scholarly journals Antitumor Agents 288: Design, Synthesis, SAR, and Biological Studies of Novel Heteroatom-Incorporated Antofine and Cryptopleurine Analogues as Potent and Selective Antitumor Agents

2011 ◽  
Vol 54 (14) ◽  
pp. 5097-5107 ◽  
Author(s):  
Xiaoming Yang ◽  
Qian Shi ◽  
Shuenn-Chen Yang ◽  
Chi-Yuan Chen ◽  
Sung-Liang Yu ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Design Synthesis ◽  
Biological Studies

scholarly journals Novel Steroidal 5α,8α-Endoperoxide Derivatives with Semicarbazone/Thiosemicarbazone Side-chain as Apoptotic Inducers through an Intrinsic Apoptosis Pathway: Design, Synthesis and Biological Studies

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1209 ◽  
Author(s):  
Liwei Ma ◽  
Haijun Wang ◽  
Jing Wang ◽  
Lei Liu ◽  
Song Zhang ◽  
...  
Keyword(s):  
Hepg2 Cells ◽  
Antitumor Agents ◽  
Human Cancer ◽  
Side Chain ◽  
Design Synthesis ◽  
Apoptosis Pathway ◽  
Human Cancer Cell Lines ◽  
Biological Studies ◽  
Intrinsic Apoptosis Pathway

A series of novel steroidal 5α,8α-endoperoxide derivatives bearing semicarbazone (7a–g) or thiosemicarbazone (7h–k) side chain were designed, synthesized and evaluated for their cytotoxicities in four human cancer cell lines (HepG2, HCT-116, MCF-7, and A549) using the MTT assay in vitro. The results showed that compound 7j exhibited significant cytotoxic activity against HepG2 cells (IC50 = 3.52 μM), being more potent than ergosterol peroxide. Further cellular mechanism studies in HepG2 cells indicated that compound 7j triggered the mitochondrial-mediated apoptosis by decreasing mitochondrial membrane potential (MMP), which was associated with up-regulation of Bax, down-regulation of Bcl-2, activation levels of the caspase cascade, and formation of reactive oxygen species (ROS). The above findings indicated that compound 7j may be used as a promising skeleton for antitumor agents with improved efficacy.

Lavendamycin Antitumor Agents: Structure-Based Design, Synthesis, and NAD(P)H:Quinone Oxidoreductase 1 (NQO1) Model Validation with Molecular Docking and Biological Studies

2008 ◽  
Vol 51 (11) ◽  
pp. 3104-3115 ◽  
Author(s):  
Mary Hassani ◽  
Wen Cai ◽  
Katherine H. Koelsch ◽  
David C. Holley ◽  
Anthony S. Rose ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Model Validation ◽  
Antitumor Agents ◽  
Design Synthesis ◽  
Biological Studies

scholarly journals Zinc Complexes with Nitrogen Donor Ligands as Anticancer Agents

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5814
Author(s):  
Marina Porchia ◽  
Maura Pellei ◽  
Fabio Del Bello ◽  
Carlo Santini
Keyword(s):  
Human Body ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Physiological Role ◽  
Zinc Complexes ◽  
Redox Activity ◽  
Donor Ligands ◽  
Design Synthesis ◽  
Biological Studies ◽  
Ligands Exchange

The search for anticancer metal-based drugs alternative to platinum derivatives could not exclude zinc derivatives due to the importance of this metal for the correct functioning of the human body. Zinc, the second most abundant trace element in the human body, is one of the most important micro-elements essential for human physiology. Its ubiquity in thousands of proteins and enzymes is related to its chemical features, in particular its lack of redox activity and its ability to support different coordination geometries and to promote fast ligands exchange. Analogously to other trace elements, the impairment of its homeostasis can lead to various diseases and in some cases can be also related to cancer development. However, in addition to its physiological role, zinc can have beneficial therapeutic and preventive effects on infectious diseases and, compared to other metal-based drugs, Zn(II) complexes generally exert lower toxicity and offer few side effects. Zinc derivatives have been proposed as antitumor agents and, among the great number of zinc coordination complexes which have been described so far, this review focuses on the design, synthesis and biological studies of zinc complexes comprising N-donor ligands and that have been reported within the last five years.

Design, Synthesis of Novel Quinazolone Alkaloids Derivatives as Potential Antitumor Agents

2011 ◽  
Vol 7 (4) ◽  
pp. 295-300
Author(s):  
Youguang Zheng ◽  
Min Sun ◽  
Yi Liu ◽  
Mingdong Li ◽  
Min Ji
Keyword(s):  
Antitumor Agents ◽  
Design Synthesis ◽  
Potential Antitumor

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.

1-Methyl-3H-pyrazolo[1,2-a]benzo[1,2,3,4]tetrazin-3-ones. Design, Synthesis, and Biological Activity of New Antitumor Agents

2005 ◽  
Vol 48 (8) ◽  
pp. 2859-2866 ◽  
Author(s):  
Anna Maria Almerico ◽  
Francesco Mingoia ◽  
Patrizia Diana ◽  
Paola Barraja ◽  
Antonino Lauria ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis

scholarly journals Design, Synthesis, and Biological Activity of Sulfonamide Analogues of Antofine and Cryptopleurine as Potent and Orally Active Antitumor Agents

2015 ◽  
Vol 58 (19) ◽  
pp. 7749-7762 ◽  
Author(s):  
Yongseok Kwon ◽  
Jayoung Song ◽  
Honggu Lee ◽  
Eun-Yeong Kim ◽  
Kiho Lee ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antitumor Agents ◽  
Design Synthesis ◽  
Orally Active

ChemInform Abstract: Antitumor Agents. Part 202. Novel 2′-Amino Chalcones: Design, Synthesis, and Biological Evaluation.

ChemInform ◽  
2010 ◽  
Vol 31 (29) ◽  
pp. no-no
Author(s):  
Yi Xia ◽  
Zheng-Yu Yang ◽  
Peng Xia ◽  
Kenneth F. Bastow ◽  
Yuka Nakanishi ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

ChemInform Abstract: Design, Synthesis, and Biological Testing of 4β-[(4-Substituted)-1,2,3-triazol-1-yl]podophyllotoxin Analogues as Antitumor Agents.

ChemInform ◽  
2008 ◽  
Vol 39 (22) ◽  
Author(s):  
Pitta B. Reddy ◽  
David V. Paul ◽  
Satyam K. Agrawal ◽  
Ajit K. Saxena ◽  
Halmuthur M. S. Kumar ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Testing ◽  
Design Synthesis
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