NEW APPROACHES OF 4-ARYL-2-HYDRAZINOTHIAZOLE DERIVATIVES SYNTHESIS, MOLECULAR DOCKING, AND BIOLOGICAL EVALUATIONSAbstract
In the field of the preparation of chemotherapeutic agents with new mechanism distinct from currently approved drugs is important. However, the clinically effective approved small inhibitor molecule is still lacking. Previous reports indicated that 4-aryl-2-hydrazinothiazole derivatives provided a useful start point to develop HAT inhibitors (histone acetyltransferase). Consequently, preparation and biological evaluation of a focused library of 4-aryl-2-hydrazinothiazole based derivatives as useful as anti-cancer agents. Synthesis of 4-aryl-2-hydrazinothiazoles (1a-d), (2a-d), (3a-c), (4a-b), (5a-b), (6a-b) studied by either conventional method and free solvent microwave one-pot method, and the synthesized compounds were proved by spectroscopic methods (IR, 1HNMR, 13CNMR, GC-Ms, and elemental analysis). The activity against different cancer cell lines and the antimicrobial activities different organisms also studied, and all of the synthesized compounds were of high activity as an antibacterial for gram positive and gram negative; however, it showed also an antifungal activity were the most active compounds were 4a, 4b, 5b, 6a. It was found that all of the prepared thiazoles derivatives were active toward many cell lines (breast, liver, and prostate) where the more active compounds were 4a, 4b, and 6a. Molecular docking studies guided and proved the biological activities of these novel 4-aryl-2-hydrazinothiazoles.
M. H. Abdellattif *, M. A. Hussien and E. Alzahrani
Department of Pharmaceutical Chemistry, Deanship of Scientific Research, Taif University, 21974, KSA.
25 April, 2018
15 June, 2018
20 June, 2018
01 December, 2018