Dendrimers are three dimensional, multifunctional polymeric structures which are composed of a core and branches emanating from these structures, resembling a tree. Here, we review the key highlights of the dendrimers for diagnostic uses as MRI contrast agents, X-ray computed tomography and particularly for cancer treatment as an effective carrier for drug delivery and in boron capture therapy. We will discuss how dendrimers represent a new class of carriers that are able to deliver drugs effectively and in a sustained manner to the target tumor sites. Dendrimers are being utilized to a variety of cancer therapies to improve the safety and effectiveness of anticancer therapeutics. This review will also investigates the benefits utilizing dendrimers for cancer diagnosis and therapy.