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Deciphering the key heterocyclic scaffolds in targeting microtubules, kinases and carbonic anhydrases for cancer drug development

  1. Author:
    Peerzada, Mudasir Nabi
    Hamel,Ernest
    Bai,Ruoli
    Supuran, Claudiu T.
    Azam, Amir
  2. Author Address

    Jamia Millia Islamia, Dept Chem, Med Chem Res Lab, New Delhi 110025, India.Natl Inst Hlth, Mol Pharmacol Branch, Dev Therapeut Program,Natl Canc Inst, Div Canc Treatment & Diag,Frederick Natl Lab Canc, Frederick, MD 21702 USA.Univ Florence, Sect Pharmaceut & Nutraceut Sci, Dept NEUROFARBA, Polo Sci, Via U Schiff 6, I-50019 Florence, Italy.
    1. Year: 2021
    2. Date: Sep
    3. Epub Date: 2021 04 22
  1. Journal: Pharmacology & therapeutics
  2. PERGAMON-ELSEVIER SCIENCE LTD,
    1. 225
  3. Type of Article: Review
  4. Article Number: 107860
  5. ISSN: 0163-7258
  1. Abstract:

    Heterocyclic scaffolds are widely utilized for drug design by taking into account the molecular structure of ther-apeutic targets that are related to a broad spectrum of ailments, including tumors. Such compounds display var-ious covalent and non-covalent interactions with the specific residues of the target proteins while causing their inhibition. There is a substantial number of heterocyclic compounds approved for cancer treatment, and these compounds function by interacting with different therapeutic targets involved in tumorogenesis. In this review, we trace and emphasize the privileged heterocyclic pharmacophores that have immense potency against several essential chemotherapeutic tumor targets: microtubules, kinases and carbonic anhydrases. Potent compounds currently undergoing pre-clinical and clinical studies have also been assessed for ascertaining the effective class of chemical scaffolds that have significant therapeutic potential against multiple malignancies. In addition, we also describe briefly the role of heterocyclic compounds in various chemotherapy regimens. The optimized molecular hybridization of delineated motifs may result in the discovery of more active anticancer therapeutics and circumvent the development of resistance by specific targets in the future. (c) 2021 Elsevier Inc. All rights reserved.

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External Sources

  1. DOI: 10.1016/j.pharmthera.2021.107860
  2. PMID: 33895188
  3. WOS: 000669506100003

Library Notes

  1. Fiscal Year: FY2020-2021
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