Despite incredible advancement made in recent years, treatment of cancer still remains
the most challenging task for the mankind. The new small molecule therapeutic drugs are more
specific, exhibit better therapeutic efficacy and mostly contain scaffolds of β-lactam, sulfonamide,
quinoline, quinazoline, quinoxaline, purine, pyrimidine, resorcinol, pyrazole/isoxazole,
benzamide etc. The structure-activity relationships of different pharmacophores that have been
reported to potently inhibit cell growth of human tumour cell lines are constantly being investigated.
Development of products of natural origin can also prove effective without submitting to
harmful radiation and chemotherapy treatments. Under these circumstances, the practicing organic chemists are greatly facing the challenge
of designing new and leading anti-cancer drugs based on natural products and scaffolds of potent pharmacaophores. The review intends
to cover new approach of anti-cancer drug design using natural and synthetic pharmacophores. The plausible synthetic routes to
major drugs for oncology that were approved recently by Food and Drug Administration (FDA) are also discussed.