A review on pharmacophoric designs of antiproliferative agents

• Published in: Medicinal chemistry research Vol. 24; no. 3; pp. 903 - 920
• Main Authors: Rana, Anil, Alex, Jimi Marin, Chauhan, Monika, Joshi, Gaurav, Kumar, Raj
• Format: Journal Article
• Language: English
• Published: Boston Springer US 01.03.2015
• Subjects: Biochemistry; Biomedical and Life Sciences; Biomedicine; Cell Biology; Pharmacology/Toxicology; Review Article; Pharmacophores; Multi inhibitors; Anti-proliferative agents; Dual inhibitors; Cancer
• ISSN: 1054-2523; 1554-8120
• DOI: 10.1007/s00044-014-1196-5

Past few decades have witnessed the dawn of new diseases in which cancer is a major problem and the race ensued to eradicate cancer by charting out various effective therapeutic regimens. Circumventing resistance issues and combating the toxicity and selectivity problems are matter-of-concern in cancer treatment. Persistent failure to ensure complete remission and eradication of cancer instigated the researchers to exploit the strategies of combining pharmacophores as targeted therapeutic agents. Momentous improvement in the pharmacokinetic as well as pharmacodynamic profile resulting in the enhancement of bioavailability was seen with the introduction of these pharmacophores. The scope of molecular hybridization can be clearly exemplified through the US-FDA approved estramustine and others such as CUDC-101, CBLC-137, PLX3397, E-3810, and CUDC-907 that are currently in different phases of clinical trials. This review seeks to highlight and discuss anti-proliferative activity of some important hybrid, dual, and multi-targeted pharmacophores reported to date along with their designs, structure activity relationships, scope, and limitations. Further, an emphasis has been made to summarize US-FDA approved as well as drugs currently undergoing clinical trials of anticancer drug development.