- Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors
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In the present study, we describe the design of different series of benzofuran-based derivatives as potential carbonic anhydrase inhibitors (CAIs). The adopted design is based on bioisosteric replacement for the p-fluorophenyl SLC-0111 tail with the lipop
- Shaldam, Moataz,Eldehna, Wagdy M.,Nocentini, Alessio,Elsayed, Zainab M.,Ibrahim, Tamer M.,Salem, Rofaida,El-Domany, Ramadan A.,Capasso, Clemente,Abdel-Aziz, Hatem A.,Supuran, Claudiu T.
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- Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer
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In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a–e and 7a–i) was designed and synthesised. The anticancer activity for compounds (5b–d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subjected to the five-dose screen where it showed excellent broad activity against almost all tested cancer subpanels. Furthermore, all conjugates (5a–e and 7a–i) showed a good anti-proliferative activity towards colorectal cancer SW-620 and HT-29 cell lines, with an excellent inhibitory effect for compounds 5a and 5d (IC50 = 8.7 and 9.4 μM (5a), and 6.5 and 9.8 μM for (5d), respectively). Both compounds displayed selective cytotoxicity with good safety profile. In addition, both compounds provoked apoptosis in a dose dependent manner in SW-620 cells. Also, they significantly inhibited the anti-apoptotic Bcl2 protein expression and increased the cleaved PARP level that resulted in SW-620 cells apoptosis.
- Eldehna, Wagdy M.,Salem, Rofaida,Elsayed, Zainab M.,Al-Warhi, Tarfah,Knany, Hamada R.,Ayyad, Rezk R.,Traiki, Thamer Bin,Abdulla, Maha-Hamadien,Ahmad, Rehan,Abdel-Aziz, Hatem A.,El-Haggar, Radwan
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p. 1424 - 1435
(2021/07/02)
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- Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells
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As one of the most lethal malignancies, lung cancer is considered to account for approximately one-fifth of all malignant tumours-related deaths worldwide. This study reports the synthesis and in?vitro biological assessment of two sets of 3-methylbenzofurans (4a–d, 6a–c, 8a–c and 11) and 3-(morpholinomethyl)benzofurans (15a–c, 16a–b, 17a–b and 18) as potential anticancer agents towards non-small cell lung carcinoma A549 and NCI-H23 cell lines, with VEGFR-2 inhibitory activity. The target benzofuran-based derivatives efficiently inhibited the growth of both A549 and NCI-H23 cell lines with IC50 spanning in ranges 1.48–47.02 and 0.49–68.9 μM, respectively. The three most active benzofurans (4b, 15a and 16a) were further investigated for their effects on the cell cycle progression and apoptosis in A549 (for 4b) and NCI-H23 (for 15a and 16a) cell lines. Furthermore, benzofurans 4b, 15a and 16a displayed good VEGFR-2 inhibitory activity with IC50 equal 77.97, 132.5 and 45.4 nM, respectively.
- Al-Sanea, Mohammad M.,Al-Ansary, Ghada H.,Elsayed, Zainab M.,Maklad, Raed M.,Elkaeed, Eslam B.,Abdelgawad, Mohamed A.,Bukhari, Syed Nasir Abbas,Abdel-Aziz, Marwa M.,Suliman, Howayda,Eldehna, Wagdy M.
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p. 987 - 999
(2021/05/21)
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- Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer
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Pursuing our effort for developing effective inhibitors of the cancer-related hCA IX isoform, here we describe the synthesis of novel benzofuran-based carboxylic acid derivatives, featuring the benzoic (9a-f) or hippuric (11a,b) acid moieties linked to 2-
- Abdel-Aziz, Hatem A.,Al-Sanea, Mohammad M.,Al-Warhi, Tarfah,Aljaeed, Nada,Alotaibi, Ohoud J.,Eldehna, Wagdy M.,Elsayed, Zainab M.,Nocentini, Alessio,Supuran, Claudiu T.
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p. 1022 - 1027
(2020/06/27)
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- 4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors
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Histone lysine specific demethylase 1 (LSD1 or KDM1A) is a potential therapeutic target in oncology due to its overexpression in various human tumors. We report herein a new class of benzofuran acylhydrazones as potent LSD1 inhibitors. Among the 31 compounds prepared, 14 compounds exhibited excellent LSD1 inhibitory activity with IC50 values ranging from 7.2 to 68.8 nM. In cellular assays, several compounds inhibited the proliferations of various cancer cell lines, including PC-3, MCG-803, U87 MG, PANC-1, HT-29 and MCF-7. This opens up the opportunity for further optimization and investigation of this class compounds for potential cancer treatment.
- Gao, Yuan,He, Xingrui,Hui, Zi,Shen, Guodong,Wang, Shuo,Xie, Tian,Ye, Xiang-Yang
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- Synthesis, SAR, molecular docking and antituberculosis study of 3-methyl-1-benzofuran-2-carbohydrazide
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3-Methyl-1-benzofuran-2-carbohydrazide was synthesized from 2-hydroxy acetophenone. To deduce the antibacterial and anticancer activity of the 3-methyl-1-benzofuran-2-carbohydrazide, it is docked with different biomarkers of cancer cell and bacteria. The
- Thorat, Bapu R.,Nazirkar, Bhusan,Thorat, Vaishali B.,More, Kishor,Jagtap, Ravindra,Yamgar, Ramesh
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p. 2346 - 2352
(2016/10/12)
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