Acetic Acid Mediated for One-Pot Synthesis of Novel Pyrazolyl s-Triazine Derivatives for the Targeted Therapy of Triple-Negative Breast Tumor Cells (MDA-MB-231) via EGFR/PI3K/AKT/mTOR Signaling Cascades
Here, we described the synthesis of novel pyrazole-s-triazine derivatives via an easy one-pot procedure for the reaction of β-dicarbonyl compounds (ethylacetoacetate, 5,5-dimethyl-1,3-cyclohexadione or 1,3-cyclohexadionone) with N,N-dimethylformamide dimethylacetal, followed by addition of 2-hydrazinyl-4,6-disubstituted-s-triazine either in ethanol-acetic acid or neat acetic acid to afford a novel pyrazole and pyrazole-fused cycloalkanone systems. The synthetic protocol proved to be efficient, with a shorter reaction time and high chemical yield with broad substrates. The new pyrazolyl-s-triazine derivatives were tested against the following cell lines: MCF-7 (breast cancer); MDA-MB-231 (tr…
Synthesis and Antiproliferative Activity of a New Series of Mono- and Bis(dimethylpyrazolyl)-s-triazine Derivatives Targeting EGFR/PI3K/AKT/mTOR Signaling Cascades
Here, we synthesized a newseries of mono- and bis(dimethylpyrazolyl)-s-triazine derivatives. The synthetic methodology involved the reaction of different mono- and dihydrazinyl-s-triazine derivatives with acetylacetone in the presence of triethylamine to produce the corresponding target products in high yield and purity. The antiproliferative activity of the novel mono- and bis(dimethylpyrazolyl)-s-triazine derivatives was studied against three cancer cell lines, namely, MCF-7, HCT-116, and HepG2. N-(4-Bromophenyl)-4-(3,5-dimethyl-1H-pyrazol-1-yl)-6-morpholino-1,3,5-triazin-2-amine 4f, N-(4-chlorophenyl)-4,6-bis(3,5-dimethyl-1H-pyrazol-1-yl)-1,3,5-triazin-2-amine 5c, and 4,6-bis(3,5-dimethy…
CCDC 2177427: Experimental Crystal Structure Determination
Related Article: Ihab Shawish, Assem Barakat, Ali Aldalbahi, Walhan Alshaer, Fadwa Daoud, Dana A. Alqudah, Mazhar Al Zoubi, Ma’mon M. Hatmal, Mohamed S. Nafie, Matti Haukka, Anamika Sharma, Beatriz G. de la Torre, Fernando Albericio, Ayman El-Faham|2022|Pharmaceutics|14|1558|doi:10.3390/pharmaceutics14081558
CCDC 2163940: Experimental Crystal Structure Determination
Related Article: Ihab Shawish, Assem Barakat, Ali Aldalbahi, Azizah M. Malebari, Mohamed S. Nafie, Adnan A. Bekhit, Amgad Albohy, Alamgir Khan, Zaheer Ul-Haq, Matti Haukka, Beatriz G. de la Torre, Fernando Albericio, Ayman El-Faham|2022|ACS Omega|7|24858|doi:10.1021/acsomega.2c03079
CCDC 2163939: Experimental Crystal Structure Determination
Related Article: Ihab Shawish, Assem Barakat, Ali Aldalbahi, Azizah M. Malebari, Mohamed S. Nafie, Adnan A. Bekhit, Amgad Albohy, Alamgir Khan, Zaheer Ul-Haq, Matti Haukka, Beatriz G. de la Torre, Fernando Albericio, Ayman El-Faham|2022|ACS Omega|7|24858|doi:10.1021/acsomega.2c03079