Hybrid Pharmacophore Design and Synthesis of Naphthalimide– Benzimidazole Conjugates as Potential Anticancer Agents

Title:Hybrid Pharmacophore Design and Synthesis of Naphthalimide– Benzimidazole Conjugates as Potential Anticancer Agents

Volume: 12 Issue: 5

Author(s): Ahmed Kamal, Pogula Praveen Kumar, Mohammed Naseer Ahmed Khan, Bobburi Naga Sheshadri and Naga Sheshadri

Affiliation:

Keywords: Benzimidazole, conjugates, cytotoxicity, naphthalimide, piperazine.

Abstract: Naphthalimide-benzimidazole conjugates were prepared using two different types of spacer units; either a simple alkane chain or a substituted piperazine moiety with variable alkyl side chains. Each set of conjugates was evaluated for their in vitro anticancer activity, and compounds 14a, 14b and 20c were found to exhibit significant activity against a number of cancer cell lines. In particular, compound 14a showed remarkable anticancer activity with GI₅₀ values of 0.02 μM and 0.49 μM against central nervous system (SNB-75) and leukemia (K-562) cell lines, respectively. Compound 14b showed noticeable activity against melanoma (MAME-3M) cell line with GI₅₀ value 0.09 μM. Compound 20c also displayed selectivity against leukemia cell lines with GI₅₀ values up to 0.21 μM as well as appreciable broad-spectrum cytotoxicity.

Cite this article as:

Kamal Ahmed, Praveen Kumar Pogula, Naseer Ahmed Khan Mohammed, Naga Sheshadri Bobburi and Sheshadri Naga, Hybrid Pharmacophore Design and Synthesis of Naphthalimide– Benzimidazole Conjugates as Potential Anticancer Agents, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180811666140915221955