publication . Doctoral thesis . 2011

Design, synthesis and development of novel indolocarbazole derivatives as potential anti-cancer agents

Pierce, Laurence Thomas;
Open Access English
  • Published: 01 Apr 2011
  • Publisher: University College Cork
  • Country: Ireland
This thesis describes work carried out on the design of new routes to a range of bisindolylmaleimide and indolo[2,3-a]carbazole analogs, and investigation of their potential as successful anti-cancer agents. Following initial investigation of classical routes to indolo[2,3-a]pyrrolo[3,4-c]carbazole aglycons, a new strategy employing base-mediated condensation of thiourea and guanidine with a bisindolyl β-ketoester intermediate afforded novel 5,6-bisindolylpyrimidin-4(3H)-ones in moderate yields. Chemical diversity within this H-bonding scaffold was then studied by substitution with a panel of biologically relevant electrophiles, and by reductive desulfurisation....
free text keywords: Indolocarbazole, Indole, Carbazole, Cancer, Kinase, Indole--Synthesis, Indole--Therapeutic use, Cancer--Chemotherapy
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