## 1 Introduction  
Cancer is a life-threatening disease; one of the major challenges for relieving its burden is to develop highly effective drugs with specificity for cancer, but few to no side effects on normal mammalian cells [1]. Gefitinib, the epidermal growth factor receptor (EGFR) inhibitor, was added recently to the Food and Drug Administration (FDA) list of the recommended first-line treatments for lung cancer [2]. Gefitinib is particularly recommended for non-small cell lung cancer (NSCLC) type [3]. Although that erlotinib and afatinib are also included in this list, gefitinib may be the most tolerable [4]. The most common adverse effects of this group of drugs were gastrointestinal diarrhea, nausea and/or vomiting which is due to the toxic effect of the drug on normal flora [5; 6]. The absence of antibacterial activity of the anticancer drug removes its detrimental effect against intestinal flora, suggesting a highly promising new strategy for the development of anticancer drugs with reduced side effects [7]. In 2008, [PERSON] and [PERSON] reported [8] that molecular weight is an important factor for antimicrobial activity. They did experiment on 147 antibacterial and 4623 non-antibacterial compounds and found average molecular weight for an antibacterial compound were 812 Da (Gram '+' positive) and 414 Da (Gram '-' negative). In addition, another important factor for becoming an antimicrobial active compound is polarity. According to the Lipinski's rule of five, also known as Pfizer's rule of five or simply the rule of five (RO5) [9], 70.4% of the antibacterial active compounds showed logP values ranges from 0-5. Therefore, in order to target a compound with no/little antimicrobial activity, lower molecular weight and with more logP values should be taken into consideration, isatin and its derivatives with low molecular weight could be a choice of interests [10; 11; 12]. Isatin, a natural compound, is known for more than a century and still being used extensively in medicinal compound synthesis [13; 14; 15; 16; 17; 18; 19]. It has been reported that, various substituents on isatin nucleus displayed numerous biological activities [12; 20]. In recent years, number of isatin derivatives were reported with extensive biological activities [21; 22; 23; 24; 25], included EGFR activity [26]. \(N\)-benzylisatin hydrazones of fluorescein had showed antiproliferative activity as well as topo II inhibitory activity [27]. Moreover, two series of hydrazone derivatives has been reported recently with antiproliferative activity [28; 29]. A number of marketed drugs and potential anticancer agents having isatin moiety, depicted in Figure 1, inspired us to synthesize a series of isatin hydrazones having \(N\)-benzyl protection at 1-position of isatin and hydrazone formation at 3-position with various aryl substituents. We thus anticipating that simplification of isatin molecule would prevent its inhibitory effect on different microbes, providing more selectivity in the action on cancerous cell lines with less/no toxicity on the gastrointestinal tract (GIT) lining cells. Considering the above points and the importance of the development of anticancer therapeutics with no/few side effects, we therefore designed and synthesized a series of \(N\)-protected \(N\)-benzylisatin-aryl hydrazones with a lower molecular weight (353-418 Da), evaluated their antibacterial activity against two Gram-positive, four Gram-negative bacterial strains and antifungal activity against _Candida albicans_ NRRL Y-477, and antiproliferative activities against non-small cell lung cancer cell lines 'A549', as well as human cervical cancer cells lines 'HeLa.' In addition, for comparing the potency of the synthesized compounds, \"gefitinib\" was used as a positive control for antiproliferative activity evaluation. In order to consider a compound as drug molecule, it is necessary to test their drug likeness properties as well as the analysis of physiological descriptors such as absorption, distribution, metabolism and excretion (ADME).