarnaka, Hyderabad, India. ahmedkamal@iict.res.in
authors.forename: Kamal
authors.initials: K
authors.lastname: Ahmed
authors.forename: Srikanth
authors.initials: S
authors.lastname: Yellamelli Valli Venkata
authors.forename: Naseer Ahmed Khan
authors.initials: NA
authors.lastname: Mohammed
authors.forename: Farheen
authors.initials: F
authors.lastname: Sultana
authors.forename: Kashi Reddy
authors.initials: KR
authors.lastname: Methuku
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D052160:Benzothiazoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles