Please use this identifier to cite or link to this item: http://scholarbank.nus.edu.sg/handle/10635/23224
Title: Combinatorial synthesis of some biologically active heterocycles
Authors: MAKAM SHANTHA KUMAR RAGHAVENDRA
Keywords: solid-phase, combinatorial, heterocycles, pyrazolo[3,4-d]pyrimidines, triazoles, oxazinones
Issue Date: 23-Jun-2007
Source: MAKAM SHANTHA KUMAR RAGHAVENDRA (2007-06-23). Combinatorial synthesis of some biologically active heterocycles. ScholarBank@NUS Repository.
Abstract: Small heterocyclic compounds are known to possess a wide range of biological activities and many of them are in use as drugs with clinically proven activities. Over the last 10 years, the usefulness of heterocycles as scaffolds for library generation has been very well demonstrated. With a huge therapeutic value in store, heterocycles seems to generate potential candidates for medicinal chemistry and developing solid-phase synthetic protocols for the combinatorial synthesis of heterocycles would be a useful and exciting area of research. In the current research work, we have examined and developed solid-phase synthetic protocols for the synthesis of some biologically active heterocycles. Some of the compounds prepared have been evaluated for their multidrug resistance protein (MRP4/ABCC4) inhibitory activity and two compounds were found to be active in inhibiting MRP4 mediated efflux of the bimane-glutathione conjugate. In addition, both compounds at 25 i?-M were also able to reverse MRP4 mediated resistance to the anticancer drug 6-thioguanine.
URI: http://scholarbank.nus.edu.sg/handle/10635/23224
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