Before the biomedical community had had any understanding of the molecular mechanisms that drive tumorigenesis, the discovery of cancer chemotherapy exclusively focused on the development of novel cytotoxic compounds targeting DNA processing and cell division including DNA alkylating and cross-linking agents, antimetabolites, topoisomerase inhibitors, and anti-tubulin agents. Although these drugs can be very efficacious in killing tumor cells, serious side effects accompanied due to the lack of selectivity for tumor cells versus normal cells. The side effects, such as bone marrow suppression and gastrointestinal, cardiac, hepatic, and renal toxicities, significantly limit their use. In addition, drug resistance was frequently observed after initial stabilization or regression of the disease.

Original languageEnglish
Title of host publicationThe Molecular Basis of Human Cancer
PublisherSpringer New York
Number of pages25
ISBN (Electronic)9781597454582
ISBN (Print)9781934115183
StatePublished - 1 Jan 2016


  • BCR-ABL inhibitors
  • DNMT inhibitors
  • EGFR inhibitors
  • HDAC inhibitors
  • HSP90 inhibitors
  • MEK inhibitors
  • Multitargeted tyrosine kinase inhibitors
  • PARP inhibitors
  • Small molecule protein kinase inhibitors
  • Targeted cancer therapeutics
  • VEGFR inhibitors


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