Name Mode of Action References
5-Aza2'-deoxycytidine Causes DNA demethylation or hemidemethylation, creating openings that allow transcription factors to bind to DNA and reactivate tumor suppressor genes. [96]
Cholecalciferol
(Vitamin D3)
Antiproliferative action on breast, prostate, and colon cancer cells [97]
4-Hydroxytamoxifen Metabolite of tamoxifen that is a potent selective estrogen response modifier (SERM); the trans (Z) isomer has efficacy against estrogen sensitive cancers. The cis (E) isomer is an estrogen agonist. [98]
Melatonin Enhances apoptotic death of cancer cells; inhibits proliferation/metastasis of breast cancer cells by inhibiting estrogen receptor action. [99]
Mifepristone         Progesterone receptor antagonist; stimulates prolactin secretion. Pgp inhibitor. [100]
Raloxifene Selective estrogen response modifier (SERM), may have efficacy against estrogensensitive cancers. [101]
Tamoxifen Selective estrogen response modifier (SERM), used therapeutically and prophylactically against estrogen sensitive    tumors. [102]
Troglitazone Antitumor agent; PPARγ agonist; induces apoptosis via a p53 pathway. [103]
Table 6: Gene regulators and their mode of action as anticancer agent.