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Ebaa M Elhossary - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and in vitro Anticancer Screening of some novel 4 2 amino 3 cyano 4 substituted 5 6 7 8 tetrahydroquinolin 1 4h yl benzenesulfonamides
    ChemInform, 2010
    Co-Authors: Mansour S Alsaid, Mostafa M Ghorab, Ebaa M Elhossary, Saleh I Alqasoumi, Eman Noaman
    Abstract:

    All newly synthesized compounds are evaluated for their in vitro Anticancer activity compared to doxorubicin as reference drug.

  • in vitro Anticancer Screening and radiosensitizing evaluation of some new quinolines and pyrimido 4 5 b quinolines bearing a sulfonamide moiety
    European Journal of Medicinal Chemistry, 2010
    Co-Authors: Mostafa M Ghorab, Fatma A Ragab, Helmy I Heiba, Reem K Arafa, Ebaa M Elhossary
    Abstract:

    Abstract Sulfonamide bearing compounds posses many types of biological activities and have recently been reported to show substantial antitumor activity in vitro and/or in vivo . There are a variety of mechanisms for the Anticancer activity, and the most prominent mechanism is the inhibition of carbonic anhydrase (CA) isozymes. The present work reports the synthesis of twenty novel quinoline and pyrimido[4,5- b ]quinoline derivatives bearing a sulfonamide moiety. The new synthesized compounds were designed in compliance with the general pharmacophoric requirements for CA inhibiting Anticancer drugs, as this may play a role in their Anticancer activity. All the newly synthesized compounds were evaluated for their in vitro Anticancer activity against human breast cancer cell line (MCF7). Compounds 6 , 9 and 18 showed IC 50 values (72.9 μM, 72.1 μM and 71.9 μM, respectively) comparable to that of the reference drug doxorubicin (IC 50 = 71.8 μM). On the other hand, compound 8 exhibited better activity than doxorubicin with an IC 50 value of 64.5 μM. Additionally, the most potent compounds 8 and 18 were evaluated for their ability to enhance the cell killing effect of γ-radiation.

  • synthesis and in vitro Anticancer Screening of some novel 4 2 amino 3 cyano 4 substituted 5 6 7 8 tetrahydroquinolin 1 4h yl benzenesulfonamides
    European Journal of Medicinal Chemistry, 2010
    Co-Authors: Mansour S Alsaid, Mostafa M Ghorab, Ebaa M Elhossary, Saleh I Alqasoumi, Eman Noaman
    Abstract:

    Abstract It has been reported that aryl/heteroaryl sulfonamide compounds may act as Anticancer agents through a variety of mechanisms and the most prominent of these mechanisms is through the inhibition of carbonic anhydrase isozymes. The present work reports the possible utility of 4-(cyclohexenylamino)benzenesulfonamide in the synthesis of some novel 4-(quinolin-1-yl)benzenesulfonamide derivatives 6a – u . The structures of these compounds were confirmed by elemental analyses, IR, 1 H NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in vitro Anticancer activity. Some compounds showed interesting in vitro Anticancer activities when compared with doxorubicin as a reference drug. In addition, docking of the synthesized compounds into carbonic anhydrase isozyme II (CA II) active site was performed in order to give a suggestion about the proposed mechanism of action.

Eman Noaman - One of the best experts on this subject based on the ideXlab platform.

Mostafa M Ghorab - One of the best experts on this subject based on the ideXlab platform.

  • synthesis and in vitro Anticancer Screening of some novel 4 2 amino 3 cyano 4 substituted 5 6 7 8 tetrahydroquinolin 1 4h yl benzenesulfonamides
    ChemInform, 2010
    Co-Authors: Mansour S Alsaid, Mostafa M Ghorab, Ebaa M Elhossary, Saleh I Alqasoumi, Eman Noaman
    Abstract:

    All newly synthesized compounds are evaluated for their in vitro Anticancer activity compared to doxorubicin as reference drug.

  • in vitro Anticancer Screening and radiosensitizing evaluation of some new quinolines and pyrimido 4 5 b quinolines bearing a sulfonamide moiety
    European Journal of Medicinal Chemistry, 2010
    Co-Authors: Mostafa M Ghorab, Fatma A Ragab, Helmy I Heiba, Reem K Arafa, Ebaa M Elhossary
    Abstract:

    Abstract Sulfonamide bearing compounds posses many types of biological activities and have recently been reported to show substantial antitumor activity in vitro and/or in vivo . There are a variety of mechanisms for the Anticancer activity, and the most prominent mechanism is the inhibition of carbonic anhydrase (CA) isozymes. The present work reports the synthesis of twenty novel quinoline and pyrimido[4,5- b ]quinoline derivatives bearing a sulfonamide moiety. The new synthesized compounds were designed in compliance with the general pharmacophoric requirements for CA inhibiting Anticancer drugs, as this may play a role in their Anticancer activity. All the newly synthesized compounds were evaluated for their in vitro Anticancer activity against human breast cancer cell line (MCF7). Compounds 6 , 9 and 18 showed IC 50 values (72.9 μM, 72.1 μM and 71.9 μM, respectively) comparable to that of the reference drug doxorubicin (IC 50 = 71.8 μM). On the other hand, compound 8 exhibited better activity than doxorubicin with an IC 50 value of 64.5 μM. Additionally, the most potent compounds 8 and 18 were evaluated for their ability to enhance the cell killing effect of γ-radiation.

  • synthesis and in vitro Anticancer Screening of some novel 4 2 amino 3 cyano 4 substituted 5 6 7 8 tetrahydroquinolin 1 4h yl benzenesulfonamides
    European Journal of Medicinal Chemistry, 2010
    Co-Authors: Mansour S Alsaid, Mostafa M Ghorab, Ebaa M Elhossary, Saleh I Alqasoumi, Eman Noaman
    Abstract:

    Abstract It has been reported that aryl/heteroaryl sulfonamide compounds may act as Anticancer agents through a variety of mechanisms and the most prominent of these mechanisms is through the inhibition of carbonic anhydrase isozymes. The present work reports the possible utility of 4-(cyclohexenylamino)benzenesulfonamide in the synthesis of some novel 4-(quinolin-1-yl)benzenesulfonamide derivatives 6a – u . The structures of these compounds were confirmed by elemental analyses, IR, 1 H NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in vitro Anticancer activity. Some compounds showed interesting in vitro Anticancer activities when compared with doxorubicin as a reference drug. In addition, docking of the synthesized compounds into carbonic anhydrase isozyme II (CA II) active site was performed in order to give a suggestion about the proposed mechanism of action.

Mansour S Alsaid - One of the best experts on this subject based on the ideXlab platform.

Saleh I Alqasoumi - One of the best experts on this subject based on the ideXlab platform.