Clinically useful drugs target a relatively small number of proteins that lie within a clearly defined and chemically accessible space. However, many high value biological targets lie outside this chemical space, and an ability to access such 'intractable' targets not amenable to traditional small molecule intervention would expand treatment options and be a major boost for patients and the pha...

The Medicinal Chemistry Section is part of the Experimental Therapeutics Interdisciplinary Programme that is dedicated to early Drug Discovery activities in the oncology field. Our mission is to discover and to develop new anticancer agents based on novel hypotheses and targets generated by CNIO’s Basic Research Groups, and to do so in close collaboration with these groups. Medicinal chemists a...

8 a Department of Pharmaceutical Analysis, Xuzhou Medical College, 209 Tongshan 9 Road, Xuzhou 221004, P.R.China. 10 b Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou 11 Medical College, 209 Tongshan Road, Xuzhou 221004, P.R.China. 12 c Department of Pharmacy, Xuzhou Medical College, 209 Tongshan Road, Xuzhou 13 221004, P.R.China. 14 d Department of Medicinal Chemistry...

The number of approved drugs for the market is decreasing in recent years and calls for more effective methods to discover a higher number of successful compound candidates. Medicinal chemistry at the forefront is challenged here but also since it provides the most time-consuming step in the drug discovery process. Medicinal chemistry has made transformations through several technological innov...

Polyethylenimine (PEI), an organic branched or linear polyamine polymer, has been successfully used in the past for DNA complexation and transfection in vitro and in vivo into several cell lines and tissues. PEI was also applied in different fields from gene therapy and several studies have emphasized the importance of this polymer in medicinal chemistry. In this brief critical review the uses ...

Fluorinated compounds are synthesized in pharmaceutical research on a routine basis and many marketed compounds contain fluorine. The present review summarizes some of the most frequently employed strategies for using fluorine substituents in medicinal chemistry. Quite often, fluorine is introduced to improve the metabolic stability by blocking metabolically labile sites. However, fluorine can ...

The endocannabinoid system comprises the two well characterized Gi/o -protein coupled receptors (cannabinoid receptor 1 (CB1) and CB2), their endogenous lipid ligands, and the enzymes involved in their biosynthesis and biotransformation. Drug discovery efforts relating to the endocannabinoid system have been focused mainly on the two cannabinoid receptors and the two endocannabinoid deactivatin...