Original Research Article International Journal of Pharmaceutical Chemistry and Analysis, 3(3):143-149 143 Synthesis, characterization and evaluation of some benzothiazole derivatives bearing oxindole moiety as potential anticancer agents Kakadiya Dipesh 1,* , Malleshappa N. Noolvi 2 Dept. of Pharmaceutical Chemistry, Shree Dhanvantary Pharmacy College, Surat, Gujarat *Corresponding Author: Email: dipesh9247@gmail.com Abstract This study was aimed at investigating the antitumor activity of novel 5-substituted 2-oxindole derivatives. A series of oxindole derivatives of N-(1,3,4-thiadiazol-2-yl)benzo[d]thiazol-2-amine were prepared and confirmed by 1H NMR, mass and IR data. These compounds were evaluated for their anticancer activity at National Cancer Institute (NCI), USA by single High dose (10 -5 M) in full NCI 60 cell panel. Primary in vitro one dose anticancer assay was performed in full NCI 60 cell panel representing leukaemia, melanoma and cancers of lung, colon, brain, breast, ovary, kidney and prostate. Among them compound 1[D] has showed moderate anticancer activity while compound 3[A-2] has showed significant anticancer activity with overall mean growth percent 38.25. These findings prompt us to further explore the oxindole structure as leading scaffold to design new molecules with potent antitumor activity. Keywords: 2-Oxindole, 1,3,4-thiadiazole, Benzothiazole, Anticancer, NCI Access this article online Website: www.innovativepublication.com DOI: 10.5958/2394-2797.2016.00022.8 Introduction Cancer is a group of diseases in which cells can be aggressive (grow and divide without respect to normal limits), invasive (invade and destroy adjacent tissues) and/or metastatic (spread to other locations in body). These three malignant properties of cancer differentiate them from benign tumors, which are self-limited in their growth and do not invade or metastasize. Cancer may affect people at all ages, even fetuses, but risk for the more common varieties tends to increase with age [1] . Cancer causes about 13% of all deaths [2] . According to the American Cancer Society, 7.6 million people died from cancer in the world during 2007 [3] . Nearly all cancers are caused by abnormalities in the genetic material of the transformed cells [4] . With the current chemotherapy, lack of selectivity of chemotherapeutic agents against cancerous cells is a significant problem. Unlike normal cells, cancer cells lose the ability to control their cell cycle and continue growing unchecked. In most forms of cancer deregulation of the cell signalling pathways that are intimately involved in regulating and governing cell cycle status leads to altered response to growth stimuli. In today’s era of personalized medicine clinicians need to type cancers based on which pathways are activated and which are inactive to aid selection of the right type of modern anti-cancer drugs which specifically target and shut down overactive pathways [5] . The search for novel anticancer agents with more selectivity and lower toxicity continues to be an area of intensive investigation. The unique structural features of Oxindoles together with diverse biological activities have made them privileged structures in new drug discovery [6] . Oxindole-core synthetic molecules are currently being developed as anticancer drugs that target protein tyrosine kinases associated with growth factor receptors [7,8,9] . The search for novel anticancer agents with more selectivity and lower toxicity continues to be an area of intensive investigation. The unique structural features of Oxindoles together with diverse biological activities of 1, 3, 4-thiadiazole [10,11,12] and Benzothiazole [13,14,15] can prove the area of research quite unique. All three core nucleus has been found to have potential anticancer activity. So there is a need to combine these molecules in a single structural composition to explore its activity. In this study, 5 derivatives of oxindole with Substituted benzothiazole coupled by 1,3,4-thiadiazole were synthesized and evaluated for anticancer activity on the NCI 60 cell panel. Materials and Methods  Synthesis  Reagents All the chemicals and solvents used were of AR- grade and LR-grade and obtained from Sigma-Aldrich, Sisco Research Laboratories, Qualigens, Rankem, S.D. Fine, Hi-Media and Merck and were used without further purification.