Helmy I. Heiba

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Computer-Based Ligand Design and Synthesis of Some New Sulfonamides Bearing Pyrrole or Pyrrolopyrimidine Moieties Having Potential Antitumor and Radioprotective Activities

Phosphorus, sulfur, and silicon and the related elements (2007)

Mostafa M. Ghorab Helmy I. Heiba Amira Khalil Dalal A. Abou El Ella Eman Noaman

A series of new Pyrrole and pyrrolo[2,3-d]pyrimidine derivatives ( 5–15 ) was designed, synthesized, and biologically evaluated for their in vitro cytotoxic activity. The design of these compounds was based upon the molecular modeling simulation of the fitting values and conformational energy values of the best-fitted conformers to VEGFRTK inhibitors hypothesis. This hypothesis was generated from its corresponding lead compounds using CATALYST software. Some of the newly synthesized compounds 8 , 11 , 12 , and 13 showed interesting cytotoxic activity compared with Doxorubicin as a reference drug. These results are nearly consistent with the molecular modeling studies. Moreover, Compound 7 showed significant radioprotective activity.

Pyrrole

Conformational isomerism

Molecular model

10.1080/10426500701557104

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Citations (18)

Novel Antitumor and Radioprotective Sulfonamides Containing Pyrrolo[2,3‐d]pyrimidines.

ChemInform (2006)

Moustafa M. Ghorab Eman Noaman Magda M. F. Ismail Helmy I. Heiba Yousry A. Ammar

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

10.1002/chin.200643177

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Citations (10)

Anticancer and radio-sensitizing evaluation of some new thiazolopyrane and thiazolopyranopyrimidine derivatives bearing a sulfonamide moiety

European Journal of Medicinal Chemistry (2011)

Mostafa M. Ghorab Fatma A. Ragab Helmy I. Heiba Reham M. M. El‐Hazek

Moiety

Sulfonamide

10.1016/j.ejmech.2011.08.026

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Citations (43)

Novel Antitumor and Radioprotective Sulfonamides Containing Pyrrolo[2,3-d]pyrimidines

Arzneimittelforschung (2011)

Moustafa M. Ghorab Eman Noaman Magda M. F. Ismail Helmy I. Heiba Yousry A. Ammar

Several sulfonamides having pyrrole (5a-c, 8, 11b-19, 23, 24), pyrrolo[2,3-d] pyrimidine (6, 7, 10, 20, 21, 25) and pyrrolo[2,3-b]pyridine (22) were synthesized and evaluated for their antitumor and radioprotective activities. The structure of the synthesized compounds was elucidated by elemental analyses and spectral data. Compounds 5a, 16, 17, 19, and 23 displayed more potent antitumor activities than the reference drug, doxorubicin. On the other hand compounds 19, 23 and 25 exhibited radioprotective activities.

Pyrrole

10.1055/s-0031-1296742

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Citations (24)

ChemInform Abstract: Novel Thiophenes, Thienopyrimidines, and Triazolothienopyrimidines for the Evaluation of Anticancer and Augmentation Effects of γ‐Radiation.

ChemInform (2010)

Mohamed A. Shaaban Mostafa M. Ghorab Helmy I. Heiba Mona M. Kamel Nashwa H. Zaher

Abstract Compounds (III), (IV), (VIII) and (X) show significant in vitro cytotoxic activity against hepatocellular carcinoma compared to the reference drug doxorubicin.

Anticancer drug

10.1002/chin.201047156

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Citations (0)

ChemInform Abstract: Design and Synthesis of Some Novel Quinoline Derivatives as Anticancer and Radiosensitizing Agents Targeting VEGFR Tyrosine Kinase.

ChemInform (2012)

Mostafa M. Ghorab Fatma A. Ragab Helmy I. Heiba Walid M. Ghorab

Abstract A variety of novel quinoline and pyrimidoquinoline derivatives (XVI) is synthesized from enaminone (I), and evaluated for in vitro effects against the human cancer cell line MCF7.

