Cancer is a serious disease with a complex pathogenesis, which threats human life greatly. Currently, great efforts have been put to the identification of novel anticancer targets and the discovery of anticancer drugs following the progress of chemogenomics, which will be reviewed briefly in this article. Furthermore, during the past 5 years, the global effort of sequencing human genome has provided us with an enormous number of potential targets associated with cancer therapy. As a result, the New Drug Discovery (NDD) is undergoing a transition "from gene to drug". Accordingly, the targets for anticancer drugs studies now are focused on some biological macromolecular targets associated with cancer and several interactive mechanisms involved in the growth and metastasis of cancer cells as well as tumorangiogenesis, such as Matrix Metalloproteinases (MMPs), Aminopeptidase N (APN), Tyrosine Kinase (TK), Farnesyltransferase (FTase) and cell Signal Transduction Pathway and so forth. Among these targets the MMP-2, -9 and APN are the most extensively studied enzymes in our laboratory. The peptidomimetics Matrix Metalloproteinase Inhibitors (MMPIs) and APN inhibitors (APNIs) with the molecular scaffold of pyrrolidine, 3-amino-2-hydroxy-4-phenyl butyric acid (AHPA) and glutamylide, which have been designed and synthesized in our laboratory, will be described in the review, among which the pyrrolidine scaffold is patented with the IC50 ranging from 1nM to 300nM against MMP-2, and MMP-9.

A series of novel L-iso-glutamine derivatives were prepared by condensing of compound 4 with various amino acid methyl esters. These compounds have not been reported in literature, and their chemical structures were confirmed by ESI-MS, IR and NMR.

The crystal structure of (4S)-5-(2-methoxy-2-oxoethylamino)-5-oxo-4-(3,4,5-trimethoxybenzamido) pentanoic acid 5 (C18H24N2O9, Mr=412.39) has been determined by single-crystal X-ray diffraction analysis. The crystal belongs to monoclinic, space group P2(1)/c with a=27.665(9), b=5.1444(16), c=13.907(4) Å, β=98.401(5)º, V=1958.0(11) Å3, Z=4, Dc=1.399 g/cm3, μ=0.113mm－1, F(000)=872, R=0.0606 and wR=0.1405 (I>2σ(I)). The results confirmed that 5 could be assigned to the tautomeric form. The intermolecular hydrogen bonds between O(5)-H(5)…O(7), N(2)-H(2)…O(6) and N(1)-H(1)…O(4) have been observed.

The title compound, C18H24N2O9, was synthesized by the condensation of N-(3,4,5-trimethoxybenzoyl) glutamic acid anhydride with l-glycine methyl ester hydrochloride in dichloromethane solution. The structure is stabilized by intermolecular hydrogen bonds.