Department Of Pharmaceutical Sciences and Natural Products

Permanent URI for this communityhttps://kr.cup.edu.in/handle/32116/52

Browse

Author: search.filters.author.Garg, Mansi

Search Results

Now showing 1 - 2 of 2
  • Thumbnail Image
    Item
    Pyrazoloquinazolines: Synthetic strategies and bioactivities
    (2015) Garg, Mansi; Chauhan, Monika; Singh, Pankaj Kumar; Singh, Pankaj Kumar; Alex, Jimi Marin; Kumar, Raj
    Numerous N-heterocycles are indisputably evidenced to exhibit myriad biological activities. In the recent past, attempts made to condense the various heterocycles have resulted in derivatives possessing better bioactivities. Among many such condensed heterocycles, pyrazoloquinazolines have managed to hold the attention of many researchers, owing to the broad spectrum of activities they portray. This review is the first of its kind to congregate the various pyrazoloquinazolines reported until now and categorizes these structurally isomeric classes into eleven different groups based on the fusion pattern of the ring such as [1,5-c], [5,1-b], [4,3-h], etc. Furthermore, this review is a concerted effort to highlight design, synthetic strategies as well as biological activities of each class of this condensed heterocycle. Structure-activity relationship studies and in silico approaches wherever reported have also been discussed. In addition, manuscript also offers scope for design, synthesis and generation of libraries of unreported classes of pyrazoloquinazolines for the biological evaluation. Copyright ? 2014 Elsevier Masson SAS. All rights reserved.
  • Thumbnail Image
    Item
    Identification of new insulin growth factor receptor-1 (IGF-1R) inhibitors via exploring ATPas kinase domain of IGF-1R through virtual screening
    (Birkhauser Boston, 2017) Garg, Mansi; Chauhan, Monika; Kumar, Raj
    Insulin growth factor receptor-1 is a trans-membrane tyrosine kinase receptor that mediates the polypeptide protein hormone insulin growth factor-1, responsible for normal function and growth of human cells. The overexpression of insulin growth factor receptor-1 has been associated with a variety of cancers. A number of small molecule inhibitors of insulin growth factor receptor-1 are discovered by various researchers but all of them get failed in preclinical trials due to less potency and resistance. In the present paper, we have identified new insulin growth factor receptor-1 inhibitors through virtual screening based on ATPase kinase domain having phosphate, sugar and hydrophobic regions lined with amino acid residues such as Asp 1150, Lys 1003, Phe 1124 and Lys 1033. A total of 7659 compounds were selected from PubChem database. Then on applying, the rule of five, 4482 compounds were enlisted and downloaded. Further on performing high throughput virtual screening, standard precision and extra precision three best scoring compounds were identified, which could be taken further for drug development. ? 2016, Springer Science+Business Media New York.