211817-58-2Relevant academic research and scientific papers
Pharmacophore-based virtual screening, synthesis, biological evaluation, and molecular docking study of novel pyrrolizines bearing urea/thiourea moieties with potential cytotoxicity and CDK inhibitory activities
Shawky, Ahmed M.,Ibrahim, Nashwa A.,Abourehab, Mohammed A. S.,Abdalla, Ashraf N.,Gouda, Ahmed M.
, p. 15 - 33 (2020/11/04)
In the current study, virtual screening of a small library of 1302 pyrrolizines bearing urea/thiourea moieties was performed. The top-scoring hits were synthesised and evaluated for their cytotoxicity against three cancer (MCF-7, A2780, and HT29) and one normal (MRC-5) cell lines. The results of the MTT assay revealed potent cytotoxic activities for most of the new compounds (IC50 = 0.16–34.13 μM). The drug-likeness study revealed that all the new compounds conform to Lipinski’s rule. Mechanistic studies of compounds 18 b, 19a, and 20a revealed the induction of apoptosis and cell cycle arrest at the G1 phase in MCF-7 cells. The three compounds also displayed potent inhibitory activity against CDK-2 (IC50 = 25.53–115.30 nM). Moreover, the docking study revealed a nice fitting of compound 19a into the active sites of CDK-2/6/9. These preliminary results suggested that compound 19a could serve as a promising scaffold in the discovery of new potent anticancer agents.
Novel pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety: design, synthesis, molecular docking, and biological evaluation as potential multi-target cytotoxic agents
Shawky, Ahmed M.,Ibrahim, Nashwa A.,Abdalla, Ashraf N.,Abourehab, Mohammed A. S.,Gouda, Ahmed M.
, p. 1313 - 1333 (2021/06/25)
In the present study, two new series of pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety were designed, synthesised, and evaluated for their cytotoxic activity. The benzamide derivatives 16a–e showed higher cytotoxicity than their corresponding Schiff b
Optimization of pyrrolizine-based Schiff bases with 4-thiazolidinone motif: Design, synthesis and investigation of cytotoxicity and anti-inflammatory potency
Shawky, Ahmed M.,Abourehab, Mohammed A.S.,Abdalla, Ashraf N.,Gouda, Ahmed M.
, (2019/10/28)
Two new series of pyrrolizine-5-carboxamides were synthesized and evaluated for their anticancer and anti-inflammatory activities. The new compounds exhibited potent cytotoxicity (IC50 = 0.10–22.96 μM) against three cancer (MCF-7, A2780 and HT2
Antitumor activity of pyrrolizines and their Cu(II) complexes: Design, synthesis and cytotoxic screening with potential apoptosis-inducing activity
Gouda, Ahmed M.,El-Ghamry, Hoda A.,Bawazeer, Tahani M.,Farghaly, Thoraya A.,Abdalla, Ashraf N.,Aslam, Akhmed
, p. 350 - 359 (2018/01/17)
Two novel series including Schiff bases of the pyrrolizine-5-carboxamides and their Cu(II) complexes were designed, synthesized and analysed using spectral and analytical techniques. The analytical results indicated the formation of the complexes in 1:1 o
Pyrrolizines: Design, synthesis, anticancer evaluation and investigation of the potential mechanism of action
Gouda, Ahmed M.,Abdelazeem, Ahmed H.,Omar, Hany A.,Abdalla, Ashraf N.,Abourehab, Mohammed A.S.,Ali, Hamed I.
, p. 5637 - 5651 (2017/10/09)
A novel set of pyrrolizine-5-carboxamides has been synthesized and evaluated for their anticancer potential against human breast MCF-7, lung carcinoma A549 and hepatoma Hep3B cancer cell lines. Compound 10c was the most active against MCF-7 with IC50
Novel substituted and fused pyrrolizine derivatives: Synthesis, anti-inflammatory and ulcerogenecity studies
Abbas, Safinaz E.,Awadallah, Fadi M.,Ibrahim, Nashwa A.,Gouda, Ahmed M.
scheme or table, p. 482 - 491 (2010/04/02)
Synthesis of several substituted pyrrolizines 10a-f, 11a-f, 13a-c, pyrimidopyrrolizines 14a-c, 15a-c, and pyrrolizinopyrimidoisoindoles 12a-c was discussed. The starting compounds 6-amino-7-cyano-N-(4-(un)substitutedphenyl)-2,3-dihydro-1H-pyrrolizine-5 -c
