Mini Reviews in Medicinal Chemistry - Volume 2, Issue 6, 2002

Since tubulin is a known anticancer and anthelmintic drug target, the investigation of protozoal tubulin could lead to the development of new antiparasitic drugs. This review outlines the current state of knowledge concerning drug-mammalian tubulin interactions, the effects of antimicrotubule agents on parasites and parasite tubulin, and our current hypotheses regarding the development of selective ligands for Read More

αVβ3 integrin, a cell surface protein, has been targeted by a variety of natural and synthetic antagonists in the search for potential cancer and osteoporosis drug candidates. This review discusses chemical and structural requirements for activity and selectivity deduced from SAR studies and draws a tentative picture of the pharmacophore.

The full-scale commercial appearance of antibiotics in the 1950's caused a shift of the nature of our lethal diseases from infectious / acute to non-infectious / chronic. In this situation, biological response modifiers (BRM's), which are not based on selective toxicity, are expected to be useful. There exist several types of BRM's, including retinoids which act directly on cells at the gene expression level, and thalidomide (and relat Read More

Polyamines are essential cell constituents for all organisms. The present review highlights important differences in the synthesis, degradation, and interconversion of polyamines between the protozoan parasites (Trypanosoma brucei, Trypanosoma cruzi, Cryptosporidium parvum and Trichomonas vaginalis) and their mammalian hosts. Approaches include development of mono- and di-substituted polyamine analogs tar Read More

Morphiceptin (Tyr-Pro-Phe-Pro-NH2) is one of the most selective agonists for the μ-opioid receptor. In this review structure-activity relationships of morphiceptin analogues and studies resulting in defining low energy conformations are discussed. Finally, new developments in the control of tumour growth and cell proliferation by morphiceptin analogues are surveyed, which open future perspectives in the diagnosis and treat Read More

Chemical insights into artemisinin's biological mechanism of action have allowed rational design of some new trioxane and endoperoxide antimalarial drug candidates that are efficacious and safe. This review summarizes recent achievements in this area of peroxide drug development for malaria chemotherapy.

NO is produced endogenously from L-arginine by NOSs. Among its multiple activities, the homeostatic control of the vascular endothelium is crucial for atherosclerosis, a pathogenic condition connected with elevated levels of LDL, the main plasma cholesterol carrier. Oxidised LDL is proatheromatic, and toxic peroxidation products contribute to further endothelial damage. .NO controls vascular tone, inhibits LDL oxida Read More

Chemoprotection has established itself as a “major arm” in the “war against cancer” and induction of phase 2 detoxification enzymes as an effective strategy. Prominent among inducers are Michael reaction acceptors. Such functionalities are intrinsic to many phenylpropanoids present in edible plants, where they play roles in plant defense. This minireview focuses on the ability of such plant metabolites to elevate phase Read More

The present review concentrates on camptothecin (CPT) analogues, the most extensively studied topoisomerase I (topo I) inhibitors, and provides concise information on the structural features of human topo I enzyme, mechanisms of interaction of CPT with topo I, structure-activity relationship study of CPT analogues including the influence of lactone stability on antitumor activity, and recent updates of valuable CPT analogues.