- Aqua mediated synthesis of substituted 2-amino-4H-chromenes and in vitro study as antibacterial agents
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A simple, clean, environmentally benign route to the synthesis of 2-amino-chromenes is described using K2CO3 as a green catalyst in water under microwave irradiation. This implies a convenient route avoiding the usage of hazardous or
- Kidwai, Mazaahir,Saxena, Shilpi,Khan, M. Khalilur Rahman,Thukral, Sharanjit S.
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- Discovery of novel rigid analogs of 2-naphthol with potent anticancer activity through multi-target topoisomerase I & II and tyrosine kinase receptor EGFR & VEGFR-2 inhibition mechanism
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A novel oxygen-containing heterocyclic linked 1H-benzo[f]chromene moieties (4a-g) and (6a-g) with anti-proliferative activity against cancer cell lines was designed, synthesized, and established on the basis of spectral data. All the prepared compounds were evaluated in vitro for their anti-proliferative activity against MCF-7, HCT-116, HepG-2 cell lines and normal cell lines HFL-1, WI-38. Compounds 4a, 4b, and 6e exhibited good activity against MCF-7, HCT-116, and HepG-2 cell lines, comparable to that of Vinblastine and Doxorubicin, and weak active against normal cell lines. Moreover, the potential mechanisms of the cytotoxic activity of the promising compounds 4a, 4b, and 6e on the more sensitive cell line MCF-7 were studied. We found that compounds 4a, 4b, and 6e induce cell cycle arrest at G2/M phases for MCF-7 treated cells compared to untreated cells, which causes apoptosis and inhibits both the topoisomerase I and II enzymes. In addition, compounds 4a and 4b exhibited comparable inhibitory activity on tyrosine kinase receptors EGFR and VEGFR-2 kinases to that of the reference protein kinases inhibitor Sorafenib. The in silico molecular docking of the most active compounds into the active sites of EGFR kinase and Topo I & II enzymes provides us with a reasonable clarification of the interpreted biological data.
- Alshahrani, Mohammed Y.,El-Agrody, Ahmed M.,El-Mawgoud, Heba K. A.,El-Nassag, Mohammed A. A.,Elhenawy, Ahmed A.,Fouda, Ahmed M.
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- Clean, one-pot synthesis of naphthopyran derivatives in aqueous media
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A general and practical one-pot synthesis of naphthopyran derivatives using hexadecyltrimethylammonium bromide (HTMAB) as catalyst (10 mol%) is described. This method provides several advantages such as neutral conditions, high yields and simple workup pr
- Jin, Tong-Shou,Zhang, Jian-She,Liu, Li-Bin,Wang, Ai-Qing,Li, Tong-Shuang
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p. 2009 - 2015
(2007/10/03)
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- Heterocycles synthesis through reactions of nucleophiles with acrylonitriles: Part XI - A convenient one-pot synthesis of 4H-chromenes
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Several new 4H-chromenes (IVa-j and Va-j) have been synthesised by a one-step and facile method in excellent yields. The reaction mechanism is also reported.
- Abdel-Latif
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p. 664 - 666
(2007/10/02)
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