A concise diastereoselective approach to enantioenriched substituted piperidines and their in vitro cytotoxicity evaluation

  • Bioorg Med Chem Lett. 2014 Sep 15;24(18):4439-4443. doi: 10.1016/j.bmcl.2014.08.003.
Gullapalli Kumaraswamy  1 ,  Rangaraju Satish Kumar  2 ,  Bitla Sampath  2 ,  Y Poornachandra  3 ,  C Ganesh Kumar  3 ,  Sahithya Phani Babu Vemulapalli  4 ,  Jagadeesh Bharatam  4
Affiliations
  • 1. Organic & Biomolecular Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India. Electronic address: [email protected].
  • 2. Organic & Biomolecular Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
  • 3. Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
  • 4. Center for NMR & Structural Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
PMID: 25172418 DOI: 10.1016/j.bmcl.2014.08.003
Abstract

A library of diversely stereo-oriented, highly substituted 2,6-cis piperidine derivatives were synthesized, and evaluated for their Anticancer activity in Cancer cells that included A549 (lung Cancer, CCL-185), MCF7 (breast Cancer (HTB-22), DU145 (prostate Cancer (HTB-81), and HeLa (cervical Cancer, CCL-2). One stereo-variant emerged as a promising candidate for further design based structure-activity studies.

Keywords
Anti-tumor activity; Asymmetric Mannich reaction; Cytotoxic activity; Grubbs cross-metathesis; Piperidine scaffolds.