1, 3, 5-triazine derivatives have received considerable attention owing to their broad biological activities, which have made it an indispensable anchor for development of new therapeutic agents. Owing to fast development of new drugs possessing 1, 3, 5-triazine nucleus, many research reports are generated in a short span of time. Although only a few compounds have at present progressed into human clinical trials, the prospect of finding safe agents useful in therapy, particularly in the cancer setting, is still positive. To our knowledge, few systematic reviews on triazines have been conducted to date. In this review, we have highlighted various inhibitors with 1, 3, 5-triazine core which targeting different kinases with an aim to help medicinal chemists for developing structure-activity relationship on 1, 3, 5-triazine derived compounds for antitumor activity.