Quinoline

Cancer cell lines

10.1002/chin.201216155

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Citations (0)

Design and synthesis of some novel 4-Chloro- N -(4-(1-(2-(2-cyanoacetyl)hydrazono)ethyl)phenyl) benzenesulfonamide derivatives as anticancer and radiosensitizing agents

European Journal of Medicinal Chemistry (2016)

Mostafa M. Ghorab Fatma A. Ragab Helmy I. Heiba Aiten M. Soliman

10.1016/j.ejmech.2016.04.009

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Citations (46)

Novel thioureido-benzenesulfonamide derivatives with enaminone linker as potent anticancer, radiosensitizers and VEGFR2 inhibitors

Bioorganic & Medicinal Chemistry Letters (2018)

Mostafa M. Ghorab Fatma A. Ragab Helmy I. Heiba Marwa G. El‐Gazzar Mostafa G.M. El-Gazzar

Linker

IC50

Docking (animal)

Molecular model

10.1016/j.bmcl.2018.03.089

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Citations (27)

Synthesis of Some Novel Sulfonamides Containing Biologically Active Alkanoic Acid, Acetamide, Thiazole, and Pyrrole Moieties of Expected Antitumor and Radiosensitizing Activities

Mostafa M. Ghorab Fatma A. Ragab Helmy I. Heiba Hebaallah M. Agha

Several novel N 4 substituted sulfapyridine derivatives were synthesized by condensation of 2-ChloroN-(4-(N-pyridin-2-ylsulfamoyl)phenyl) acetamide 2 with different amino acids, amines, malononitrile, or ammonium thiocyanate to yield the corresponding alkanoic acid derivatives 3a-f, acetamide derivatives 4- 8, pyrrole derivatives 9- 12, and thiazolidinone derivative 13. The newly synthesized compounds were screened in-vitro against human breast cancer cell line (MCF-7). Compounds 3b, 10 and 12 showed the highest activity with IC50 values 26.1, 22.4, 22.1 µM compared to doxorubicin as a reference drug. The promising compounds 3b, 10 and 12 showed the ability to sensitize cancer cells to the lethal effects of ionizing radiation.

Acetamide

Thiazole

Chloroacetic acid

Ammonium thiocyanate

Source

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Citations (6)

Synthesis, in vitro anticancer screening and radiosensitizing evaluation of some new 4-[3-(substituted)thioureido]-N-(quinoxalin-2-yl)-benzenesulfonamide derivatives

Acta Pharmaceutica (2011)

Mostafa M. Ghorab Fatma A. Ragab Helmy I. Heiba Marwa G. El‐Gazzar Mostafa G.M. El-Gazzar

Synthesis, in vitro anticancer screening and radiosensitizing evaluation of some new 4-[3-(substituted)thioureido]- N -(quinoxalin-2-yl)-benzenesulfonamide derivatives Sulfonamides and quinoxaline derivatives possess many types of biological activities and have been recently reported to show substantial antitumor activity. This paper reports the synthesis of novel thioureido sulfaquinoxaline derivatives. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against a human liver cell line (HEPG2) and showed higher activity than the reference drug doxorubicin. 4-(3-(4-Ethylbenzoate) thioureido)- N -(quinoxalin-2-yl)benzenesulfonamide ( 9 ) ( IC 50 = 15.6 μmol L -1 ), N -(pyridin-2-yl)-4-(3-(4-( N -quinoxalin-2-yl-sulfamoyl)phenyl)thioureido)benzenesulfonamide ( 10 ) ( IC 50 = 26.8 μmol L -1 ) and N -(quinoxalin-2-yl)-4-(3-(4-( N -thiazol-2-ylsulfamoyl)phenyl)thioureido)benzenesulfonamide ( 11 ) ( IC 50 = 24.4 μmol L -1 ) were the most potent compared to doxorubicin ( IC 50 = 71.8 μmol L -1 ). The most potent compounds 9, 10 and 11 were evaluated as radiosensitizing agents by subjecting the compounds to γ-irradiation (8 kGy).

Quinoxaline

10.2478/v10007-011-0040-4

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Citations (26)