Abdelfattah Hassan

Abdelfattah Hassan

South Valley University

H-index: 4

Africa-Egypt

Abdelfattah Hassan Information

University

South Valley University

Position

Assistant Lecturer Faculty of pharmacy

Citations(all)

59

Citations(since 2020)

58

Cited By

7

hIndex(all)

4

hIndex(since 2020)

4

i10Index(all)

2

i10Index(since 2020)

2

Email

University Profile Page

South Valley University

Abdelfattah Hassan Skills & Research Interests

Medicinal Chemistry

Top articles of Abdelfattah Hassan

Design and biological evaluation of 3-substituted quinazoline-2,4(1H,3H)-dione derivatives as dual c-Met/VEGFR-2-TK inhibitors

The dual c-Met/vascular endothelial growth factor receptor 2 (VEGFR-2) TK inhibition is a good strategy to overcome therapeutic resistance to small molecules VEGFR-2 inhibitors. In this study, we designed 3-substituted quinazoline-2,4(1H,3H)-dione derivatives as dual c-Met/VEGFR-2 TK inhibitors. We introduced new synthetic methods for reported derivatives of 3-substituted quinazoline-2,4(1H,3H)-dione 2a–g, in addition to the preparation of some new derivatives namely, 3 and 4a–j. Three compounds namely, 2c, 4b, and 4e showed substantial amount of inhibition for both c-Met and VEGFR-2 TK (IC50 range 0.052–0.084 µM). Both compounds 4b, 4e showed HB with highly conserved residue Asp1222 in the HB region of c-Met TK. For VEGFR-2 TK, compound 4b showed HB with a highly conserved residue Asp1046 in the HB region. Compound 4e showed HB with Glu885 and Asp1046. Moreover, in silico …

Authors

Abdelfattah Hassan,Fawzy AF Mubarak,Ihsan A Shehadi,Ahmed M Mosallam,Hussain Temairk,Mohamed Badr,Aboubakr H Abdelmonsef

Journal

Journal of Enzyme Inhibition and Medicinal Chemistry

Published Date

2023/12/31

Novel 3-phenylquinazolin-2,4(1H,3H)-diones as dual VEGFR-2/c-Met-TK inhibitors: design, synthesis, and biological evaluation

Multitarget anticancer drugs are more superior than single target drugs regarding patient compliance, drug adverse effects, drug-drug interactions, drug resistance as well as pharmaceutical industry economics. Dysregulation of both VEGFR-2 and c-Met tyrosine kinases (TKs) could result in development and progression of different human cancers. Herein, we reported a novel series of 3-phenylquinazolin-2,4(1H,3H)-diones with thiourea moiety as dual VEGFR-2/c-Met TKs. Compared to sorafenib, cabozantinib went behind VEGFR-2 inhibition to target c-Met TK. The dual VEGFR-2/c-Met inhibitory activity of cabozantinib is due to a longer HB domain than that of sorafenib. Based on pharmacophore of cabozantinib analogues, we designed new dual VEGFR-2/c-Met TKs. We synthesized the target compounds via a new single pot three-component reaction. The cytotoxic activity of synthesized compounds was …

Authors

Abdelfattah Hassan,Ahmed M Mosallam,Amal OA Ibrahim,Mohamed Badr,Aboubakr H Abdelmonsef

Journal

Scientific Reports

Published Date

2023/10/30

Design, synthesis in vitro and in vivo evaluation of new diaryltriazoles carboxylic and hydroxamic acid derivatives as inhibitors of tumor necrosis alpha converting enzyme (TACE)

