- Facile synthesis of β-lactam-grafted spirooxindolopyrrolidine through regioselective 1,3-dipolar cycloaddition reaction
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One-pot synthesis of novel β-lactam-grafted spiropyrrolidines has been accomplished in good yield via a facile [3+2] cycloaddition reaction of azomethine ylides, derived from β-lactam aldehyde and sarcosine, with various p-substituted (E)-2-oxoindoline-3-
- Arumugam, Natarajan,Raghunathan, Raghavachary
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- Application of isatin analogues in preparing antineoplastic drugs
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The invention belongs to the field of medicinal chemistry, and in particular relates to an application of isatin analogues in preparing antineoplastic drugs. A series of isatin analogues can be synthesized by splicing isatin and [alpha],[beta]-unsaturated ketone via a medicinal chemistry splicing principle. The compounds (the isatin analogues) are relatively good in inhibitory activity on three tumor cells, and an antineoplastic effect can be achieved by inhibiting growth and migration of tumor cells and by blocking cell cycle G2/M period; and based upon in vivo experimental results, it is also indicated that the compounds can inhibit tumor growth.
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Paragraph 0035; 0036; 0040; 0042
(2018/07/30)
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- Design, synthesis and QSAR study of novel isatin analogues inspired Michael acceptor as potential anticancer compounds
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Molecular hybridization is considered as an effective tactic to develop drugs for the treatment of cancer. A series of novel hybrid compounds of isatin and Michael acceptor were designed and synthesized on the basis of association principle. These hybrid compounds were tested for cytotoxic potential against human cancer cell lines namely, BGC-823, SGC-7901 and NCI-H460 by MTT assay. Most compounds showed good anti-growth activities in all tested human cancer cells. SAR and QSAR analysis may provide vital information for the future development of novel anti-cancer inhibitors. Notably, compound 6a showed potent growth inhibition on BGC-823, SGC-7901 and NCI-H460 with the IC50 values of 3.6 ± 0.6, 5.7 ± 1.2, 3.2 ± 0.7 μM, respectively. Besides, colony formation assays, wound healing assays and flow cytometry analysis indicated 6a exhibited a potent anti-growth and anti-migration ability in a concentration-dependence manner through arrested cells in the G2/M phase of cell cycle. Moreover, 6a significantly repressed tumor growth in a NCI-H460 xenograft mouse model. Overall, our findings suggested isatin analogues inspired Michael acceptor may provide promising lead compounds for the development of cancer chemotherapeutics.
- Wang, Jiabing,Yun, Di,Yao, Jiali,Fu, Weitao,Huang, Fangyan,Chen, Liping,Wei, Tao,Yu, Cuijuan,Xu, Haineng,Zhou, Xiaoou,Huang, Yanqing,Wu, Jianzhang,Qiu, Peihong,Li, Wulan
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p. 493 - 503
(2018/01/01)
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- Highly efficient regioselective synthesis of pyrroles via a tandem enamine formation-Michael addition-cyclization sequence under catalyst- and solvent-free conditions
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A convenient catalyst-free, three-component procedure was developed for the synthesis of tetrasubstituted pyrroles under solvent-free conditions and in green solvents glycerol, PEG-200 and water. A sequential enamine-formation, Michael addition and intram
- Vivekanand, Thavaraj,Vinoth, Perumal,Agieshkumar,Sampath, Natarajan,Sudalai, Arumugam,Menéndez, J. Carlos,Sridharan, Vellaisamy
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p. 3415 - 3423
(2015/06/25)
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- Synthesis and biological evaluation of spiro[cyclopropane-1,3′-indolin]-2′-ones as potential anticancer agents
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Libraries of spiro[cyclopropane-1,3′-indolin]-2′-ones were synthesized and evaluated for their biological activity against five different human cancer cell lines HT-29 (colon cancer), DU-145 (prostate cancer), Hela (cervical cancer), A-549 (Lung cancer),
- Reddy, Chada Narsimha,Nayak, V. Lakshma,Mani, Geeta Sai,Kapure, Jeevak Sopanrao,Adiyala, Praveen Reddy,Maurya, Ram Awatar,Kamal, Ahmed
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p. 4580 - 4586
(2015/10/12)
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- Studies on the stereochemical assignment of 3-acylidene 2-oxindoles
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The designation of E/Z-geometrical isomers in 3-acylidene 2-oxindoles by NMR spectroscopy can lead to erroneous assignment of alkene stereochemistry because of the narrow chemical shift range observed over a large series of analogues. In contrast, UV-Vis spectroscopy offers a convenient and more reliable method for alkene stereochemical assignment. A combination of X-ray crystallography and theoretical studies shows that the observed differences in UV-Vis spectroscopic behaviour relate to the twisted conformation of the Z-isomers that provides reduced conjugation and weaker hypsochromic (blue-shifted) absorbances relative to those of the E-isomers.
- Edeson, Steven J.,Jiang, Julong,Swanson, Stephen,Procopiou, Panayiotis A.,Adams, Harry,Meijer, Anthony J. H. M.,Harrity, Joseph P. A.
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p. 3201 - 3210
(2014/05/06)
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- Reaction of isatins with acylmethylenetriphenylphosphoranes
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The Wittig reaction of isatin, 5-bromoisatin, and 1-acetylisatin with methoxycarbonyl- or aroylmethylenetriphenylphosphoranes proceeds regioselectively to give Z- or combined Z- and E-isomeric 3-acetylmethyleneindol-2-ones. Ethoxymethylenetriphenylphospho
- Koz'minykh,Berezina,Koz'minykh
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p. 1100 - 1105
(2007/10/03)
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