Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity

Aim: Encouraged by the antitumor activity exhibited by triazolylpeptidyl penicillins, we decided to synthesize and evaluate a library of peptoid analogs. Results: The replacement of the dipeptide unit of the reference compound, TAP7f, was investigated. In addition, the effect of the triazole linking group on the biological activity of these new derivatives was evaluated, exchanging it with a glycine spacer. The cytotoxic effect of the library compounds was determined in the B16-F0 cell line and compared with the effects on normal murine mammary gland cells. Conclusion: Among the tested compounds, peptoid 4e exhibited the highest antiproliferative activity.

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Faculty Opinions recommendation of Design, synthesis, and biological activity of a family of novel ceramide analogues in chemoresistant breast cancer cells.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1165832.628901 ◽

2009 ◽

Author(s):

Jane Endicott ◽

Christiane Riedinger

Keyword(s):

Breast Cancer ◽

Biological Activity ◽

Cancer Cells ◽

Breast Cancer Cells ◽

Design Synthesis

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Design, Synthesis and Biological Activity of Aromatic Diketone Derivatives as HIV-1 Integrase Inhibitors

Medicinal Chemistry ◽

10.2174/1573406410666140829154131 ◽

2015 ◽

Vol 11 (2) ◽

pp. 180-187 ◽

Cited By ~ 2

Author(s):

Liming Hu ◽

Zhipeng Li ◽

Zhanyang Wang ◽

Gengxin Liu ◽

Xianzhuo He ◽

...

Keyword(s):

Biological Activity ◽

Integrase Inhibitors ◽

Design Synthesis ◽

Hiv 1

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Discovery of pyrano[2,3-d]pyrimidine-2,4-dione derivatives as novel PARP-1 inhibitors: design, synthesis and antitumor activity

RSC Advances ◽

10.1039/d0ra10321g ◽

2021 ◽

Vol 11 (8) ◽

pp. 4454-4464

Author(s):

Nour E. A. Abd El-sattar ◽

Eman H. K. Badawy ◽

Eman Z. Elrazaz ◽

Nasser S. M. Ismail

Keyword(s):

Cell Death ◽

Dna Repair ◽

Antitumor Activity ◽

Cancer Cell ◽

Cytotoxic Agents ◽

Repair Mechanism ◽

Design Synthesis ◽

Parp 1

PARP-1 are involved in DNA repair damage and so PARP-1 inhibitors have been used as potentiators in combination with DNA damaging cytotoxic agents to compromise the cancer cell DNA repair mechanism, resulting in genomic dysfunction and cell death.

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Design, synthesis, and antitumor activity of PLGA nanoparticles incorporating a discovered benzimidazole derivative as EZH2 inhibitor

Chemico-Biological Interactions ◽

10.1016/j.cbi.2021.109530 ◽

2021 ◽

pp. 109530

Author(s):

Hoda A. Elkot ◽

Ibrahim Ragab ◽

Noha M. Saleh ◽

Mohamed N. Amin ◽

Sara T. Al-Rashood ◽

...

Keyword(s):

Antitumor Activity ◽

Benzimidazole Derivative ◽

Plga Nanoparticles ◽

Design Synthesis

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Design, Synthesis, and Evaluation of Novel Imidazo[1,2-a][1,3,5]triazines and Their Derivatives as Focal Adhesion Kinase Inhibitors with Antitumor Activity

Journal of Medicinal Chemistry ◽

10.1021/jm500784e ◽

2014 ◽

Vol 58 (1) ◽

pp. 237-251 ◽

Cited By ~ 25

Author(s):

Pascal Dao ◽

Nikaia Smith ◽

Céline Tomkiewicz-Raulet ◽

Expédite Yen-Pon ◽

Marta Camacho-Artacho ◽

...

Keyword(s):

Antitumor Activity ◽

Focal Adhesion Kinase ◽

Focal Adhesion ◽

Kinase Inhibitors ◽

Design Synthesis

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Design, Synthesis, and Antitumor Activity of Olmutinib Derivatives Containing Acrylamide Moiety

Molecules ◽

10.3390/molecules26103041 ◽

2021 ◽

Vol 26 (10) ◽

pp. 3041

Author(s):

Xiaohan Hu ◽

Sheng Tang ◽

Feiyi Yang ◽

Pengwu Zheng ◽

Shan Xu ◽

...

Keyword(s):

Antitumor Activity ◽

Cell Lines ◽

Cancer Cell ◽

Antitumor Agents ◽

Cancer Cell Lines ◽

Design Synthesis ◽

Structure Activity ◽

Excellent Activity ◽

Ic50 Values ◽

Mcf 7

Two series of olmutinib derivatives containing an acrylamide moiety were designed and synthesized, and their IC50 values against cancer cell lines (A549, H1975, NCI-H460, LO2, and MCF-7) were evaluated. Most of the compounds exhibited moderate cytotoxic activity against the five cancer cell lines. The most promising compound, H10, showed not only excellent activity against EGFR kinase but also positive biological activity against PI3K kinase. The structure–activity relationship (SAR) suggested that the introduction of dimethylamine scaffolds with smaller spatial structures was more favorable for antitumor activity. Additionally, the substitution of different acrylamide side chains had different effects on the activity of compounds. Generally, compounds H7 and H10 were confirmed as promising antitumor agents.

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Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

MedChemComm ◽

10.1039/c8md00396c ◽

2018 ◽

Vol 9 (11) ◽

pp. 1905-1909 ◽

Cited By ~ 7

Author(s):

Faustine d'Orchymont ◽

Jeannine Hess ◽

Gordana Panic ◽

Marta Jakubaszek ◽

Lea Gemperle ◽

...

Keyword(s):

Biological Activity ◽

Antimalarial Drug ◽

Biological Evaluation ◽

Design Synthesis ◽

Drug Candidates ◽

Derivatives Of

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.

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