Combining two peptides addressing two different receptors to a heterobivalent peptidic ligand (HBPL) is thought to enable an improved tumor-targeting sensitivity and thus tumor visualization, compared to monovalent peptide ligands. In the case of melanoma, the Melanocortin-1 receptor (MC1R), which is stably overexpressed in the majority of primary malignant melanomas, and integrin αvβ3, which is involved in lymph node metastasis and therefore has an important role in the transition from local to metastatic disease, are important target receptors. Thus, if a radiolabeled HBPL could be developed that was able to bind to both receptor types, the early diagnosis and correct staging of the disease would be significantly increased. Here, we report on the design, synthesis, radiolabeling and in vitro and in vivo testing of different SiFAlin-modified HBPLs (SiFA = silicon fluoride acceptor), consisting of an MC1R-targeting (GG-Nle-c(DHfRWK)) and an integrin αvβ3-affine peptide (c(RGDfK)), being connected by a symmetrically branching framework including linkers of differing length and composition. Kit-like 18F-radiolabeling of the HBPLs 1–6 provided the labeled products [18F]1–[18F]6 in radiochemical yields of 27–50%, radiochemical purities of ≥95% and non-optimized molar activities of 17–51 GBq/μmol within short preparation times of 25 min. Besides the evaluation of radiotracers regarding logD(7.4) and stability in human serum, the receptor affinities of the HBPLs were investigated in vitro on cell lines overexpressing integrin αvβ3 (U87MG cells) or the MC1R (B16F10). Based on these results, the most promising compounds [18F]2, showing …

Authors

Xia Cheng,Ralph Hübner,Valeska von Kiedrowski,Gert Fricker,Ralf Schirrmacher,Carmen Wängler,Björn Wängler

Journal

Pharmaceuticals

Published Date

2021/6/7

Design, synthesis, in vitro antiproliferative evaluation and in silico studies of new VEGFR-2 inhibitors based on 4-piperazinylquinolin-2 (1H)-one scaffold

Angiogenesis is essential in the growth of solid tumors which need oxygen and nutrients supply to grow in size. The VEGF/VEGFR-2 signaling pathway plays an important role in tumor angiogenesis. Sorafenib is an FDA approved cancer therapeutic with activity against many protein kinases, including VEGFR. We designed 4-piperazinylquinolin-2(1H)-ones with variable aromatic moieties and Mannich bases as Sorafenib analogues as potential inhibitors of angiogenesis. In this study, we investigated the impact of replacing the linker aromatic ring with cyclic tertiary amines and the effect of incorporation of variably substituted distal rings. We hypothesized that cyclic tertiary amines would improve pharmacokinetic properties and contribute to enzyme interactions. Two series of piperazinylquinolinone-based compounds were synthesized, characterized, and evaluated for bioactivity against adenocarcinoma EKVX …

Authors

Abdelfattah Hassan,Mohamed Badr,Dalia Abdelhamid,Heba A Hassan,Mohammed AS Abourehab,Gamal El‐Din A Abuo‐Rahma

Journal

Bioorganic Chemistry

Published Date

2022/3/1

SYNTHETIC APPROACHES TOWARD CERTAIN STRUCTURALLY RELATED ANTIMICROBIAL THIAZOLE DERIVATIVES (2010-2020)

SYNTHETIC APPROACHES TOWARD CERTAIN STRUCTURALLY RELATED ANTIMICROBIAL THIAZOLE DERIVATIVES (2010-2020) | CiNii Research CiNii 国立情報学研究所 学術情報 ナビゲータ[サイニィ] 詳細へ移動 検索フォームへ移動 論文・データをさがす 大学図書館の本をさがす 日本の博士論文をさがす English 検索 タイトル 人物/団体名 所属機関 ISSN DOI 期間 ~ 本文リンク 本文リンクあり データソース JaLC IRDB Crossref DataCite NDL NDL-Digital RUDA JDCat NINJAL CiNii Articles CiNii Books CiNii Dissertations DBpedia Nikkei BP KAKEN Integbio MDR PubMed LSDB Archive 公共データカタログ ムーンショット型研究開発事業 すべて 研究データ 論文 本 博士論文 プロジェクト SYNTHETIC APPROACHES TOWARD CERTAIN STRUCTURALLY RELATED ANTIMICROBIAL THIAZOLE DERIVATIVES (2010-2020) Abdelfattah Hassan Heba A. Hassan Dalia Abdelhamid Gamal El-Din A. Abuo-Rahma この論文をさがす NDL …

Authors

Abdelfattah Hassan,Heba A Hassan,Dalia Abdelhamid,Gamal El-Din A Abuo-Rahma

Journal

Heterocycles: an international journal for reviews and communications in heterocyclic chemistry

