Synthesis of Novel Methotrexate Derivatives for Enhanced Anticancer Activity

Abstract

Cancer has become a burning issue due to its deadly effects worldwide. Chemist is trying to synthesize drugs with less cytotoxicity, minimum side effects and better efficacy. Methotrexate is a drug having strong anticancer activity, but with serious side effects. Several derivatives have been synthesized by modification at different sites of methotrexate to reduce its side effects and enhance efficacy. Schiff bases achieved a special place due to their biological activities like antitumor activity, antifungal activity, anti-malarial, antivirus, antibacterial and many others. Nine Schiff bases have been synthesized by the reaction of methotrexate with different aldehydes. These schiff base derivatives tested for anticancer activity on gliomas cell lines and compared with the parent drug. Methotrexate derivatives with 2- Chlorobenzaldehyde, 2-Thiocarboxyaldehyde, and 2- pentenal show better results on 100 μM even on lower concentration than Methotrexate, which shows the same result at higher concentration 400 μM. Characterization techniques used are IR, HNMR and CNMR.