A series of 1-substituted-1H-tetrazole-5-thiol building blocks were synthesized and introduced to the N-4 piperazinyl group at C-7 position of the quinolone core, and these novel compounds (5a-g and 8a-g) were screened for their antibacterial and antiproliferative activities. Bioactive assay studies manifested that most of new compounds exhibited significant antibacterial activity against the tested strains, including multi-drug-resistant MRSA in comparison with reference drugs ciprofloxacin, streptomycin B and pipemidic acid. Among the synthesized compounds, only ciprofloxacin (5a-g) derivatives displayed significant activity ([Formula: see text]) compared to reference drugs. In addition, these compounds were evaluated for their in vitro inhibition of human cancer cell lines viz human cervical carcinoma cell line (SiHA), breast adenocarcinoma (MDA-MB-235) and human pancreas carcinoma (PANC-1) cell lines by using the SRB assay method. Most of the target compounds showed broad potent growth inhibition activity ([Formula: see text]) against all the tested cancer cell lines compared with reference drug. The most promising active compounds in this series were 5c, 5d, 8c, 8d and 8f endowed with excellent antiproliferative activity. A new class of compounds was designed rationally by introducing tetrazole building block on N-4 piperazinyl group at C-7 position of quinolones core. The titled compounds were evaluated for their preliminary antibacterial and antiproliferative activities.

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Cancer is a major cause of death around the world from decades. The WHO estimated 12 million deaths by cancer with current therapeutics by 2030. Among all the characterized cancers, only lung, stomach, liver, colon, and breast cancers are main cause of cancer mortality worldwide [1] . There probable causes for the difficulty in the control and treatment cancer could be the genetic instability and poor prognosis of cancer [2] . Among all types of cancer treatment, chemotherapy is an important option. Cancer cells become simultaneously resistant to different structural types of chemotherapeutic agents due to the multidrug resistance. Hence, the development of efficient, selective and less toxic anticancer agents are necessary to overcome the multidrug resistance of cancer cells [3] .The tetrazoles are five-membered ring 6π-heterocycles, containing four contiguous nitrogen atoms and these are not found in nature, but there is scarce data available on their biological activity [4] . Further, 5-sulfenyl tetrazoles are congeners of tetrazoles that can be found as a distinguished scaffold in active pharmaceutical