Synthesisof anti cancer drugs and folate receptor targeted delivery

Abstract

Gallinamide A, a marine cyanobacterial natural product, is an excellent inhibitor towards human cathepsin L with IC50 value of 5 nM for 30 minutes pre-incubation. Cathepsin L is a lysosomal endopeptidese which helps to degrade extracellular matrix leading to metastasize. We probably synthesized cysteinyl, isoleucinyl and alanyl derivatives of the natural product by solid phase peptide synthesis. These derivatives of natural product might have better or similar type activity like Gallinamide A.The problem of toxicity in drug delivery arises due to uptake of drugs by healthy cells. Therefore targeted drug delivery has a vital role in therapeutic applications. Folate receptor, overexpressed on certain malignant cancer cells, is a crucial biomarker for delivery of toxic drugs during chemotherapy. It has very high affinity towards folic acid and also folate conjugates. It is very important to synthesis new folate receptor inhibitors. We have synthesized two new folate receptor inhibitors such as pteroate and hydrazidepteroate linkers and these two new inhibitors may have good affinity towards folate receptor.