Synthesis and Biological Evaluation of Some New Ferrocenyl Phenyl Guanidines as Antibacterial, Antifungal Agents
Rukhsana Gul,
Zainab Nawaz,
Amin Badshah,
Azim Khan,
Asif Junaid,
Rabia Naz,
Muhammad Kamran Rauf,
Saima Hayat
Issue:
Volume 2, Issue 4, August 2016
Pages:
35-39
Received:
29 February 2016
Accepted:
29 March 2016
Published:
1 August 2016
Abstract: A series of new ferrocenylphenylguanidines (d-1 to d-4) were synthesized via multistep protocol. The purity of synthesized compounds were determined by melting point and TLC and their structures were established by various analytical techniques such as elemental analysis, multinuclear (1H and 13C) NMR and FTIR spectroscopy. The newly synthesized compounds were screened for antimicrobial activity against a panel of microorganisms (five bacterial strains, i.e three Gram positive, Staphylococcus aureus (ATCC 6538), Pseudomonas aeruginosa (ATCC 6538), Bacillus subtilis (ATCC 6633) and two Gram negative, Klebsiella pneumonia (ATCC 43816), Escherichia coli (ATCC 15224) and three fungal strains, i.e. Fusa riumm oniliforme, Aspergillus fumigates and Aspergillusflavus. These compounds were found to have moderate antibacterial and good antifungal activities, especially for compounds having electronegative substituent on phenyl group.
Abstract: A series of new ferrocenylphenylguanidines (d-1 to d-4) were synthesized via multistep protocol. The purity of synthesized compounds were determined by melting point and TLC and their structures were established by various analytical techniques such as elemental analysis, multinuclear (1H and 13C) NMR and FTIR spectroscopy. The newly synthesized co...
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Synthesis and Biological Evaluation of 3-Aryl Pyrazoles as CDK2/HDAC Inhibitor for Anticancer Agents
Xianfeng Huang,
Bei Yang,
Yuanyuan Liu,
Cheng Zhang,
Guoqiang Song
Issue:
Volume 2, Issue 4, August 2016
Pages:
40-46
Received:
17 May 2016
Accepted:
20 June 2016
Published:
1 August 2016
Abstract: A novel series of pyrazole derivatives containing hydroxamic acid group were designed and synthesized as multi-target inhibitors targeting CDK2 (cyclin-dependent kinases 2) and HDAC (histone deacetylase). Compounds 6e and 6f exhibited most potent CDK2 inhibition as well as HDAC inhibition. In vitro antiproliferative assay indicated that several compounds showed better antiproliferative potency compared to olomoucine and SAHA. Docking simulation suggested a common mode of interaction at the active binding sites of CDK2 and HDAC, which demonstrates that compound 6f is a potential agent for cancer therapy deserving further researching.
Abstract: A novel series of pyrazole derivatives containing hydroxamic acid group were designed and synthesized as multi-target inhibitors targeting CDK2 (cyclin-dependent kinases 2) and HDAC (histone deacetylase). Compounds 6e and 6f exhibited most potent CDK2 inhibition as well as HDAC inhibition. In vitro antiproliferative assay indicated that several com...
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