A Review on Camptothecin Analogs with Promising Cytotoxic Profile

2019 ◽  
Vol 18 (13) ◽  
pp. 1796-1814 ◽  
Author(s):  
Sk. Abdul Amin ◽  
Nilanjan Adhikari ◽  
Tarun Jha ◽  
Shovanlal Gayen
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Structure Property ◽  
Cytotoxic Potential ◽  
Structure Property Relationships ◽  
Structure Activity ◽  
Camptothecin Analogs ◽  
Pharmacokinetic Properties ◽  
Quantitative Structure Activity Relationships

Camptothecin (CPT), obtained from Camptotheca acuminata (Nyssaceae), is a quinoline type of alkaloid. Apart from various traditional uses, it is mainly used as a potential cytotoxic agent acting against a variety of cancer cell lines. Though searches have been continued for last six decades, still it is a demanding task to design potent and cytotoxic CPTs. Different CPT analogs are synthesized to enhance the cytotoxic potential as well as to increase the pharmacokinetic properties of these analogs. Some of these analogs were proven to be clinically effective in different cancer cell lines. In this article, different CPT analogs have been highlighted extensively to get a detail insight about the structure-property relationships as well as different quantitative structure-activity relationships (QSARs) modeling of these analogs are also discussed. This study may be beneficial for designing newer CPT analogs in future.

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.

Structure–activity studies of quinuclidinone analogs as anti-proliferative agents in lung cancer cell lines

2006 ◽  
Vol 16 (5) ◽  
pp. 1156-1159 ◽  
Author(s):  
Ahmed Malki ◽  
Aravinda B. Pulipaka ◽  
Susan C. Evans ◽  
Stephen C. Bergmeier
Keyword(s):  
Lung Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Lung Cancer Cell ◽  
Structure Activity

scholarly journals Thiourea and Guanidine Compounds and their Iridium Complexes in Drug-Resistant Cancer Cell Lines: Structure-Activity Relationships and Direct Luminescent Imaging

2019 ◽  
Author(s):  
Samuel J. Thomas ◽  
Barbora Balonova ◽  
Jindrich Cinatl ◽  
Mark Wass ◽  
Christopher Serpell ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Nature Medicine ◽  
Cancer Cell Lines ◽  
Resistance Mechanisms ◽  
New Drugs ◽  
Iridium Complexes ◽  
Safety Issues ◽  
Structure Activity Relationships ◽  
Structure Activity

<p>Thiourea and guanidine units are found in nature, medicine, and materials. Their continued exploration in applications as diverse as cancer therapy, sensors, and electronics means that their toxicity is an important consideration. We have systematically synthesised a set of thiourea compounds and their guanidine analogues, and elucidated structure-activity relationships in terms of cellular toxicity in three ovarian cancer cell lines and their cisplatin-resistant sub-lines. We have been able to use the intrinsic luminescence of iridium complexes to visualise the effect of both structure alteration and cellular resistance mechanisms. These findings provide starting points for the development of new drugs and consideration of safety issues for novel thiourea- and guanidine-based materials.</p>

Comprehensive Study of Sansalvamide A Derivatives and their Structure–Activity Relationships against Drug-Resistant Colon Cancer Cell Lines

2008 ◽  
Vol 51 (3) ◽  
pp. 530-544 ◽  
Author(s):  
Katerina Otrubova ◽  
Gerald Lushington ◽  
David Vander Velde ◽  
Kathleen L. McGuire ◽  
Shelli R. McAlpine
Keyword(s):  
Colon Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Colon Cancer Cell ◽  
Drug Resistant ◽  
Structure Activity ◽  
Colon Cancer Cell Lines ◽  
Sansalvamide A ◽  
Comprehensive Study

scholarly journals The cytotoxic potential of cationic triangulenes against tumour cells

MedChemComm ◽  
2019 ◽  
Vol 10 (11) ◽  
pp. 1881-1891 ◽  
Author(s):  
Euphemia Leung ◽  
Lisa I. Pilkington ◽  
Mohinder M. Naiya ◽  
David Barker ◽  
Ayesha Zafar ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Tumour Cells ◽  
Cytotoxic Potential ◽  
Dna Intercalators

Close-shelled carbocations DNA intercalators Pr-ADOTA and Pr-DAOTA are very cytotoxic against the cancer cell lines MDA-MB-231 (breast) and HCT116 (colon).

The Uses of Dimedone for the Synthesis of Thiophene, Thiazole and Annulated Derivatives with Antitumor, Pim-1 Kinase Inhibitions, PAINS Evaluations and Molecular Docking

2021 ◽  
Vol 21 ◽  
Author(s):  
Wagnat W. Wardakhan ◽  
Amira M. Elmetwally ◽  
Abeer A. Mohamed ◽  
Rafat M. Mohareb
Keyword(s):  
Molecular Docking ◽  
Cell Lines ◽  
Cancer Cell ◽  
Tyrosine Kinases ◽  
Heterocyclic Compounds ◽  
Cancer Cell Lines ◽  
Strong Impact ◽  
Structure Activity ◽  
Anti Cancer ◽  
Target Molecules

Background: Dimedone is considered as one of the most important class of compounds belonging to cyclohexan-1,3-dione. Such group of compounds were considered as precursors for many pharmaceutically active heterocyclic compounds. Objective: The target molecules through this work were synthesized from arylhydrazones of dimedone with different substituent’s enhancing study of their structure activity relationship. Methods: Arylhydrazones of dimedones were subjected to a series of heterocyclization reactions affording annulated compounds. The antiproliferative activities of the synthesized molecules were evaluated against six cancer cell lines. In addition, inhibitions toward tyrosine kinases, Pim-1 kinases and PAINS of the most active compounds were also studied. c-Met enzymatic inhibitions and molecular docking studied were carried for three compounds. Results: Anti-cancer evaluations together with tyrosine and Pim-1 kinases of most of the synthesized compounds were carried out through this work. The study revealed that changing of substituent had a strong impact on the activity of themolecule. Conclusion: Many of the synthesized compounds exhibited high inhibitions toward the six cancer cell lines and this will encourage further work through the synthesis of target molecule with the same ring systems. The three compounds 7b, 8c and 12b that revealed excellent inhibitions were tested against c-Met kinase and their molecular modelling was expressed.

Sign in / Sign up

Export Citation Format

Share Document