Structure-activity relationship of flavonoids for inhibition of epidermal growth factor-induced transformation of JB6 Cl 41 cells

2007 ◽  
Vol 46 (6) ◽  
pp. 436-445 ◽  
Author(s):  
Daisuke Ichimatsu ◽  
Masaaki Nomura ◽  
Seiji Nakamura ◽  
Shuzo Moritani ◽  
Koichi Yokogawa ◽  
...  
Keyword(s):  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Epidermal Growth ◽  
Relationship Of

Therapeutic Journey of Pyrazolines as EGFR Tyrosine Kinase Inhibitors: An Insight into Structure-Activity Relationship

2020 ◽  
Vol 16 (9) ◽  
pp. 1260-1272
Author(s):  
Navdeep Singh ◽  
Monika Gupta
Keyword(s):  
Epidermal Growth Factor Receptor ◽  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Tyrosine Kinase ◽  
Inhibitory Activity ◽  
Growth Factor Receptor ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Epidermal Growth

Background: Pyrazolines are five-membered heterocycles with two adjacent nitrogen atoms present in the ring and they have attracted many researchers all over the world to assess their potential therapeutic significance. Pyrazolines are known for their crucial role in numerous diseases like cancer via various mechanisms. Pyrazoline and its derivatives have been found to have potent anticancer activity by inhibiting EGFR (Epidermal Growth Factor Receptor Tyrosine Kinase) and other types of RTKs. Rapid advances in the understanding of cellular signaling by EGFR in normal and malignant cells have brought to light the EGFR as a selective anticancer target. The review enlists some recently developed pyrazolines as EGFR tyrosine kinase inhibitor along with their structure-activity relationships. Methods: The structure-activity relationship of different pyrazoline derivatives was discussed along with their epidermal growth factor receptor inhibitory activity. Both review and research articles have been considered and cited in the paper. Results: Pyrazolines have assisted medicinal chemistry by their diverse biological activities which make them a beneficial scaffold. The structure-activity relationship studies on pyrazolines revealed that the structural characteristics and different substitutions on pyrazoline ring alter the EGFR inhibitory activity. Conclusion: In the present review, pyrazoline derivatives with EGFR kinase inhibitory activity are described based on their structure-activity relationships based on their structural substitution pattern around the pyrazoline scaffold.

Structure-activity relationship of (-) mammea A/BB derivatives against Leishmania amazonensis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
MA Brenzan ◽  
CV Nakamura ◽  
BPD Filho ◽  
T Ueda-Nakamura ◽  
MCM Young ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Leishmania Amazonensis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of

Antineoplastic Activity, Structural Modification, Synthesis and Structure-activity Relationship of Dammarane-type Ginsenosides: An Overview

2019 ◽  
Vol 23 (5) ◽  
pp. 503-516 ◽  
Author(s):  
Qiang Zhang ◽  
Xude Wang ◽  
Liyan Lv ◽  
Guangyue Su ◽  
Yuqing Zhao
Keyword(s):  
Structural Modification ◽  
Gastrointestinal Disease ◽  
Structure Activity Relationship ◽  
Cerebrovascular Diseases ◽  
Activity Relationship ◽  
Cycle Arrest ◽  
Structure Activity ◽  
Wide Range ◽  
Structural Association ◽  
Relationship Of

Dammarane-type ginsenosides are a class of tetracyclic triterpenoids with the same dammarane skeleton. These compounds have a wide range of pharmaceutical applications for neoplasms, diabetes mellitus and other metabolic syndromes, hyperlipidemia, cardiovascular and cerebrovascular diseases, aging, neurodegenerative disease, bone disease, liver disease, kidney disease, gastrointestinal disease and other conditions. In order to develop new antineoplastic drugs, it is necessary to improve the bioactivity, solubility and bioavailability, and illuminate the mechanism of action of these compounds. A large number of ginsenosides and their derivatives have been separated from certain herbs or synthesized, and tested in various experiments, such as anti-proliferation, induction of apoptosis, cell cycle arrest and cancer-involved signaling pathways. In this review, we have summarized the progress in structural modification, shed light on the structure-activity relationship (SAR), and offered insights into biosynthesis-structural association. This review is expected to provide a preliminary guide for the modification and synthesis of ginsenosides.

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