Synthesis and antiproliferative activity of imidazo[1,2-a]pyrimidine Mannich bases

Eur J Med Chem. 2015 Jul 15:100:18-23. doi: 10.1016/j.ejmech.2015.05.037.

Raghunath Aeluri ¹, Manjula Alla ², Sowjanya Polepalli ³, Nishant Jain ⁴

Affiliations

1 Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, 500607, India.
2 Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, 500607, India. Electronic address: manjula@iict.res.in.
3 Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, 500607, India.
4 Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, 500607, India. Electronic address: nishant@iict.res.in.

PMID: 26067381 DOI: 10.1016/j.ejmech.2015.05.037

Abstract

A series of imidazo[1,2-a]pyrimidine Mannich Bases were designed, synthesized in two phases. Mannich Bases were obtained by one pot three component condensation of imidazo[1,2-a]pyrimidine with secondary amine or piperazine and excess of formaldehyde solution in methanol. The synthesized Mannich Bases were screened for in vitro growth inhibition against a panel of 3 different human Cancer cell lines. Most of the synthesized compounds exhibited antiproliferative activity with GI50 values ranging from 0.01 to 79.4 μM. Compounds 5e, 6b and 7k were found to be effective inhibitors of growth of all cell lines, with GI50 values similar to that of standard drug. The structure and activity relationship has been disclosed.

Keywords

Antiproliferative activity; Growth inhibition; Imidazo[1,2-a]pyrimidine; Mannich reaction; Piperazine.

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