Noscapine is an opium alkaloid which has been historically used as an anti-tussive medicine. Its activity is attributed to its ability to bind stoichiometrically to tubulin, thus arresting cell division at the metaphase stage and leading to apoptosis. Its action as a safe, low toxicity drug has been confirmed and many different routes of synthesizing its naturally occurring, biologically active (-)-α isomer have been established. While noscapine has many advantages over present anti-cancer drugs - such as low toxicity, safety, high bioactivity (especially against drug-resistant strains of cancer) and oral administration - it faces the drawback of requiring a large Effective Dose (ED50) to show significant bioactivity. The analogues of noscapine show much higher activity, making these compounds more desirable as anti- cancer agents. This review explores in-depth the chemistry of noscapine and its analogues synthesized till date, including brief discussions about the bioactivity of different derivatives. In the coming years, noscapine and its analogues will present an exciting avenue for cancer therapeutics.