Design and Synthesis of Novel Piperazine (2-Chloroethyl)-1-nitrosourea Analogues as Anticancer Agents

Sudharshanacharyulu Sowmithri1,*,, J.V. Shanmukha Kumar1,*,, Palla Mahesh2, and T. Krishnamohan1,

1Department of Chemistry, Koneru Lakshmaiah Education Foundation (KLEF), Green Fields,Vaddeswaram, Guntur-522502, India

2Therapiva Pvt Ltd, IDA Pashamylaram, Hyderabad-502307, India

*Corresponding author: E-mail:


A series of piperazine (2-chloroethyl)-1-nitrosourea analogues (6a-h) have been designed, synthesized, characterized and screened for anticancer activity against five human cancer cell lines viz. human colorectal cancer (HCT-116 and HCT-15), human colon cancer (Colo-205), human breast cancer (MCF-7) and leukaemia (Molt-4). Among the screened compounds, compound 6f exhibits potent activity against HCT-116 cell line with an IC50 of 1.0 μM, which regarded as promising drug candidate for the development of anticancer agents.


Anticancer agents, Human breast cancer, Human colon cancer, Leukaemia, Piperazine, (2-Chloroethyl)-1-nitrosourea.

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