4.5 Article

Targeting tyrosine kinase: Development of acridone - pyrrole - oxindole hybrids against human breast cancer

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 1, Pages 32-35

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.11.021

Keywords

Pyrrole; Oxindole; Acridone; Molecular modeling; Tyrosine kinase; Anticancer

Funding

  1. Science and Engineering Research Board - Department of Science and Technology, New Delhi
  2. UGC, New Delhi
  3. University Grants Commission, New Delhi

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Based on the molecular modelling studies, a rational modification of the lead molecule was made to develop highly potent compounds showing anti-cancer activity against human breast cancer cell lines MCF 7, MDA-MB-468 and T-47D. The most potent compounds have Log P and total polar surface area 4.4-5.4 and 59.8 angstrom, respectively and they also exhibited promising ADME profile.

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