2. Academic Validation
  3. Synthesis of neolignans as microtubule stabilisers

Synthesis of neolignans as microtubule stabilisers

  • Bioorg Med Chem. 2014 Feb 15;22(4):1342-54. doi: 10.1016/j.bmc.2013.12.067.
B Sathish Kumar 1,  Aastha Singh 1,  Amit Kumar 2,  Jyotsna Singh 2,  Mohammad Hasanain 2,  Arjun Singh 1,  Nusrat Masood 1,  Dharmendra K Yadav 1,  Rituraj Konwar 2,  Kalyan Mitra 2,  Jayanta Sarkar 2,  Suaib Luqman 1,  Anirban Pal 1,  Feroz Khan 1,  Debabrata Chanda 1,  Arvind S Negi 3
Affiliations

Affiliations

  • 1 CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), Kukrail Picnic Spot Road, P.O. CIMAP, Lucknow 226015, India.
  • 2 CSIR-Central Drug Research Institute (CSIR-CDRI), B.S. 10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
  • 3 CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP), Kukrail Picnic Spot Road, P.O. CIMAP, Lucknow 226015, India. Electronic address: arvindcimap@rediffmail.com.
PMID: 24457094 DOI: 10.1016/j.bmc.2013.12.067
Abstract

Tubulin is a well established target for Anticancer drug development. Lignans and neolignans were synthesized as tubulin interacting agents. Neolignans 10 and 19 exhibited significant Anticancer activity against MCF-7 and MDAMB-231 human breast Cancer cell lines. Both the compounds effectively induced stabilization of microtubule at 4 and 20 μM concentrations respectively. Neolignan 10 induced G2/M phase arrest in MCF-7 cells. Docking experiments raveled that 10 and 19 occupied the same binding pocket of paclitaxel with some difference in active site Amino acids and good bioavailability of both the compounds. In in vivo acute oral toxicity 10 was well tolerated up to 300 mg/kg dose in Swiss-albino mice.

Keywords

Acute oral toxicity; Anticancer; In silico studies; Lignans; Microtubules; Neolignans.

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