Abstract
A series of 1-acyl-4-sulfonylpiperazine derivatives has been prepared. The antiproliferative effect of these compounds was evaluated in vitro against human prostate cancer cell line C4-2, several among them exhibited interesting growth inhibitory against this particular cell line. Finally, a molecular modeling study was employed to analyze the structure/activity relationships (SAR) of these novel compounds..
Highlights
Prostate cancer (PC) is the second most commonly diagnosed cancer in men in western world and is the leading cause of cancer death in elderly [1,2]
Progression of prostate cancer to androgen independence is the primary barricade in improving patient survival due to complex mechanisms underlying the evolution to androgen independence, and at present, there is no curative treatment for hormone refractory prostate cancer (HRPC) and bone metastatic disease [4,5,6,7,8,9]
In our Laboratory, we have shown that 6-[4-(2-Bromo-5-methoxybenzoyl)-piperazin-1-yl]-N-phenylpropyl nicotinamide (Compound A, Figure 1) induces growth arrest of prostate cancer cell lines in vitro and inhibits LnCap and C4-2 tumour growth in vivo [12]
Summary
Prostate cancer (PC) is the second most commonly diagnosed cancer in men in western world and is the leading cause of cancer death in elderly [1,2]. It is considered a major research and public health priority [3]. Progression of prostate cancer to androgen independence is the primary barricade in improving patient survival due to complex mechanisms underlying the evolution to androgen independence, and at present, there is no curative treatment for HRPC and bone metastatic disease [4,5,6,7,8,9]. Development of new drugs with high action against the prostate cancer and with low adverse effects is the most urgent demand to treat cancer [10,11]
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