From a biological perspective, 1,4-dihydroisoquinolinones are an interesting class of heterocyclic small molecules.  They and their isotypes, namely 3,4- and 2,4-dihydroisoquinolinones, have been shown to inhibit a wide variety of enzymatic processes.  The synthesis, however, has been documented to be long and drawn out and a more direct means to accessing this structural motif has been left to desire.  These and other skeletally diverse structures can now be accessed in a simple single pot protocol utilizing multicomponent coupling reactions in the presence of microwave irradiation.  This talk will illustrate the influence of microwaves in this single pot process and examine plausible mechanistic insights leading to substituted 1,4-dihydroisoquinolinones (1), tricyclic lactam cores (2) and spiro-quinones (3) as a diverse array of small molecules.  In addition, their biological activity will be discussed.  The inhibition of a tyrosine kinase p56 (lck) enzyme will be the focus as our research efforts are directed at understanding the process by which polysaccharides are presented on the cell surface of dendrite cells.