Biochemical Evaluation Of The Compounds For Cytotoxicity On Cancer Cell Lines

Chemotherapy halts the process of carcinogenesis by administration of cytotoxic compounds which attack rapidly dividing cells (both cancerous and normal), as a result, cells such as those in the digestive tract, bone marrow and hair follicles are also damaged by these drugs. At present, more than 100 different chemotherapeutic drugs are currently in use in the treatment of various types of cancer, including DNA alkylating agents, topoisomerase inhibitors, antimetabolites, and microtubule-active agents (Broxterman and Georgopapadakou, 2004). A DNA alkylating agent attaches an alkyl group to the nitrogen at position 7 of guanine residues in DNA, resulting in cross linking or abnormal base pairing and ultimately leading to apoptosis.

DNA alkylating agents can be divided into the following types: the nitrogen mustards, nitrosoureas, tetrazines, aziridines, cisplatins and derivatives, and non-classical alkylating agents. Melphalan (Alkeran^TM) (Figure 1.35) is a nitrogen mustard alkylating agent, used in the treatment of multiple myeloma, ovarian cancer and ocular retinoblastoma.