Published Date

2021/9/1

Novel 4-(piperazin-1-yl) quinolin-2 (1H)-one bearing thiazoles with antiproliferative activity through VEGFR-2-TK inhibition

A new series of 2-(4-(2-oxo-1,2-dihydroquinolin-4-yl)piperazin-1-yl)-N-(4-phenylthiazol-2-yl)acetamide derivatives were synthesized and evaluated for anticancer activity. All target compounds showed anticancer activity higher than that of their 2-oxo-4-piperazinyl-1,2-dihydroquinolin-2(1H)-one precursors. Multidose testing of target compounds was performed against breast cancer T-47D cell line. Five compounds showed higher cytotoxic activity than Staurosporine. The dihalogenated derivative showed the best cytotoxic activity with IC50 2.73 ± 0.16 µM. In addition, the VEGFR-2 inhibitory activity of all synthetic compounds was evaluated. Two compounds of 6-fluoro-4-(piperazin-1-yl)quinolin-2(1H)-ones showed inhibitory activity comparable to sorafenib with IC50 46.83 ± 2.4, 51.09 ± 2.6 and 51.41 ± 2.3 nM, respectively. The cell cycle analysis of two compounds namely, 2-(4-(6-fluoro-2-oxo-1,2-dihydroquinolin-4 …

Authors

Abdelfattah Hassan,Mohamed Badr,Heba A Hassan,Dalia Abdelhamid,Gamal El‐Din A Abuo‐Rahma

Journal

Bioorganic & Medicinal Chemistry

Published Date

2021/6/15

Abdelfattah Hassan FAQs

What is Abdelfattah Hassan's h-index at South Valley University?

The h-index of Abdelfattah Hassan has been 4 since 2020 and 4 in total.

What are Abdelfattah Hassan's top articles?

The articles with the titles of

Design and biological evaluation of 3-substituted quinazoline-2,4(1H,3H)-dione derivatives as dual c-Met/VEGFR-2-TK inhibitors

Novel 3-phenylquinazolin-2,4(1H,3H)-diones as dual VEGFR-2/c-Met-TK inhibitors: design, synthesis, and biological evaluation

Design, synthesis in vitro and in vivo evaluation of new diaryltriazoles carboxylic and hydroxamic acid derivatives as inhibitors of tumor necrosis alpha converting enzyme (TACE)

Design, synthesis, in vitro antiproliferative evaluation and in silico studies of new VEGFR-2 inhibitors based on 4-piperazinylquinolin-2 (1H)-one scaffold

SYNTHETIC APPROACHES TOWARD CERTAIN STRUCTURALLY RELATED ANTIMICROBIAL THIAZOLE DERIVATIVES (2010-2020)

Novel 4-(piperazin-1-yl) quinolin-2 (1H)-one bearing thiazoles with antiproliferative activity through VEGFR-2-TK inhibition

are the top articles of Abdelfattah Hassan at South Valley University.

What are Abdelfattah Hassan's research interests?

The research interests of Abdelfattah Hassan are: Medicinal Chemistry

What is Abdelfattah Hassan's total number of citations?

Abdelfattah Hassan has 59 citations in total.

What are the co-authors of Abdelfattah Hassan?

The co-authors of Abdelfattah Hassan are Mohammed AS Abourehab, Dalia Abdelhamid, Aboubakr H. Abdelmonsef, Dr Mohamed badr, Dr. Sameh Elnabtity.

    Co-Authors

    H-index: 29
    Mohammed AS Abourehab

    Mohammed AS Abourehab

    Umm Al-Qura University

    H-index: 20
    Dalia Abdelhamid

    Dalia Abdelhamid

    Minia University

    H-index: 18
    Aboubakr H. Abdelmonsef

    Aboubakr H. Abdelmonsef

    South Valley University

    H-index: 9
    Dr Mohamed badr

    Dr Mohamed badr

    Menoufia University

    H-index: 8
    Dr. Sameh Elnabtity

    Dr. Sameh Elnabtity

    Zagazig University

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