2. Academic Validation
  3. Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition

Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition

  • Eur J Med Chem. 2020 Feb 15:188:111986. doi: 10.1016/j.ejmech.2019.111986.
Amit Kumar Verma 1,  Kaneez Fatima 2,  Rajesh Kumar Dudi 3,  Misbah Tabassum 3,  Hina Iqbal 1,  Yogesh Kumar 2,  Suaib Luqman 2,  D M Mondhe 4,  Debabrata Chanda 2,  Feroz Khan 2,  Karuna Shanker 2,  Arvind S Negi 5
Affiliations

Affiliations

  • 1 CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow, 226 015, Uttar Pradesh, India.
  • 2 CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow, 226 015, Uttar Pradesh, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, Uttar Pradesh, India.
  • 3 CSIR-Indian Institute of Integrative Medicine (CSIR-IIIM), Canal Road, Jammu, 180001, India.
  • 4 Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, Uttar Pradesh, India; CSIR-Indian Institute of Integrative Medicine (CSIR-IIIM), Canal Road, Jammu, 180001, India.
  • 5 CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow, 226 015, Uttar Pradesh, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, Uttar Pradesh, India. Electronic address: arvindcimap@rediffmail.com.
PMID: 31884407 DOI: 10.1016/j.ejmech.2019.111986
Abstract

Breast Cancer is the second leading cause of deaths in women globally. Present communication deals with design and synthesis of a few diarylnaphthyls as possible anti-breast Cancer agents. Among the thirty three representatives with significant antiproliferative activity compounds 23 and 50 were quite efficacious against human breast Cancer cells. Compound 50 induced Apoptosis in both MCF-7 and MDA-MB-231 cells and exerted S phase and G2/M phase arrest respectively via distinct mechanistic pathways. It showed moderate microtubule destabilization. Further, it exhibited DNA topoisomerase-II inhibition effect in MCF-7 cells. It was well tolerable and found safe up to 300 mg/kg dose in Swiss albino mice. The dual action antiproliferative effect of compound 50 is quite interesting and warrants for future development.

Keywords

Acute oral toxicity; Apoptosis; Breast cancer; Microtubule destabilization; Molecular docking studies; Topoisomerase.

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