Design, synthesis, and evaluation of a water-soluble antofine analogue with high antiproliferative and antitumor activity

2013 ◽  
Vol 21 (4) ◽  
pp. 1006-1017 ◽  
Author(s):  
Yongseok Kwon ◽  
Jayoung Song ◽  
Boeun Lee ◽  
Jinkyung In ◽  
Hohyun Song ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Design Synthesis

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

RSC Advances ◽  
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.

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

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

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

2014 ◽  
Vol 58 (1) ◽  
pp. 237-251 ◽  
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

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

Molecules ◽  
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.

Design, synthesis, and antitumor activity evaluation of steroidal oximes

2021 ◽  
pp. 116360
Author(s):  
Ana R. Gomes ◽  
Ana S. Pires ◽  
Ana M. Abrantes ◽  
Ana C. Gonçalves ◽  
Saul C. Costa ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Design Synthesis ◽  
Activity Evaluation

Novel water soluble phosphate prodrugs of taxol® possessing in vivo antitumor activity

1993 ◽  
Vol 3 (8) ◽  
pp. 1761-1766 ◽  
Author(s):  
Yasutsugu Ueda ◽  
Amarendra B. Mikkilineni ◽  
Jay O. Knipe ◽  
William C. Rose ◽  
Anna Maria Casazza ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Water Soluble ◽  
Soluble Phosphate ◽  
In Vivo Antitumor Activity

Design, synthesis and antitumor activity evaluation of novel HDAC inhibitors with tetrahydrobenzothiazole as the skeleton

2021 ◽  
Vol 108 ◽  
pp. 104652
Author(s):  
Simin Sun ◽  
Wenwen Zhao ◽  
Yongliang Li ◽  
Ziwei Chi ◽  
Xixi Fang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Hdac Inhibitors ◽  
Design Synthesis ◽  
Activity Evaluation

scholarly journals Design, synthesis and biological evaluation of imidazopyridine–propenone conjugates as potent tubulin inhibitors

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 1000-1006 ◽  
Author(s):  
Ibrahim Bin Sayeed ◽  
V. Lakshma Nayak ◽  
Mohd Adil Shareef ◽  
Neeraj Kumar Chouhan ◽  
Ahmed Kamal
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Human Cancer Cell Lines ◽  
Tubulin Inhibitors ◽  
Synthesis And Biological Evaluation

A library of imidazopyridine–propenone conjugates (8a–8u) were synthesized and evaluated for their antitumor activity against four human cancer cell lines.

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