Synthesis and SAR studies of marine natural products ma'edamines A, B and their analogues

Sanjay Saha; Ch Venkata Ramana Reddy; Shili Xu; Saranya Sankar; Nouri Neamati; Balaram Patro

doi:10.1016/j.bmcl.2013.07.017

Synthesis and SAR studies of marine natural products ma'edamines A, B and their analogues

Bioorg Med Chem Lett. 2013 Sep 15;23(18):5135-9. doi: 10.1016/j.bmcl.2013.07.017. Epub 2013 Jul 19.

Authors

Sanjay Saha¹, Ch Venkata Ramana Reddy, Shili Xu, Saranya Sankar, Nouri Neamati, Balaram Patro

Affiliation

¹ GVK Biosciences Private Limited, Medicinal Chemistry Division, 28A, IDA, Nacharam, Hyderabad 500076, India.

PMID: 23927972
DOI: 10.1016/j.bmcl.2013.07.017

Abstract

The synthesis of several analogues of ma'edamines A and B are reported. The synthesized compounds were tested on hormone receptor positive and HER2 positive breast cancer cell lines, by MTT assay. MED-114, 115, 117, 119, 120, 124, 128 and 131 were found to be equally active as Lapatinib on HER2 +ve cell line SKBR3.

Keywords: Anticancer; Antiproliferative activity; Breast cancer; HER2; Marine natural products.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Biological Products / chemical synthesis
Biological Products / chemistry
Biological Products / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Pyrazines / chemical synthesis
Pyrazines / chemistry
Pyrazines / pharmacology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Biological Products
Pyrazines
ma'edamine A
ma'edamine B