Wednesday , 20 September 2017

Anticancer activity of Piperazine Propyl-4-Oxo-3,4-Dihydroquinazoline-2-Carboxylate Derivatives

A. Gopi Reddy1, V. Harinadha Babu1*, Y. Jaya Prakash Rao2
1Department of Pharmaceutical Chemistry, G. Pulla Reddy College of Pharmacy, Hyderabad.
2Department of Chemistry, Telangana University, Nizamabad, Telangana

In this study, The synthesized piperazine propyl-4-oxo-3,4-dihydroquinazoline-2-carboxylate derivatives were screened for their in vitro anti proliferative activity in these four different human cancer cell lines He La (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR 32 (neuroblastoma) by the standard SRB assay method. Among all the compounds only two compounds 8e and 8g showed potent anti proliferative activity with GI50 values of 0.02, less than 0.01 μM against MIAPACA human cancer cell line and some compounds showed significant activity within the range of 0.1-0.87 μM against human cancer cell lines. Potencies of all the compounds were comparable to the standard drugs Doxorubicin and Paclitaxel. The structure-activity relationship (SAR) study revealed that not only the electron accepting substituents on the quinazolinone moiety but also the quinazolinone with a propyl linker is required for inducing anti-proliferative activity against the MIAPACA as well as remaining human cancer cell line. The substituent at ring-B on quinazolinone moiety with propyl linker of ortho-fluoropiperazine (8e) and para-fluoropiperazine (8g) were associated with a potent increase in the growth inhibitory effect against MIAPACA.
Keywords: Cell lines, anticancer activity, quinazoline moiety

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