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Novel coumarin-6-sulfonamides as Apoptotic Anti-Proliferative Agents: Synthesis, in Vitro Biological Evaluation, and QSAR Studies

Novel coumarin-6-sulfonamides as Apoptotic Anti-Proliferative Agents: Synthesis, in Vitro Biological Evaluation, and QSAR Studies

Ahmed Sabt, Omaima M Abdelhafez, Radwan S El-Haggar, Hassan M F Madkour, Wagdy M Eldehna, Ezz El-Din A M El-Khrisy, Mohamed A Abdel-Rahman, Laila A Rashed

J Enzyme Inhib Med Chem. 2018 Dec;33(1):1095-1107.

PMID: 29944015

Abstract:

Herein, we report the synthesis of different novel sets of coumarin-6-sulfonamide derivatives bearing different functionalities (4a, b, 8a-d, 11a-d, 13a, b, and 15a-c), and in vitro evaluation of their growth inhibitory activity towards the proliferation of three cancer cell lines; HepG2 (hepatocellular carcinoma), MCF-7 (breast cancer), and Caco-2 (colon cancer). HepG2 cells were the most sensitive cells to the influence of the target coumarins. Compounds 13a and 15a emerged as the most active members against HepG2 cells (IC50 = 3.48 ± 0.28 and 5.03 ± 0.39 µM, respectively). Compounds 13a and 15a were able to induce apoptosis in HepG2 cells, as assured by the upregulation of the Bax and downregulation of the Bcl-2, besides boosting caspase-3 levels. Besides, compound 13a induced a significant increase in the percentage of cells at Pre-G1 by 6.4-folds, with concurrent significant arrest in the G2-M phase by 5.4-folds compared to control. Also, 13a displayed significant increase in the percentage of annexin V-FITC positive apoptotic cells from 1.75-13.76%. Moreover, QSAR models were established to explore the structural requirements controlling the anti-proliferative activities.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP38215360	Coumarin 6		38215-36-0	Price

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