Abstract
Molecular targeted therapy is a type of cancer treatment which attempts to interfere with specific molecules involved in the growth of cancer. Several drugs have been approved for certain types of cancer, including breast cancer, colon cancer, lung cancer, gastrointestinal stromal tumour and renal cell carcinoma. Base on the clinical application of targeted molecular therapy, the outcome shown more acceptable toxicity profiles than chemotherapy. It can be understood that the molecular targeted therapy drugs target the processes, pathways, and unique physiology which are particular to cancer cells, and thus they have the ability to reduce the cancer's destructive behavior.These studies explore the receptor tyrosine kinase (RTK) inhibitor from natural and artificial synthesized compounds. Candidates screening from compound libraries which are highly effective in blocking kinase activity of RTKs in intact cells were picked out and used to evaluate their in vitro/in vivo antitumor efficiency. Both PDGFR□ and FLT3 belong to type III receptor tyrosine kinase. They have been identified to be related to some tumor formation in previous study. Aim to test the hypothesis of targeting therapy for sarcoma and acute myeloid leukemia with PDGFR and FLT3 inhibitors. The inhibition of cellular phosphorylation of PDGFR□ and FLT3 were verified in the presence exogenous growth factor. The most potent kinase inhibitor was picked out and identified as a druglike compound with good pharmaceutical properties, superior efficacy, and tolerability in a tumor xenograft model.In conclusion, the sennoside B and novel azulenes have potential in RTK inhibition for cancer therapy. The novel compounds were screening for kinase inhibition, and the lead optimization generated from SAR study. More druglike molecules were discovered in the experimental stages. We hope that further clinical studies could be developed for cancer therapy and more or better molecular targeted drugs will become available in near future.