Hot Topics in Medicinal Chemistry (Track)



SINGLE BUILDING BLOCK ARCHITECTURE: TOWARD THE DESIGN AND DISCOVERY OF NOVEL AND TISSUE SELECTIVE ANTICANCER DRUG LEAD

Taleb H. Al-Tel and Stephen L. Craig

College of Pharmacy, University of Sharjah, P.O.Box 27272, Sharjah, UAE

Abstract:

Despite the availability of improved drugs, including targeted cancer therapies, cancer is still one of the leading causes of mortality worldwide. In this regard, extensive synthesis and design of new structural motifs to improve antitumor activity and selectivity are highly desirable [1]. In this context, diversity- oriented synthesis to generate a plethora of novel scaffolds, is a powerful and highly productive tool for lead development and analog design. To minimize the gap between chemical and biological spaces, a single building block protocol was designed to synthesize diverse molecular scaffolds with rich stereochemical complexity. In this meeting, the synthesis, design and qualitative SAR analysis of novel motifs, such as the complex molecular scaffolds exemplified in Scheme 1, and assessing their potential as selective anticancer agents, will be presented.


Scheme 1

REFERENCE

[1]        Al-Tel, T. H. et al.; Eur. J. Org. Chem., (2010), DOI: 10.1002/ejoc.201000808; Al-Tel, T. H. et al. Eur. J. Med. Chem., 2010, 45, 4615-4621; Al-Tel, T. H. et al. Org. Biomol. Chem., (2010), DOI:10.1039/c0ob00289e.