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(searched for: doi:10.5155/eurjchem.3.2.179-185.562)
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Ayaz Anwar, , Abdul Hameed, Muhammad R. Shah,
Medicinal Chemistry, Volume 16, pp 841-847; https://doi.org/10.2174/1573406415666190722113412

Abstract:
Background: Acanthamoeba is an opportunistic pathogen widely spread in the environment. Acanthamoeba causes excruciating keratitis which can lead to blindness. The lack of effective drugs and its ability to form highly resistant cyst are one of the foremost limitations against successful prognosis. Current treatment involves mixture of drugs at high doses but still recurrence of infection can occur due to ineffectiveness of drugs against the cyst form. Pyridine and its natural and synthetic derivatives are potential chemotherapeutic agents due to their diverse biological activities. Objective: To study the antiamoebic effects of four novel synthetic dihydropyridine (DHP) compounds against Acanthamoeba castellanii belonging to the T4 genotype. Furthermore, to evaluate their activity against amoeba-mediated host cells cytopathogenicity as well as their cytotoxicity against human cells. Methods: Dihydropyridines were synthesized by cyclic dimerization of alkylidene malononitrile derivatives. Four analogues of functionally diverse DHPs were tested against Acanthamoeba castellanii by using amoebicidal, encystation and excystation assays. Moreover, Lactate dehydrogenase assays were carried out to study cytopathogenicity and cytotoxicity against human cells. Results: These compounds showed significant amoebicidal and cysticidal effects at 50 μM concentration, whereas, two of the DHP derivatives also significantly reduced Acanthamoebamediated host cell cytotoxicity. Moreover, these DHPs were found to have low cytotoxicity against human cells suggesting a good safety profile. Conclusion: The results suggest that DHPs have potential against Acanthamoeba especially against the more resistant cyst stage and can be assessed further for drug development.
Hina Yousuf, Shahbaz Shamim, , , Kanwal, Shehryar Hameed, Muhammad Naseem Khan, Muhammad Taha,
Published: 15 January 2020
Bioorganic Chemistry, Volume 96; https://doi.org/10.1016/j.bioorg.2020.103581

The publisher has not yet granted permission to display this abstract.
, Syeda Tazeen Zehra, Saba Abbas, Riffat Un Nisa, , , Mariya Al-Rashida, Jürgen Bajorath, Khalid Mohammed Khan,
Published: 21 January 2016
Bioorganic Chemistry, Volume 65, pp 38-47; https://doi.org/10.1016/j.bioorg.2016.01.004

The publisher has not yet granted permission to display this abstract.
Nafees Iqbal, , Syed Abid Ali, , , Shakeel Ahmad, Khalid Mohammed Khan, Fatima Zahra Basha, ,
Published: 30 October 2015
RSC Advances, Volume 5, pp 95061-95072; https://doi.org/10.1039/C5RA16075H

Abstract:
The role of ionic liquids as catalyst and solvent to mediate organic reactions is well documented.
Ayaz Anwar, , Shahida Perveen, Maliha Uroos, Muhammad Iqbal Choudhary, Fatima Zahra Basha
European Journal of Chemistry, Volume 5, pp 189-191; https://doi.org/10.5155/eurjchem.5.1.189-191.916

European Journal of Chemistry, Volume 4, pp 49-52; https://doi.org/10.5155/eurjchem.4.1.49-52.701

Abstract:
A novel series of tricyano substituted polyfunctional 5,6-dihydropyridine 8a-n bearing functionalized aromatic rings at C-4 and C-6 position have been prepared from (α-methylbenzylidene) malononitriles in good to excellent yields (52-98%) in solvent free conditions. All the synthesized compounds (8a-n) were evaluated for their in vitro urease inhibition and anticancer activity against prostate cancer (PC3) and Hela cell lines. Compound 8k (4,6-bis(4-methoxyphenyl)-5,6-dihydropyridin) showed slightly better urease inhibitory potential (IC50 = 20.47 µM) as compared to standard thiourea (IC50 = 21 µM). Whilst in the case of anticancer studies the compound 8a 2-(4,6-bis(4-bromophenyl)-6-methyl-5,6-dihydropyridin found to be most active (IC50 = 4.40 and 8.80 µM) among the series when compared with standard doxorubicin 4 (IC50 = 0.91 and 3.1 µM) in both cell lines respectively. A structure-activity relationship of this series has been established on the basis of electronic effects and position of different substituents (H, Br, Cl, I, F, Me, OMe, OH, and NO2) present on the C-4 and C-6 phenyl rings. The anticancer activity evaluation of these pyridine derivatives envisage that the compound 8a could be putatively linked with doxorubicin IV to developed new anticancer prodrugs for multidrug resistant (MDR) cancer cells. All the synthesized compounds were characterized by spectroscopic techniques.
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