Enzyme inhibitory activities an insight into the structure–Activity relationship of biscoumarin derivatives

• Published in: European journal of medicinal chemistry Vol. 141; pp. 386 - 403
• Main Authors: Faisal, Muhammad, Saeed, Aamer, Shahzad, Danish, Fattah, Tanzeela Abdul, Lal, Bhajan, Channar, Pervaiz Ali, Mahar, Jamaluddin, Saeed, Shomaila, Mahesar, Parvez Ali, Larik, Fayaz Ali
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 01.12.2017
• Subjects: alpha-Amylases - antagonists & inhibitors; alpha-Amylases - metabolism; alpha-Glucosidases - metabolism; Animals; Aromatase; Aromatase - metabolism; Biscoumarin; c-Met inhibitors; Coumarins - chemistry; Coumarins - pharmacology; Enzyme inhibitor; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; HIV Integrase - metabolism; HIV-1 integrase inhibition; Humans; Proto-Oncogene Proteins c-met - antagonists & inhibitors; Proto-Oncogene Proteins c-met - metabolism; SAR; Steroid sulfatase; Steryl-Sulfatase - antagonists & inhibitors; Steryl-Sulfatase - metabolism; Urease; Urease - antagonists & inhibitors; Urease - metabolism; α-Amylase inhibitors; α-Glucosidase; α-Glucosidase; Steroid sulfatase; SAR; Biscoumarin; Aromatase; HIV-1 integrase inhibition; α-Amylase inhibitors; Enzyme inhibitor; c-Met inhibitors; Urease
• ISSN: 0223-5234; 1768-3254; 1768-3254
• DOI: 10.1016/j.ejmech.2017.10.009

Biscoumarin derivatives, a dimeric form of coumarin, are well known derivatives of coumarin, occurred in the bioactive metabolites of marine and terrestrial organisms. On account of pharmacological and biological applications, biscoumarins have long been the subject of innumerable enzyme inhibition studies. In this review the pros and cons of enzyme inhibition studies of biscoumarins as urease inhibitors, aromatase inhibitors, NPPs, α-glucosidase inhibitors, α-amylase inhibitors, HIV-1 integrase inhibition, steroid sulfatase inhibitors and c-Met inhibitors are discussed in a systematic way. Moreover, the review discusses the structure activity relationship of biscoumarin scaffold with enzyme inhibitory potency which would unleash new avenues for further development. The purpose of the current review is to disclose the value of biscoumarins as potent and efficient enzyme inhibitor. This review provides a guideline to elaborate the diversity of biscoumarin inhibitors by exploring the effects of electronic groups linked with biscoumarin nucleus. [Display omitted] •Biscoumarins are naturally active dimeric coumarins, found in marine and terrestrial organisms.•Biscoumarins inhibit urease, aromatase, NPPs, α-glucosidase, α-amylase, HIV-1 integrase, steroid sulfatase and c-Met enzymes.•The insights into structure activity relationship of biscoumarin scaffold for enzyme inhibitory potency have been discussed.