The book reported that the literature survey of the chemistry of thiocarbamoyl in organic synthesis. The development of one- pot reactions represents a great challenge in organic synthesis today. Indeed, this strategy allows the construction of highly active molecules from relatively simple reagents under developed reaction condition. The promising biological activity of them and their expedient synthetic strategy were investigated. Furthermore, the obtained results were discussed, 41 novel compounds were synthesized and evaluated for in vitro and in vivo antitumor, in addition to their molluscicidal activity. Also, chemical structures of the newly synthesized compounds were assigned by analytical and spectral data.