Synthesis and Anticancer Evaluations of Novel Thiazole Derivatives Derived from 4-Phenylthiazol-2-amine

Abstract

Many novel thiazole derivatives were designed and synthesized using 4-phenylthiazol-2-amine. The reactivity of the latter compound toward different chemical reagents was studied. The structure of the newly synthesized compounds was established based on elemental analysis and spectral data. Furthermore, twenty compounds of the synthesized systems were selected and evaluated in (μM) as significant anticancer agents towards three human cancer cell lines [MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and SF-268 (CNS cancer)] and normal fibroblasts human cell line (WI-38). The results showed that compounds 9 and 14a displayed higher effeciency than the reference doxorubicin.

Multi-component synthesis of pyrazolo[1,5-a]quinazoline, thiazole and thiophene derivatives as cytotoxic agents

“…In this present study, and due to the remarkable role of pyrazolo [1,5-a]quinazoline, thiazole, and thiophene as anticancer agents in many pharmaceutical drugs, and in continuation of our interest and according to our previous reports [17][18][19][20][21][22][23][24][25] a number of novel bioactive systems were synthesized. The later products that were prepared underwent multi-component reactions, followed by their estimation for six cancer cell lines compared to the standard reference Foretinib.…”

“…1 H NMR (δ, ppm): 0.95-1.05 (s, 6H, 2CH3), 2.22 (s, 2H, CH2), 3.86 (s, 3H, OCH3), 6.77 (s, 1H, =CH), 7.04-7.99 (m, 9H, C6H5, C6H4). 13 (5,5-dimethyl-3-phenyl-2-thioxo-2,3,5,6-tetrahydrobenzo[d]thiazol-7(4H)ylidene)hydrazinyl)acetonitrile (24). To a solution of compounds 18 (2.89 g, 0.01 mol) in ethanol/DMF (15/5 mL), 2-cyanoacetohydrazide 23 (0.99 g, 0.01 mol) was added.…”

Cytotoxic Activities and Morphological Sudies of Thiophene, Thiazole and Pyridazine Derivatives Synthesized from Benzo[d]thiazole Derivatives

“…Our previous work demonstrated that many of the synthesized compounds were useful in future drug designing. [23][24][25][26] In continuation of the previous work we are describing here a rapid and efficient preparation of a set of new benzo [d] thiazole derivatives starting from ortho-aminothiophenol that reacted with either ethyl cyanoacetate, diethylmalonate or ethyl acetoacetate. This new approach enables more rapid generation of a higher number of benzo [d]thiazole derivatives that were obtained using simple reactions using readily available reagents.…”

Novel 5,6,7,8-tetrahydrobenzo[b]pyran Derivatives: Synthesis and Anticancer Activity

“…The current study constitutes a further thread in green organic chemistry and one-pot multi-component reactions (MCRs); it aims to improve the synthetic procedures of various prepared compounds. [26][27][28][29][30] Herein preparations of many 5,6,7,8-tetrahydrobenzo[b]pyrans are described through multi-component reactions and via other simple methods. The obtained products were tested on three human tumor cell lines, including A-549 (lung carcinoma), HC-29 (colorectal adenocarcinoma), and MKN-45 (gastric cancer).…”